Synthetic growth hormone secretagogues were found to act on a G protein-coupled receptor present in pituitary and hypothalamus of swine and humans, and its characterization defined a neuroendocrine pathway for pulsatile GH release [6]. The endogenous ligand of this receptor was later identified as ghrelin, a 28-amino-acid acylated peptide from stomach that releases GH in vivo and in vitro [7]. A review described growth hormone secretagogues as acting as functional somatostatin antagonists that potentiate GHRH and enhance pulsatile GH secretion [9].
In GH3 pituitary cells, GHRP-6 stimulated GH secretion in a time- and dose-dependent manner and enhanced the effect of GHRH [2]. It induced CREB phosphorylation, and GH secretion was reduced by PKC inhibitors and by PKC sigma knockdown, leading the authors to conclude that PKC sigma mediates both effects [2].
In the rat, receptor mRNA was prominent in the arcuate and ventromedial hypothalamic nuclei and hippocampus, with little signal in the pituitary under the conditions used [8]. Continuous exposure to GHRP-6 in normal female rats did not change receptor expression in the arcuate or ventromedial nuclei [8].
","origin":"Synthetic hexapeptide with the sequence His-D-Trp-Ala-Trp-D-Phe-Lys-NH2 [5]","published":true,"reg_status":"not_approved","regulatory":{"fda":"GHRP-6 is not approved by the US FDA for any use [10]. FDA's categorization of nominated 503A bulk drug substances (updated May 14, 2026) lists GHRP-6 in Category 3, bulk drug substances nominated without adequate support [10].","wada":"The WADA 2026 Prohibited List names GHRP-6 under S2.2.4 (growth hormone releasing factors, including GH-releasing peptides); S2 substances are prohibited at all times, in and out of competition, and are non-Specified Substances [11]."},"research":{"human":"In children with short stature and adults with GH deficiency, the GH response to GHRP-6 was lower than in normal children but overlapped considerably, and an almost complete blockade was reported in patients with pituitary stalk transection [1]. In 49 patients with suspected hypothalamic or pituitary disease and 20 healthy controls, GHRP-6 alone was reported as highly specific but of limited sensitivity compared with the insulin tolerance test, and the authors observed no side effects during testing [3]. In 6 healthy men, GHRP-6 raised plasma GH, slightly raised prolactin and cortisol after administration, and repeated short-term administration was followed by a rise in IGF-I [5].","animal":"The sources reviewed contain one rat study in which continuous GHRP-6 exposure did not alter hypothalamic receptor expression in normal females; no animal efficacy studies of GHRP-6 are summarized here [8].","in_vitro":"In cultured GH3 pituitary cells, GHRP-6 stimulated GH secretion and CREB phosphorylation, with PKC sigma implicated as a mediator [2]."},"slug":"ghrp-6","status_note":"Not approved by the US FDA for any use [10]; US FDA lists GHRP-6 in Category 3 of nominated 503A bulk drug substances, those nominated without adequate support [10].","unknowns":"No data on long-term human exposure were identified in the sources reviewed, and the human studies are small and short. Controlled trials of treatment outcomes were not identified here. The sources reviewed contain no animal toxicology summary for GHRP-6.","id":"6ada7ecb0097a56525f6b8dd","created_date":"2026-10-22T21:23:23.421000","updated_date":"2026-10-23T17:31:40.835000"},{"adverse_events":[{"event":"Any treatment-emergent adverse event","frequency":"87.5% ipamorelin vs 94.8% placebo","population":"Phase 2 trial, adults after bowel resection","severity":"Mostly mild to moderate and related to surgery or underlying disease, per the authors","ref":4},{"event":"Hypokalemia","frequency":"12.5% vs 3.4% placebo","population":"Same trial, as summarized by FDA","severity":"Not specified","ref":7},{"event":"Insomnia","frequency":"10.7% vs 5.2% placebo","population":"Same trial, as summarized by FDA","severity":"Not specified","ref":7},{"event":"Hyperglycemia at discharge","frequency":"14.3% vs 8.6% placebo","population":"Same trial, as summarized by FDA","severity":"Not specified","ref":7},{"event":"Serious adverse events (infection, anastomotic leak, readmission)","frequency":"17.9% vs 15.5% placebo","population":"Same trial, as summarized by FDA","severity":"Includes two fatal events in the ipamorelin arm (postoperative complications after colon cancer resection); FDA considered the relationship to the drug unclear","ref":7},{"event":"Nausea, vomiting, abdominal distention","frequency":"Similar in both groups, numerically lower with ipamorelin","population":"Same trial","severity":"Not specified","ref":7}],"components":[],"compound_class":"Ghrelin receptor agonist; growth hormone secretagogue (GHRP-like pentapeptide)","evidence_grade":"B","faqs":[{"q":"What is ipamorelin?","a":"It is a synthetic pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) that stimulates growth hormone release through a GHRP-like receptor and has been described as a ghrelin receptor agonist [1, 2]."},{"q":"Is ipamorelin US FDA-approved?","a":"No. US FDA states there are no US FDA-approved drug products containing ipamorelin, and it proposed in 2024 not to add it to the 503A bulks list [7, 11]."},{"q":"How is ipamorelin different from GHRP-6 and GHRP-2?","a":"In swine, GHRP-6 and GHRP-2 increased ACTH and cortisol, while ipamorelin did not raise them beyond the GHRH response, and the authors described it as selective for GH release [1]."},{"q":"What human research exists?","a":"A pharmacokinetic and pharmacodynamic study in healthy male volunteers and two registered phase 2 trials in postoperative ileus after bowel resection; the published one found no significant efficacy difference from placebo [3, 4, 5, 6]."},{"q":"How long does ipamorelin act?","a":"In healthy men, the terminal half-life was about 2 hours and GH release was a single episode peaking at about 0.67 hours [3]."},{"q":"What safety concerns has FDA raised?","a":"FDA cited higher rates of hypokalemia, insomnia and hyperglycemia and two deaths of unclear relationship in the ileus trial, potential immunogenicity, and a lack of data for other routes [7, 8]."},{"q":"Did ipamorelin work for postoperative ileus?","a":"In rats, it shortened time to first bowel movement [2]. In the human phase 2 trial, median time to first tolerated meal was numerically shorter (25.3 vs 32.6 hours) but not significantly different from placebo [4]."},{"q":"Is ipamorelin prohibited in sport?","a":"Yes. It is named on the WADA Prohibited List 2026 under S2.2.4, prohibited at all times [9]."}],"key_studies":[{"citation":"Raun et al., European Journal of Endocrinology","year":1998,"model":"Cells and animals (primary rat pituitary cells, anesthetized rats, conscious swine)","design":"In vitro and in vivo pharmacology with GHRP-6, GHRP-2 and GHRH comparators","finding":"GH release comparable to GHRP-6; in swine, no increase in ACTH or cortisol beyond the GHRH response and no effect on FSH, LH, prolactin or TSH [1].","ref":1},{"citation":"Gobburu et al., Pharmaceutical Research","year":1999,"model":"Humans (healthy male volunteers)","design":"Dose-escalation study with pharmacokinetic-pharmacodynamic modeling","finding":"Dose-proportional pharmacokinetics, terminal half-life of about 2 hours, and a single episode of GH release peaking at about 0.67 hours [3].","ref":3},{"citation":"Venkova et al., Journal of Pharmacology and Experimental Therapeutics","year":2009,"model":"Animals (rats, postoperative ileus model)","design":"Laparotomy with intestinal manipulation; ipamorelin, GHRP-6 or vehicle","finding":"Ipamorelin shortened time to first bowel movement; repeated administration increased fecal pellet output, food intake and body weight gain [2].","ref":2},{"citation":"Beck et al., International Journal of Colorectal Disease","year":2014,"model":"Humans (adults after small or large bowel resection)","design":"Randomized, double-blind, placebo-controlled phase 2 proof-of-concept (NCT00672074), 117 patients","finding":"Median time to first tolerated meal was 25.3 vs 32.6 hours (p = 0.15); no significant differences from placebo in key or secondary efficacy analyses; treatment-emergent adverse events in 87.5% vs 94.8% [4].","ref":4}],"label_dosing":[],"label_warnings":[],"last_reviewed":"2026-10-22","mechanism":"Ipamorelin (Aib-His-D-2-Nal-D-Phe-Lys-NH2) is a pentapeptide that stimulates growth hormone release through a GHRP-like receptor, as shown by antagonist profiling with GHRP and GHRH antagonists in rat pituitary cells [1]. It has since been described as an agonist of the ghrelin receptor [2].
In conscious swine, ipamorelin did not alter FSH, LH, prolactin or TSH, and unlike GHRP-6 and GHRP-2 it did not raise ACTH or cortisol beyond the levels seen after GHRH stimulation; the authors characterized it as selective for GH release [1].
Because ghrelin receptor stimulation has prokinetic effects, ipamorelin was investigated in postoperative ileus; in a rat model, it shortened time to first bowel movement and, with repeated administration, increased fecal output, food intake and body weight gain [2].
In healthy men, ipamorelin induced a short episode of GH release rather than sustained elevation, and FDA noted that the data raise questions about responsiveness with prolonged exposure in people with partial GH deficiency [3, 7].
","origin":"Synthetic pentapeptide discovered at Novo Nordisk in a series derived from GHRP-1 that lacks the central Ala-Trp dipeptide","published":true,"reg_status":"not_approved","regulatory":{"fda":"Not US FDA-approved; US FDA states there are no US FDA-approved drug products containing ipamorelin free base or acetate, and no label was found in DailyMed [7, 11]. In its October 2024 briefing for the Pharmacy Compounding Advisory Committee, US FDA proposed not adding ipamorelin to the 503A bulks list, citing lack of data, safety concerns and lack of evidence of efficacy [7]. FDA's compounding safety page lists ipamorelin acetate among nominated-but-withdrawn substances and notes it is in category 2 under the 503B interim policy [8].","wada":"Ipamorelin is named on the WADA Prohibited List 2026 under S2.2.4 (growth hormone secretagogues and their mimetics), prohibited at all times [9]."},"research":{"human":"In healthy male volunteers, ipamorelin was associated with a single episode of GH release at all dose levels tested, and the pharmacokinetics were dose-proportional with a terminal half-life of about 2 hours [3]. In a randomized, double-blind, placebo-controlled phase 2 trial of 117 patients after bowel resection, median time to first tolerated meal was 25.3 hours with ipamorelin and 32.6 hours with placebo (p = 0.15), and no significant efficacy differences were found [4]. A second, larger phase 2 dose-finding trial (320 participants) is registered as completed with no outcome data posted [6].","animal":"In anesthetized rats and conscious swine, ipamorelin released GH with potency and efficacy comparable to GHRP-6 [1]. In a rat model of postoperative ileus, it shortened time to first bowel movement, and repeated administration was associated with greater fecal output, food intake and weight gain [2].","in_vitro":"In primary rat pituitary cells, ipamorelin released GH with a potency and efficacy similar to GHRP-6, and antagonist experiments indicated action through a GHRP-like receptor [1]."},"slug":"ipamorelin","status_note":"Not approved by the US FDA for any use; US FDA states there are no US FDA-approved drug products containing ipamorelin, and in 2024 proposed that ipamorelin not be added to the 503A bulks list after finding safety concerns and no demonstrated efficacy [7, 11].","unknowns":"No controlled human trial has demonstrated efficacy of ipamorelin for any condition; the one published efficacy trial, in postoperative ileus, did not show a significant difference from placebo [4]. Long-term safety, safety by other routes of use, and effects in people with growth hormone deficiency have not been established in the sources reviewed [3, 7, 8]. The time course of GH response with prolonged exposure is not well characterized, and the registered 320-participant phase 2 trial has no posted outcome data [3, 6, 7].","id":"6ada7ecaa32c4049a5e815d7","created_date":"2026-10-22T21:23:22.041000","updated_date":"2026-10-23T17:31:39.190000"},{"adverse_events":[{"event":"Sensation of warmth","frequency":"16.0% (listed in the 5% or higher category)","population":"Clinical experience summarized in the Japanese package insert for the diagnostic product","severity":"Not specified","ref":5},{"event":"Other listed reactions: hypotension, ALT elevation, gastrointestinal symptoms (borborygmi, nausea, abdominal discomfort or pain, bloating), somnolence, dizziness, rhinorrhea, leukocytosis, sweating, thirst, hunger, malaise, bitter taste, back pain, headache, facial flushing","frequency":"Listed in lower-frequency or frequency-unknown categories; per-event rates are not tabulated here","population":"Japanese package insert, diagnostic use","severity":"Not specified","ref":5},{"event":"Increased food intake (pharmacodynamic effect)","frequency":"About 36% more intake than saline in 7 lean men; dose-dependent in a 19-participant study","population":"Healthy lean and obese volunteers","severity":"Not applicable","ref":6}],"components":[],"compound_class":"Synthetic growth hormone-releasing peptide (growth hormone secretagogue receptor agonist)","evidence_grade":"B","faqs":[{"q":"What is GHRP-2?","a":"GHRP-2, also called pralmorelin, is a synthetic hexapeptide from a series of GH-releasing peptides developed at Tulane University and Polygen, and it mimics the actions of ghrelin [1]."},{"q":"Is GHRP-2 approved as a drug in the US or Japan?","a":"It is not US FDA-approved for any use [10]. In Japan, a single-dose pralmorelin product is a prescription diagnostic for growth hormone secretion failure [5]."},{"q":"How does GHRP-2 differ from GHRH in animal studies?","a":"In conscious rats GHRP-2 released GH more potently than exogenous GHRH, and it released GH in dogs where GHRH did not, which the authors interpreted as lower sensitivity to endogenous somatostatin [2]."},{"q":"What has been reported about GHRP-2 and appetite?","a":"In studies in healthy lean men and in lean and obese volunteers, GHRP-2 increased ad libitum food intake compared with saline or placebo [6, 7]."},{"q":"What adverse reactions are listed for the Japanese diagnostic product?","a":"The package insert lists a sensation of warmth in 16.0% and a range of less frequent reactions including hypotension, ALT elevation, gastrointestinal symptoms, dizziness and flushing [5]."},{"q":"Is GHRP-2 prohibited in sport?","a":"Yes. GHRP-2 (pralmorelin) is named in section S2.2.4 of the WADA 2026 Prohibited List, which is prohibited at all times [11]."},{"q":"Has GHRP-2 been shown to treat any condition?","a":"The sources reviewed describe diagnostic use and short physiological studies; a drug profile noted that US development for GH deficiency appeared discontinued, and no controlled treatment trials were identified here [1, 3]."}],"key_studies":[{"citation":"Chihara et al. (KP-102 Study Group), Eur J Endocrinol","year":2007,"model":"Humans (77 healthy adults, 58 adults with GH deficiency)","design":"Multicenter diagnostic validation study versus insulin tolerance test","finding":"Peak GH after GHRP-2 was significantly lower in patients than in healthy subjects, with no difference between hypothalamic and pituitary disease, and the test showed favourable reproducibility.","ref":3},{"citation":"Laferrere et al., J Clin Endocrinol Metab","year":2005,"model":"Humans (7 lean healthy men)","design":"Saline-controlled study with an ad libitum buffet meal","finding":"Participants ate about 36% more during GHRP-2 administration than during saline, every participant increased intake, and serum GH rose.","ref":6},{"citation":"Laferrere et al., Obesity","year":2006,"model":"Humans (10 lean and 9 obese healthy adults)","design":"Double-blind, randomized, placebo-controlled study at two dose levels","finding":"Food intake rose in a dose-dependent manner, obesity status did not change the response, and serum GH increased dose dependently.","ref":7},{"citation":"Doi et al., Arzneimittelforschung","year":2004,"model":"Rats, dogs and cultured rat pituitary cells","design":"In vivo and in vitro pharmacology","finding":"GH release was more potent than exogenous GHRH in conscious rats, was present in dogs, and was absent after hypophysectomy; ACTH and corticosterone were stimulated but prolactin was not.","ref":2},{"citation":"Onuki et al., J Pediatr Endocrinol Metab","year":2024,"model":"Humans (23 adolescents tested at one institution)","design":"Retrospective case series","finding":"GH peaks were low in the organic or genetic GH deficiency group but high in idiopathic GH deficiency and short stature groups, and two patients exceeded the GHRP-2 cut-off while falling below it on other tests.","ref":8}],"label_dosing":[],"label_warnings":[],"last_reviewed":"2026-10-22","mechanism":"Synthetic growth hormone secretagogues were found to act on a G protein-coupled receptor cloned from swine and human pituitary and hypothalamus [12]. The endogenous ligand for that receptor was later purified from rat stomach and named ghrelin, a 28-amino-acid acylated peptide that releases GH in vivo and in vitro [13]. GHRP-2 has been described as a synthetic agonist of ghrelin that binds the GH secretagogue receptor [6].
In conscious rats, GHRP-2 (KP-102) released GH more potently than GHRH given exogenously, and it also released GH in conscious dogs, in which GHRH did not [2]. Its GH-releasing activity was absent in hypophysectomized rats and reduced, but still present, in rats with median eminence lesions, which the authors interpreted as indicating that endogenous GHRH from the median eminence is needed for its full activity [2]. In cultured rat anterior pituitary cells it stimulated GH secretion directly, although less potently than GHRH [2]. The Japanese package insert likewise summarizes attenuated activity after hypophysectomy, arcuate nucleus destruction and median eminence destruction in animals [5].
In conscious rats, GHRP-2 stimulated ACTH and corticosterone secretion but not prolactin secretion [2].
","origin":"Synthetic hexapeptide from a series of small growth hormone-releasing peptides synthesised at Tulane University and Polygen [1]","published":true,"reg_status":"approved_ex_us","regulatory":{"fda":"GHRP-2 is not approved by the US FDA for any use [10]. FDA's categorization of nominated 503A bulk drug substances (updated May 14, 2026) lists GHRP-2 in Category 3, bulk drug substances nominated without adequate support [10]. A drug profile reported that a US phase II program for GH deficiency with Wyeth appeared to have been discontinued [1].","wada":"The WADA 2026 Prohibited List names GHRP-2 (pralmorelin) under S2.2.4 (growth hormone releasing factors, including GH-releasing peptides); S2 substances are prohibited at all times, in and out of competition, and are non-Specified Substances [11]."},"research":{"human":"In a multicenter validation study of 77 healthy adults and 58 adults with severe GH deficiency confirmed by insulin tolerance testing, peak GH after GHRP-2 was markedly lower in the patient group, and repeat testing showed favourable reproducibility [3]. In saline- or placebo-controlled studies in healthy lean and obese volunteers, GHRP-2 increased ad libitum food intake and serum GH [6, 7]. A Japanese review describes the GHRP-2 test as available there and recommended as a convenient stimulation test for adult GH deficiency [4]. Retrospective and cohort reports from Japan describe GHRP-2 testing in adolescents and in older adults with pituitary tumors, with the authors noting that adolescent cut-offs may need revisiting [8, 9].","animal":"In rats and dogs, GHRP-2 (KP-102) released GH, and three weeks of administration in normal and monosodium glutamate-treated rats was associated with growth acceleration and a slight rise in body weight and some organ weights [2].","in_vitro":"In cultured rat anterior pituitary cells, GHRP-2 directly stimulated GH secretion, with lower potency than GHRH in this system [2]."},"slug":"ghrp-2","status_note":"Not approved by the US FDA for any use [10]. In Japan, a single-dose pralmorelin product (GHRP Kaken 100, Kaken Pharmaceutical) is a prescription diagnostic agent for growth hormone secretion failure, with a listed sales start of February 2005 [5].","unknowns":"Long-term human data on repeated or chronic exposure were not identified in the sources reviewed. Human data are dominated by single-administration diagnostic testing and short administrations. No controlled trials of tissue-repair, body-composition or performance outcomes were identified. Growth-related findings in rats have not been established in people.","id":"6ada7eca72aae0fb69927f41","created_date":"2026-10-22T21:23:22.801000","updated_date":"2026-10-24T21:06:00.417000"},{"adverse_events":[],"components":[],"compound_class":"Growth hormone-releasing hormone (GHRH) analog (29-amino-acid peptide)","evidence_grade":"C","faqs":[{"q":"What is the difference between CJC-1295 with and without DAC?","a":"The DAC form has a maleimidopropionamide-lysine group that binds serum albumin and prolongs its action, while the no-DAC form is the 29-residue substituted GHRH analog without that group; US FDA lists them with different molecular formulas and weights (about 3367.95 vs 3647.95) [3]."},{"q":"Have human studies been done on CJC-1295 without DAC?","a":"No human study specific to the no-DAC form was identified [3]. The published human studies concern the DAC form, and US FDA found no clinical data to assess safety or efficacy of the free base or acetate forms [2, 3]."},{"q":"Is the no-DAC form shorter-acting?","a":"Its duration has not been characterized in the sources reviewed; the DAC group is what extends half-life to days in the DAC form, and unmodified hGRF(1-29) had a smaller and shorter growth hormone response in rats than the DAC conjugate [1, 3]."},{"q":"Why is the naming confusing?","a":"FDA noted that CJC-1295 has been used as a common name for both DAC and non-DAC structures, and that it is not possible to know which compound is meant from the common name alone [3]."},{"q":"Is CJC-1295 without DAC US FDA-approved?","a":"No. No FDA label exists, and US FDA proposed in 2024 that the free base and acetate forms not be placed on the 503A bulks list [4, 7]."},{"q":"Is CJC-1295 prohibited in sport?","a":"CJC-1295 is named on the WADA Prohibited List 2026 under growth hormone releasing factors (S2.2.4), prohibited at all times [6]."},{"q":"What safety concerns has FDA raised?","a":"FDA cited potential immunogenicity of injectable peptides from aggregation and impurities, incomplete characterization data, and a lack of safety data for the free base and acetate forms [3]."},{"q":"What did the rat studies show about the DAC group?","a":"The DAC conjugate produced about a 4-fold larger GH response than unmodified hGRF(1-29) over 2 hours and persisted in plasma beyond 72 hours [1]."}],"key_studies":[{"citation":"Jette et al., Endocrinology","year":2005,"model":"Animals (rats) and cultured rat pituitary cells","design":"Synthesis and characterization of hGRF(1-29)-albumin bioconjugates versus unmodified hGRF(1-29)","finding":"The DAC conjugate CJC-1295 produced about a 4-fold larger GH area under the curve over 2 hours than unmodified hGRF(1-29) and was present in plasma beyond 72 hours; the study did not test the no-DAC peptide itself [1].","ref":1},{"citation":"Teichman et al., Journal of Clinical Endocrinology & Metabolism","year":2006,"model":"Humans (healthy adults aged 21 to 61)","design":"Two randomized, placebo-controlled, double-blind ascending-dose studies of the long-acting CJC-1295 (DAC form)","finding":"Dose-dependent increases in GH and IGF-I and an estimated half-life of 5.8 to 8.1 days were reported; FDA reads the clinical references as concerning the DAC form, so these findings are not evidence for the no-DAC form [2, 3].","ref":2},{"citation":"FDA Pharmacy Compounding Advisory Committee evaluation","year":2024,"model":"Regulatory review of published literature on CJC-1295-related substances","design":"Evaluation of physical/chemical characterization, safety and efficacy","finding":"US FDA found no nonclinical or clinical data to assess the safety or efficacy of CJC-1295 free base or acetate, and noted that safety assessment of the class rested on the DAC forms [3].","ref":3}],"label_dosing":[],"label_warnings":[],"last_reviewed":"2026-10-22","mechanism":"Like other analogs of the first 29 residues of GHRH, the peptide is expected to act on the pituitary GHRH receptor to stimulate growth hormone release, but FDA's 2024 evaluation stated that nonclinical studies were not identified to establish whether the CJC-1295 free base and acetate forms are pharmacologically active [3]. Pharmacology described in the literature belongs to the DAC form and to unmodified GRF(1-29) [1, 3].
The DAC form carries a maleimidopropionamide-lysine unit at the C-terminus that binds covalently to serum albumin; the no-DAC peptide lacks this group [3]. In rats, the albumin-bound conjugate stimulated a growth hormone response about 4 times larger than unmodified hGRF(1-29) over 2 hours and remained in plasma beyond 72 hours [1].
FDA noted that CJC-1295 has been described with and without the DAC group and that it is not possible to know which structure is intended when only a common name is used [3]. The identification of CJC-1295 without DAC in the literature dates to 2010, when it was reported in an unknown pharmaceutical preparation seized by Norwegian police and customs [3].
","origin":"Synthetic, multiply substituted analog of human GHRH(1-29) without the albumin-binding drug affinity complex (DAC) group","published":true,"reg_status":"not_approved","regulatory":{"fda":"Not US FDA-approved; no label for CJC-1295 was found in DailyMed [7]. In December 2024, FDA presented its evaluation of CJC-1295-related bulk drug substances, including the free base and acetate forms, to its Pharmacy Compounding Advisory Committee and proposed that these forms not be included on the 503A bulks list [3, 4]. FDA's public safety summary lists CJC-1295 among nominated-but-withdrawn substances [5].","wada":"CJC-1295 is named on the WADA Prohibited List 2026 under S2.2.4 (growth hormone releasing factors, GHRH and its analogues), prohibited at all times [6]."},"research":{"human":"No published human study specific to CJC-1295 without DAC was identified; the human studies in healthy adults used the DAC form, which has an estimated half-life of 5.8 to 8.1 days [2, 3]. FDA's 2024 evaluation found no clinical data to assess safety or efficacy of the free base or acetate forms [3].","animal":"No animal study specific to the no-DAC form was identified by FDA, which stated that pharmacological activity of the free base and acetate forms was not established in nonclinical studies [3]. Rat studies on the DAC conjugate used unmodified hGRF(1-29) as the comparator [1].","in_vitro":"Albumin conjugates of hGRF(1-29) derivatives were bioactive in a GH secretion assay in cultured rat anterior pituitary cells and were more stable against dipeptidylpeptidase-IV than the unmodified peptide in vitro [1]. No in vitro study specific to the no-DAC form was identified [3]."},"slug":"cjc-1295-no-dac","status_note":"Not approved by the US FDA for any use; US FDA reviewed the CJC-1295 free base and acetate forms for the compounding bulks list in 2024, found no nonclinical or clinical data to assess their safety and efficacy, and proposed that they not be included [3, 4, 7].","unknowns":"Evidence specific to the no-DAC form is limited: whether it is pharmacologically active in the same way as the DAC form, its half-life, its effects on growth hormone and IGF-I, and its safety in humans have not been established in the sources reviewed [3]. The published human studies were of the DAC form [2, 3]. Because the name CJC-1295 is used for both structures, literature and product labels can be ambiguous about which compound is meant [3].","id":"6ada7ec9884d82ce6f80387b","created_date":"2026-10-22T21:23:21.183000","updated_date":"2026-10-24T21:06:04.648000"},{"adverse_events":[{"event":"Transient facial flushing","frequency":"Not quantified in the source abstract","population":"Children receiving sermorelin, per a published review","severity":"Transient; reported among the most common adverse events","ref":3},{"event":"Administration-site pain","frequency":"Not quantified in the source abstract","population":"Children receiving sermorelin, per a published review","severity":"Reported among the most common adverse events","ref":3}],"components":[],"compound_class":"Growth hormone-releasing hormone (GHRH) analog","evidence_grade":"B","faqs":[{"q":"What is sermorelin?","a":"A synthetic 29-amino-acid analog of growth hormone-releasing hormone that was described as the shortest synthetic peptide with full GHRH biological activity [3]."},{"q":"Was sermorelin ever US FDA-approved?","a":"Yes. Geref (sermorelin acetate) was US FDA-approved under NDA 19-863 on 28 December 1990 (diagnostic use) and NDA 20-443 on 26 September 1997 (growth hormone deficiency in children) [1]."},{"q":"Was sermorelin withdrawn because of safety problems?","a":"FDA's 2013 notice states the Geref products were not withdrawn from sale for reasons of safety or efficacy [1]."},{"q":"What were Geref's US FDA-approved indications?","a":"The vials were indicated for idiopathic growth hormone deficiency in children with growth failure, and the ampule for evaluating the ability of the pituitary somatotroph to secrete growth hormone [1]."},{"q":"Is there a current US FDA-approved sermorelin product?","a":"Drugs@FDA lists the Geref products as Discontinued, and no current label was identified [2]."},{"q":"What human evidence exists?","a":"A 110-child open-label study reported higher height velocity with GHRH(1-29) [4], and a review described its use as a diagnostic stimulation test [3]."},{"q":"Is sermorelin permitted in sport?","a":"No. It is named as an example GHRH analog in WADA's S2 category, prohibited at all times [6]."}],"key_studies":[{"citation":"Thorner et al. (Geref International Study Group), J Clin Endocrinol Metab","year":1996,"model":"Humans (110 prepubertal children with growth hormone deficiency; 86 evaluable for efficacy)","design":"Multicenter, open-label, no placebo control","finding":"Mean height velocity rose from 4.1 cm/yr at baseline to 8.0 cm/yr and 7.2 cm/yr; 74% were considered good responders; no change in fasting glucose or excessive IGF-1 generation was noted [4].","ref":4},{"citation":"Prakash and Goa, BioDrugs","year":1999,"model":"Humans (review of studies in children with idiopathic growth hormone deficiency)","design":"Narrative review","finding":"The review described sermorelin as a growth hormone-stimulation test with fewer false-positive responses than some other provocative tests, and reported that growth effects of daily sermorelin were smaller than those of somatropin in non-head-to-head comparison; the effect on final adult height was undetermined [3].","ref":3},{"citation":"FDA notice, 78 Federal Register 14095","year":2013,"model":"Regulatory record","design":"Agency determination under 21 CFR 314.161","finding":"US FDA reviewed its files and the literature, including postmarketing adverse event data, and determined both Geref products were not withdrawn from sale for reasons of safety or efficacy [1].","ref":1}],"label_dosing":[],"label_warnings":[],"last_reviewed":"2026-10-22","mechanism":"Sermorelin is a 29-amino-acid analog of human growth hormone-releasing hormone (GHRH); sermorelin has been reported to stimulate growth hormone secretion from the anterior pituitary [3].
GHRH, also called growth hormone-releasing factor, is a hypothalamic peptide that acts on pituitary somatotroph cells to stimulate synthesis and pulsatile release of endogenous growth hormone [5]. Sermorelin acts at this same level of the axis rather than supplying growth hormone itself [3, 5].
","origin":"Synthetic 29-amino-acid analog of human growth hormone-releasing hormone, the shortest synthetic fragment described as retaining full GHRH biological activity [3].","published":true,"reg_status":"not_approved","regulatory":{"fda":"Sermorelin has no currently marketed US FDA-approved product. Geref NDA 19-863 and NDA 20-443 were US FDA-approved in 1990 (diagnostic use) and 1997 (growth hormone deficiency in children) and withdrawn as of 18 June 2009 after discontinuation by the sponsor, and Drugs@FDA lists the Geref products as Discontinued [1, 2]. US FDA determined in 2013 that the products were not withdrawn for safety or efficacy reasons, which allows ANDAs referencing them to be considered [1].","wada":"Sermorelin is named as an example GHRH analog, with CJC-1295 and tesamorelin, in the S2 category of WADA's 2026 Prohibited List, which is prohibited at all times [6]."},"research":{"human":"A published review concluded that a single sermorelin dose can serve as a provocative test for growth hormone deficiency and that limited data suggest effects on growth in some prepubertal children [3].","animal":"No animal studies were reviewed for this entry.","in_vitro":"No in vitro studies were reviewed for this entry."},"slug":"sermorelin","status_note":"Not currently US FDA-approved. The sponsor notified FDA of discontinuation in 2008 and US FDA withdrew approval of both applications as of 18 June 2009; in 2013 US FDA determined the products were not withdrawn for reasons of safety or efficacy [1, 2].","unknowns":"No current FDA label exists, so there are no labeled warnings or labeled dosing. Frequency data for adverse events were not available in the sources reviewed. Elimination half-life was not located in the primary sources reviewed. Effects on final adult height after long-term use were described as undetermined [3]. The current legal status of compounded sermorelin was not assessed for this entry.","id":"6ada7ec69335b5cf983f24b4","created_date":"2026-10-22T21:23:18.043000","updated_date":"2026-10-23T17:31:39.655000"},{"adverse_events":[{"event":"Administration-site reaction (composite)","frequency":"17% tesamorelin versus 6% placebo in the label's Table 1; the warnings section reports 25% versus 14% for administration-site reactions during the first 26 weeks","population":"HIV-infected adults with lipodystrophy, phase of combined studies (n=543 vs 263)","severity":"Erythema, pruritus, pain, irritation, bruising","ref":1},{"event":"Arthralgia","frequency":"13% versus 11%","population":"Same combined data","severity":"Fluid-retention-related; transient or resolved on discontinuation per label","ref":1},{"event":"Pain in extremity","frequency":"6% versus 5%","population":"Same combined data","severity":"Not graded in the label table","ref":1},{"event":"Myalgia","frequency":"6% versus 2%","population":"Same combined data","severity":"Not graded in the label table","ref":1},{"event":"Peripheral edema","frequency":"6% versus 2%","population":"Same combined data","severity":"Fluid-retention-related","ref":1},{"event":"Paresthesia","frequency":"5% versus 2%","population":"Same combined data","severity":"Not graded in the label table","ref":1},{"event":"Hypersensitivity reactions (pruritus, erythema, flushing, urticaria, rash)","frequency":"4% of treated patients across clinical trials","population":"HIV-infected adults with lipodystrophy","severity":"Label advises immediate discontinuation if suspected","ref":1},{"event":"New HbA1c of 6.5% or higher","frequency":"5% versus 1% (hazard ratio 3.3, 95% CI 1.4-9.6)","population":"Clinical trials, through week 26","severity":"Evaluate glucose before and during therapy per label","ref":1}],"components":[],"compound_class":"Growth hormone-releasing hormone (GHRH/GRF) analog","evidence_grade":"A","faqs":[{"q":"What is tesamorelin approved for?","a":"The FDA labels list reduction of excess abdominal fat in HIV-infected adult patients with lipodystrophy, and state that it is “not indicated for weight loss management” [1, 2]."},{"q":"How does tesamorelin act?","a":"It is a GRF analog that binds human GRF receptors and, per the label, stimulates pituitary GH secretion with a subsequent rise in IGF-1 and IGFBP-3 [1]."},{"q":"How large was the effect on visceral fat in the pivotal studies?","a":"At week 26 the mean change in visceral adipose tissue was -27 versus +4 cm2 in Study 1 and -21 versus 0 cm2 in Study 2 for tesamorelin versus placebo [1]."},{"q":"What are the most commonly reported adverse reactions?","a":"The label lists arthralgia, administration-site erythema, administration-site pruritus, pain in extremity, peripheral edema and myalgia as reactions reported in more than 5% of patients [1]."},{"q":"Who should not receive tesamorelin according to the label?","a":"The label contraindicates it in people with disruption of the hypothalamic-pituitary axis, active malignancy, known hypersensitivity, and in pregnancy [1, 2]."},{"q":"How long does tesamorelin stay in the circulation?","a":"Mean elimination half-life was about 11 minutes (Egrifta WR) and 8 minutes (Egrifta SV) in healthy subjects after a single dose [1, 2]."},{"q":"Has tesamorelin been studied for liver fat?","a":"Two small randomized trials in people with HIV reported reductions in liver fat compared with placebo, but long-term effects on liver histology remain to be determined [5, 6]."},{"q":"Is tesamorelin allowed in sport?","a":"No. It is named as a GHRH analog in WADA's S2 category, which is prohibited at all times [7]."}],"key_studies":[{"citation":"Falutz et al., N Engl J Med","year":2007,"model":"Humans (412 HIV-infected adults with abdominal fat accumulation)","design":"Randomized, placebo-controlled, 26 weeks","finding":"Visceral adipose tissue changed by -15.2% with tesamorelin versus +5.0% with placebo; IGF-1 rose 81.0% versus a 5.0% decrease; more tesamorelin participants withdrew because of adverse events [3].","ref":3},{"citation":"Falutz et al., J Clin Endocrinol Metab","year":2010,"model":"Humans (806 HIV-infected adults with excess abdominal fat)","design":"Pooled analysis of two randomized, double-blind phase 3 trials with safety extension","finding":"Visceral adipose tissue changed by -24 versus +2 cm2 at week 26 (treatment effect -15.4%); the reduction was maintained to week 52 in the group continuing tesamorelin; IGF-1 rose by a mean of 108 versus a 7 ng/mL decrease [4].","ref":4},{"citation":"EGRIFTA WR prescribing information, Section 14 (Studies 1 and 2; NCT00123253, NCT00435136)","year":2025,"model":"Humans (412 and 404 HIV-infected adults with lipodystrophy)","design":"Two randomized, double-blind, placebo-controlled studies, main phase plus extension","finding":"Mean change in visceral adipose tissue at week 26 was -27 versus +4 cm2 (Study 1) and -21 versus 0 cm2 (Study 2); IGF-1 rose by 107 and 108 ng/mL versus -15 and +3 ng/mL with placebo [1].","ref":1},{"citation":"Stanley et al., JAMA","year":2014,"model":"Humans (50 antiretroviral-treated HIV-infected adults with abdominal fat accumulation)","design":"Randomized, double-blind, placebo-controlled, 6 months","finding":"Visceral adipose tissue changed by -34 versus +8 cm2 and liver fat (lipid-to-water percentage) by a median of -2.0% versus +0.9%; fasting glucose was higher at 2 weeks with tesamorelin but not significantly different at 6 months [5].","ref":5},{"citation":"Stanley et al., Lancet HIV","year":2019,"model":"Humans (61 people with HIV and hepatic fat fraction of 5% or more)","design":"Randomized, double-blind, placebo-controlled, 12 months plus open-label phase","finding":"Hepatic fat fraction changed by an absolute -4.1% more than placebo; 35% versus 4% had hepatic fat fraction below 5% at 12 months; administration-site complaints were more frequent with tesamorelin [6].","ref":6}],"label_dosing":[{"text":"For reduction of excess abdominal fat in HIV-infected adult patients with lipodystrophy (EGRIFTA SV, 2 mg/vial): the labeled dose is 1.4 mg given once daily.","ref":2},{"text":"For reduction of excess abdominal fat in HIV-infected adult patients with lipodystrophy (EGRIFTA WR, 11.6 mg/vial): the labeled dose is 1.28 mg given once daily.","ref":1},{"text":"The EGRIFTA WR label states that EGRIFTA WR and EGRIFTA SV are not substitutable because they differ in dosage, number of vials needed to prepare a dose, reconstitution instructions and storage requirements; the EGRIFTA SV label likewise states that its recommendations apply only to the 2 mg/vial formulation and that the formulations differ in these respects. Preparation and administration steps are set out in the prescribing information and are not reproduced here [1, 2].","ref":1},{"text":"The label states that tesamorelin is “not indicated for weight loss management”.","ref":1},{"text":"The pivotal trials described on the labels administered 2 mg of the original EGRIFTA formulation (1 mg/vial) once daily; the EGRIFTA WR label states that its approval rests on those studies plus comparable bioavailability between EGRIFTA WR 1.28 mg and the original EGRIFTA 2 mg dose [1].","ref":1},{"text":"Labels' limitations of use: long-term cardiovascular safety has not been established, and the labels say: “Consider risk/benefit of continuation of treatment in patients who have not had a reduction in visceral adipose tissue.” [1, 2].","ref":1}],"label_warnings":[{"text":"Contraindications: disruption of the hypothalamic-pituitary axis (for example hypophysectomy, hypopituitarism, pituitary tumor or surgery, head irradiation or head trauma), active malignancy, known hypersensitivity to tesamorelin or excipients, and pregnancy [1, 2].","ref":1},{"text":"Increased risk of neoplasms: tesamorelin induces release of endogenous growth hormone, a growth factor; preexisting malignancy should be inactive with treatment complete before use, and the label advises discontinuation if there is evidence of recurrent malignancy [1].","ref":1},{"text":"Elevated IGF-1: among patients treated for 26 weeks, 47% had IGF-1 above 2 standard deviation scores and 36% above 3; the effects of prolonged IGF-1 elevation are unknown, and the label advises monitoring IGF-1 [1].","ref":1},{"text":"Fluid retention (edema, arthralgia, carpal tunnel syndrome) may occur and is thought to be related to induced GH secretion [1].","ref":1},{"text":"Glucose intolerance or diabetes mellitus may develop; the label advises evaluating glucose status before and periodically during treatment and monitoring patients with diabetes for retinopathy [1].","ref":1},{"text":"Hypersensitivity reactions occurred in 4% of treated patients in clinical trials [1].","ref":1},{"text":"Administration-site reactions: 25% in treated patients versus 14% with placebo during the first 26 weeks; the label advises rotating abdominal administration sites [1].","ref":1},{"text":"Increased mortality in acute critical illness has been reported with pharmacologic amounts of growth hormone, and the label advises considering discontinuation in critically ill patients [1].","ref":1},{"text":"Pregnancy: contraindicated, because altering visceral fat offers no known advantage in pregnancy and could lead to fetal harm; the label also advises that mothers with HIV should not breastfeed. Safety and efficacy in pediatric patients have not been established, and the labels note that in children with open epiphyses tesamorelin may accelerate linear growth [1, 2].","ref":1},{"text":"Drug interactions: the label advises monitoring for interactions with CYP450-metabolized drugs and notes that patients on glucocorticoid replacement for hypoadrenalism may need dose adjustments after initiation [1].","ref":1}],"last_reviewed":"2026-10-23","mechanism":"Tesamorelin binds and stimulates human growth hormone-releasing factor (GRF) receptors in vitro with potency similar to endogenous GRF [1].
GRF, also called GHRH, is a hypothalamic peptide that acts on pituitary somatotroph cells to stimulate synthesis and pulsatile release of endogenous growth hormone (GH) [1]. According to the label, tesamorelin stimulates GH secretion and subsequently increases IGF-1 and IGFBP-3, with no clinically significant changes reported in TSH, LH, ACTH or prolactin in the clinical trials [1].
The label reports absolute bioavailability of under 4% for a 2 mg dose of the earlier formulation, a median time to peak concentration of 0.15 hours, and no formal human metabolism studies [1].
","origin":"Synthetic 44-amino-acid sequence of human growth hormone-releasing factor with a hexenoyl group attached to the N-terminal tyrosine, prepared as an acetate salt [1].","published":true,"reg_status":"fda_approved","regulatory":{"fda":"Tesamorelin is US FDA-approved (initial U.S. approval 2010) as Egrifta SV and Egrifta WR for the reduction of excess abdominal fat in HIV-infected adult patients with lipodystrophy; the labels describe limitations of use, including that it is “not indicated for weight loss management” [1, 2].","wada":"Tesamorelin is named, together with sermorelin and CJC-1295, as an example of a GHRH analog in the S2 category of WADA's 2026 Prohibited List, which is prohibited at all times [7]."},"research":{"human":"Tesamorelin has been studied in randomized placebo-controlled trials in HIV-infected adults with abdominal fat accumulation, in which visceral adipose tissue decreased compared with placebo over 26 weeks [1, 3, 4]. Small randomized trials in the same population have also reported changes in liver fat [5, 6].","animal":"The label reports that tesamorelin acetate given to rats during organogenesis was associated with hydrocephaly in offspring and delayed skull ossification at lower exposures, and that no adverse developmental effects were seen in rabbits [1].","in_vitro":"In vitro, tesamorelin binds and stimulates human GRF receptors, and it was reported to be non-mutagenic in the Ames test and in mammalian-cell and mouse chromosomal-damage assays [1]."},"slug":"tesamorelin","status_note":"US FDA-approved (initial U.S. approval 2010) for the reduction of excess abdominal fat in HIV-infected adult patients with lipodystrophy; marketed as Egrifta SV (2 mg/vial) and Egrifta WR (11.6 mg/vial). The labels state it is “not indicated for weight loss management” and that long-term cardiovascular safety has not been established [1, 2].","unknowns":"Long-term cardiovascular safety has not been established according to the label [1, 2]. The effects of prolonged IGF-1 elevation are unknown [1]. There is no label information for patients over 65 years or for pediatric patients, and pharmacokinetics in renal or hepatic impairment have not been established [1]. Efficacy has been studied mainly in HIV-associated lipodystrophy; use outside that setting is not covered by the labels.","id":"6ada7ec5996b301c4abb0f57","created_date":"2026-10-22T21:23:17.332000","updated_date":"2026-10-24T21:06:01.136000"}],"Comparison?q=%7B%22a%22%3A%7B%22%24in%22%3A%5B%22tesamorelin%22%2C%22sermorelin%22%2C%22cjc-1295-no-dac%22%2C%22ipamorelin%22%2C%22ghrp-2%22%2C%22ghrp-6%22%5D%7D%7D":[{"a":"ghrp-2","b":"hexarelin","differences":["Approval: GHRP-2 is an approved diagnostic product in Japan [1]; no approval was located for hexarelin [10].","Pharmacokinetics: an elimination half-life of about 0.42 to 0.69 hours is documented for pralmorelin in healthy men [1], while no half-life was located for hexarelin.","Research focus: GHRP-2's human data concern diagnostic growth hormone testing and appetite [3, 4], while hexarelin's distinctive human data are acute cardiac measures [7, 8].","FDA compounding listing: GHRP-2 is in 503B category 2, whereas hexarelin is not named on the FDA page as of 22 April 2026 [11].","Direct comparison: hexarelin has been compared with ghrelin and GHRH in the same volunteers [6]; a side-by-side comparison with GHRP-2 was located only in animal work describing both relative to GHRP-6 [12]."],"faqs":[{"q":"Is GHRP-2 approved anywhere?","a":"Yes, in Japan, as pralmorelin hydrochloride for diagnosing growth hormone secretion deficiency, marketed since February 2005 [1]. It is not US FDA-approved [11]."},{"q":"Do GHRP-2 and hexarelin affect cortisol?","a":"Both have been reported to raise ACTH and cortisol: GHRP-2 in conscious rats [5] and hexarelin in healthy men [6]."},{"q":"Can GHRP-2 and hexarelin be compared directly?","a":"No head-to-head human trial was located; their published human studies addressed different questions [3, 8]."},{"q":"What is known about their half-lives?","a":"The Japanese package insert reports an elimination half-life of about 0.42 to 0.69 hours for pralmorelin in 18 healthy men [1]. No half-life for hexarelin was located in the sources reviewed."}],"intro":"GHRP-2 and hexarelin are both synthetic growth hormone-releasing peptides acting at the ghrelin (GHS) receptor, and both raise ACTH and cortisol in addition to growth hormone [5, 6]. GHRP-2, generic name pralmorelin, is approved in Japan as a diagnostic agent for growth hormone secretion deficiency and has been marketed there since February 2005 [1]. Hexarelin (examorelin) has no approval identified, and its human literature consists of small Italian studies of acute cardiac measures [7, 8, 10]. Neither is US FDA-approved; GHRP-2 is in 503B category 2 on the FDA's compounding page while hexarelin is not named there, as of 22 April 2026 [11].","last_reviewed":"2026-10-24","limited":"No head-to-head human trial of GHRP-2 and hexarelin was located. GHRP-2's human evidence is diagnostic, with a defined cut-off rather than treatment outcomes [3], while hexarelin's is a set of small single-administration cardiac and endocrine studies, mostly from one centre and from the 1990s and early 2000s [6, 7, 8]. No half-life was located for hexarelin, so exposure cannot be compared [10]. The food-intake finding for GHRP-2 came from 7 participants [4], and the cardiac findings for hexarelin from 13 and 24 patients [7, 8].","published":true,"slug":"ghrp-2-vs-hexarelin","table":[{"field":"Class","a":"Synthetic growth hormone-releasing peptide / ghrelin receptor agonist; generic name pralmorelin [1, 2]","b":"Synthetic hexapeptide growth hormone secretagogue (ghrelin receptor agonist); also called examorelin [6]"},{"field":"Origin and structure","a":"Developed from work on small GHRP analogues at Tulane University; marketed in Japan as pralmorelin hydrochloride [2]","b":"Described as a non-natural peptidyl growth hormone secretagogue [6]"},{"field":"Proposed mechanism","a":"Stimulates growth hormone at the GHS receptor; in conscious rats it raised growth hormone more than injected GHRH and also raised ACTH and corticosterone [5]","b":"Stimulates growth hormone at the GHS receptor and in humans also raises prolactin, ACTH and cortisol [6]; separate reports describe growth hormone-independent cardiac effects [7, 8]"},{"field":"Half-life","a":"Elimination half-life of about 0.42 to 0.69 hours in 18 healthy men after administration, with plasma protein binding of 83 to 86%, per the Japanese package insert [1]","b":"Not located in the sources reviewed"},{"field":"Highest human trial phase","a":"Approved diagnostic product in Japan; validation study in 77 healthy subjects and 58 patients with growth hormone deficiency [1, 3]","b":"No phase-numbered registered trial located; published work is investigator-initiated physiology and cardiology studies [7, 8, 9]"},{"field":"FDA status","a":"Not US FDA-approved; GHRP-2 for injectable and nasal routes is in 503B category 2 (added 29 September 2023), as of 22 April 2026 [11]","b":"Not US FDA-approved; no Drugs@FDA application record located for hexarelin or examorelin (searched 24 October 2026) [10]. Not named on the FDA compounding page as of 22 April 2026 [11]"},{"field":"Published human outcomes","a":"Peak growth hormone was much lower in patients with growth hormone deficiency than in healthy subjects, supporting diagnostic use [3]; in 7 healthy men, administration was followed by greater food intake than saline [4]","b":"In 13 patients with cardiomyopathy, ejection fraction rose in the ischemic but not the dilated group despite similar growth hormone rises [7]; in 24 men during bypass surgery, ejection fraction, cardiac index and output rose while growth hormone, GHRH and placebo had no effect [8]"},{"field":"Safety signals","a":"FDA is aware of reports of serious adverse events in patients who received GHRP-2, including increased insulin requirement, deaths of critically ill study subjects, infection and pancreatitis, with causality not established [11]","b":"Short-term administration in elderly volunteers did not reduce the growth hormone response, with no adverse findings reported in the abstract [9]; no regulatory safety assessment was located [10, 11]"},{"field":"WADA status","a":"Named under S2.2.4 as GHRP-2 (pralmorelin); prohibited at all times (2026 List) [13]","b":"Named under S2.2.4 as examorelin (hexarelin); prohibited at all times (2026 List) [13]"},{"field":"Who funded the evidence","a":"Preclinical characterisation came from Kaken Pharmaceutical, which holds the Japanese product [1, 5]; the food-intake study was supported by US NIH grants [4]","b":"Academic groups, mainly the University of Turin [6, 7, 8, 9]"}],"title":"GHRP-2 (pralmorelin) vs Hexarelin","verdict":["Class: both are ghrelin-receptor growth hormone-releasing peptides that also raise ACTH and cortisol [5, 6].","Approval: GHRP-2 (pralmorelin) is an approved diagnostic in Japan; no approval was located for hexarelin [1, 10].","Evidence: GHRP-2's human data are diagnostic; hexarelin's are small acute cardiac and endocrine studies [3, 8]."],"id":"6add5a5a2fbcef8b86245eb3","created_date":"2026-10-25T01:24:42.962000","updated_date":"2026-10-25T01:24:42.962000"},{"a":"tesamorelin","b":"cjc-1295-no-dac","differences":["Approval: tesamorelin is US FDA-approved for HIV-associated abdominal fat (Egrifta); CJC-1295 in any form has never been US FDA-approved [1, 7].","Human data: tesamorelin has two phase 3 trials with over 800 participants combined [3], while US FDA found no clinical data at all for CJC-1295 without DAC [5].","Characterisation: tesamorelin's identity and composition are set out in a US FDA-approved label for HIV-associated abdominal fat [1]; US FDA judged CJC-1295 substances not well characterised [5].","Expected duration: the albumin-binding DAC unit, absent here, was what extended the molecule's time in circulation [5, 8]."],"faqs":[{"q":"What is the difference between CJC-1295 with and without DAC?","a":"The DAC is a maleimidopropionamide-lysine unit that binds serum albumin and was added to overcome the short half-life of GHRH(1-29) [5, 8]. US FDA found no pharmacological studies of the non-DAC forms and says it is unknown whether they are active [5]."},{"q":"Is tesamorelin US FDA-approved?","a":"Yes. Tesamorelin is US FDA-approved for reducing excess abdominal fat in HIV-infected adults with lipodystrophy, with initial US approval in 2010 [1]."},{"q":"Can tesamorelin and CJC-1295 (no DAC) be compared directly?","a":"No. Tesamorelin has phase 3 trial data, while US FDA states there are no nonclinical or clinical data for CJC-1295 free base or acetate [3, 5]."},{"q":"Are both named on the WADA list?","a":"Yes. WADA's 2026 Prohibited List names tesamorelin and CJC-1295 under S2.2.4, growth hormone releasing factors, prohibited at all times [11]."}],"intro":"Tesamorelin and CJC-1295 without DAC are both growth hormone-releasing hormone (GHRH) analogues, but they sit at opposite ends of the evidence spectrum [1, 5]. Tesamorelin is US FDA-approved (initial US approval 2010) for reducing excess abdominal fat in adults with HIV and lipodystrophy, with two phase 3 placebo-controlled trials behind it [1, 3]. CJC-1295 without DAC is a GHRH(1-29) analogue that FDA reviewers describe as first referenced in the literature in 2010 through an unidentified preparation seized by Norwegian authorities, with no nonclinical or clinical data to assess it [5]. It has never been US FDA-approved and appears on the FDA's compounding page of substances that may present significant safety risks, current as of 22 April 2026 [7].","last_reviewed":"2026-10-24","limited":"These two compounds cannot be compared on outcomes, because only one has human outcome data. Tesamorelin's results come from trials in adults with HIV-associated abdominal fat and are specific to that population and endpoint [2, 3]. For CJC-1295 without DAC, US FDA states there are no nonclinical or clinical data, and that published studies carrying the CJC-1295 name used DAC-containing material of unspecified salt form [5, 6]. Any inference from the DAC literature to the non-DAC form is therefore unsupported [5].","published":true,"slug":"tesamorelin-vs-cjc-1295-no-dac","table":[{"field":"Class","a":"GHRH (growth hormone-releasing factor) analogue [1]","b":"GHRH(1-29) analogue without the albumin-binding drug affinity complex [5]"},{"field":"Origin and structure","a":"The 44-amino-acid sequence of human GRF with a trans-3-hexenoyl group attached at the N-terminal tyrosine; prepared as an acetate salt [1]","b":"A 29-amino-acid GHRH analogue (Tyr-D-Ala-Asp-Ala-Ile-Phe-Thr-Gln-Ser-Tyr-Arg-Lys-Val-Leu-Ala-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Leu-Ser-Arg-NH2) per FDA's characterisation [5]"},{"field":"Proposed mechanism","a":"Binds and stimulates human GRF receptors with potency similar to endogenous GRF, causing pulsatile release of endogenous growth hormone [1]","b":"Presumed GHRH receptor agonism by analogy; US FDA states it did not identify pharmacological studies of CJC-1295 free base or acetate and that it is unknown whether these forms are pharmacologically active [5]"},{"field":"Half-life","a":"About 11 minutes in healthy subjects after administration, per the US label [1]","b":"Not located for this form; unmodified GHRH(1-29)-NH2 had a disappearance half-time of about 4 minutes in healthy men, and the DAC modification was created specifically to overcome that short half-life [5, 9]"},{"field":"Highest human trial phase","a":"US FDA-approved product for HIV-associated abdominal fat (Egrifta); two phase 3 placebo-controlled trials [1, 3, 10]","b":"No human study of this form located; US FDA states there are no nonclinical or clinical data for CJC-1295 free base or acetate [5]"},{"field":"FDA status","a":"US FDA-approved for HIV-associated abdominal fat (Egrifta); initial US approval 2010, EGRIFTA WR label revised 03/2025 [1]","b":"Never US FDA-approved; CJC-1295 appears on the FDA compounding page among substances that may present significant safety risks (nomination withdrawn), as of 22 April 2026 [7]"},{"field":"Published human outcomes","a":"Visceral fat fell 15.2% versus a 5.0% rise with placebo in a 412-patient trial [2]; a pooled analysis of the same two phase 3 trials (806 patients) reported a 15.4% treatment effect [3]; liver fat fell more than placebo in a 61-patient trial [4]","b":"None located for the non-DAC form; the published human pharmacokinetic and growth hormone studies used a DAC-containing form, and FDA notes the salt forms were not specified [5, 6]"},{"field":"Safety signals","a":"Label warnings include neoplasm risk, elevated IGF-1, fluid retention, glucose intolerance, hypersensitivity and increased mortality in acute critical illness [1]","b":"No safety data for this form; FDA cites immunogenicity and characterisation concerns, limited water solubility, and notes genotoxicity signals and administration-site findings for DAC-containing forms in animals [5, 7]"},{"field":"WADA status","a":"Named under S2.2.4 (GHRH analogues); prohibited at all times (2026 List) [11]","b":"CJC-1295 is named under S2.2.4 (GHRH analogues); prohibited at all times (2026 List) [11]"},{"field":"Who funded the evidence","a":"Phase 3 registration sponsored by Theratechnologies [10]; later liver-fat trials funded by the US NIH [4]","b":"No sponsored research located; the available assessment is FDA's own review of nominated compounding substances [5, 6]"}],"title":"Tesamorelin vs CJC-1295 (no DAC)","verdict":["Approval: tesamorelin is US FDA-approved for HIV-associated abdominal fat (Egrifta); CJC-1295 without DAC has never been US FDA-approved [1, 7].","Evidence: tesamorelin has two phase 3 trials; US FDA found no clinical or nonclinical data for CJC-1295 free base or acetate [3, 5].","Characterisation: tesamorelin is defined by a US FDA-approved label for HIV-associated abdominal fat, while US FDA judged CJC-1295 substances not well characterised [1, 5]."],"id":"6add5a5a2fbcef8b86245eb0","created_date":"2026-10-25T01:24:42.962000","updated_date":"2026-10-25T01:24:42.962000"},{"a":"ipamorelin","b":"ghrp-2","differences":["Hormone selectivity: in swine, ipamorelin raised growth hormone without raising ACTH or cortisol, whereas GHRP-2 raised both [1].","Approval: GHRP-2 is an approved diagnostic product in Japan [6]; ipamorelin has no approval identified in the sources reviewed [2, 5].","Human endpoints studied: ipamorelin's largest trial was a therapeutic study in postoperative ileus that missed its endpoint [3], while GHRP-2's human data centre on diagnostic testing and appetite [8, 9].","Half-life: about 2 hours for ipamorelin in healthy subjects [2] versus about 0.42 to 0.69 hours for pralmorelin in healthy men [6], from different sources and assays.","FDA listing: both are 503B category 2 as of 22 April 2026, but the GHRP-2 entry is limited to injectable and nasal routes [5]."],"faqs":[{"q":"Is GHRP-2 approved anywhere?","a":"Yes, in Japan: pralmorelin hydrochloride is approved as a diagnostic agent for growth hormone secretion deficiency and has been marketed since February 2005 [6]. It is not US FDA-approved [5]."},{"q":"Is ipamorelin more selective than GHRP-2?","a":"In swine, ipamorelin raised growth hormone without raising ACTH or cortisol, while GHRP-2 and GHRP-6 raised both; this is animal data and was reported by the group that developed ipamorelin [1]."},{"q":"Have ipamorelin and GHRP-2 been compared in people?","a":"No head-to-head human trial was located. Side-by-side comparisons exist only in cell and animal experiments [1]."},{"q":"What safety concerns has the FDA raised?","a":"For ipamorelin, FDA cites two fatal serious adverse events among treated participants in a postoperative ileus study, with causality unclear [2]. For GHRP-2, it cites reports of serious adverse events including increased insulin requirement, deaths in critically ill study subjects, infection and pancreatitis, with causality not established [5]."}],"intro":"Ipamorelin and GHRP-2 are both synthetic growth hormone secretagogues that act at the ghrelin (GHS) receptor rather than the GHRH receptor [1, 10]. Ipamorelin is a pentapeptide developed at Novo Nordisk and described as the first GHS with GHRH-like selectivity, because in swine it raised growth hormone without raising ACTH or cortisol [1]. GHRP-2, also called pralmorelin, is approved in Japan as a diagnostic agent for growth hormone secretion deficiency, where it has been marketed since February 2005 [6]. Neither is US FDA-approved, and both appear on the FDA's compounding page of substances that may present significant safety risks, current as of 22 April 2026 [5].","last_reviewed":"2026-10-24","limited":"No head-to-head human trial was located. The only direct comparisons are animal and cell experiments in which ipamorelin and GHRP-2 were tested side by side for hormone release [1]. Their human evidence serves different purposes: a failed therapeutic trial for ipamorelin and diagnostic validation for GHRP-2 [3, 8]. FDA reviewers note that published ipamorelin studies often do not state which chemical form was used, limiting what can be concluded about marketed material [2]. Pharmacokinetic values come from different routes, populations and sources [2, 6].","published":true,"slug":"ipamorelin-vs-ghrp-2","table":[{"field":"Class","a":"Synthetic pentapeptide growth hormone secretagogue (ghrelin receptor agonist) [1]","b":"Synthetic growth hormone-releasing peptide / ghrelin receptor agonist; generic name pralmorelin [6, 7]"},{"field":"Origin and structure","a":"Aib-His-D-2-Nal-D-Phe-Lys-NH2, identified in a series lacking the central Ala-Trp dipeptide of GHRP-1; contains unnatural amino acids [1, 2]","b":"A hexapeptide derived from work on small GHRP analogues at Tulane University; marketed in Japan as pralmorelin hydrochloride [7, 10]"},{"field":"Proposed mechanism","a":"Acts through a GHRP-like receptor; in rat pituitary cells its potency resembled GHRP-6, and in swine it did not raise ACTH or cortisol [1]","b":"Stimulates growth hormone release at the GHS receptor; in conscious rats it raised growth hormone more than injected GHRH, and it also raised ACTH and corticosterone [10]"},{"field":"Half-life","a":"About 2 hours terminal half-life in healthy subjects after administration, per FDA's review of a published study [2]; about 27 minutes in rats [2]","b":"Elimination half-life of about 0.42 to 0.69 hours in 18 healthy men after administration, per the Japanese package insert [6]"},{"field":"Highest human trial phase","a":"Phase 2 (postoperative ileus after bowel resection, 117 patients) [3, 4]","b":"Approved diagnostic product in Japan; validation study in 77 healthy subjects and 58 patients with growth hormone deficiency [6, 8]"},{"field":"FDA status","a":"Not US FDA-approved; ipamorelin acetate is in 503B category 2 (added 29 September 2023) and also appears in the nominated-but-withdrawn section, as of 22 April 2026 [5]","b":"Not US FDA-approved; GHRP-2 for injectable and nasal routes is in 503B category 2 (added 29 September 2023), as of 22 April 2026 [5]"},{"field":"Published human outcomes","a":"In the phase 2 ileus trial, time to first tolerated meal did not differ significantly from placebo [3]","b":"Peak growth hormone after GHRP-2 was much lower in patients with growth hormone deficiency than in healthy subjects, supporting its diagnostic use [8]. In 7 healthy men, administration was followed by greater food intake than saline [9]"},{"field":"Safety signals","a":"FDA notes two fatal serious adverse events in ipamorelin-treated participants in the ileus study, with causality unclear, plus higher rates of hypokalaemia and hyperglycaemia [2]; the compounding page cites immunogenicity and characterisation concerns [5]","b":"FDA is aware of reports of serious adverse events in patients who received GHRP-2, including increased insulin requirement, deaths of critically ill study subjects, infection and pancreatitis, with causality not established [5]"},{"field":"WADA status","a":"Named under S2.2.4 as a growth hormone secretagogue; prohibited at all times (2026 List) [11]","b":"Named under S2.2.4 as GHRP-2 (pralmorelin); prohibited at all times (2026 List) [11]"},{"field":"Who funded the evidence","a":"Discovery work came from Novo Nordisk [1]; the phase 2 ileus trial was sponsored by Helsinn Therapeutics (U.S.) and reported from Ochsner Clinic Foundation [3, 4]","b":"Preclinical characterisation came from Kaken Pharmaceutical, which holds the Japanese product [6, 10]; the food-intake study was supported by US NIH grants [9]"}],"title":"Ipamorelin vs GHRP-2 (pralmorelin)","verdict":["Class: both act at the ghrelin receptor, not the GHRH receptor [1, 10].","Approval: GHRP-2 (pralmorelin) is an approved diagnostic in Japan; ipamorelin is approved nowhere in the sources reviewed [2, 6].","Evidence: ipamorelin's phase 2 ileus trial missed its endpoint; GHRP-2's human data are mainly diagnostic [3, 8]."],"id":"6add5a5a2fbcef8b86245ead","created_date":"2026-10-25T01:24:42.962000","updated_date":"2026-10-25T01:24:42.962000"},{"a":"sermorelin","b":"tesamorelin","differences":["Structure: sermorelin is the 29-residue N-terminal fragment of GHRH [1], whereas tesamorelin is the full 44-residue sequence with an N-terminal hexenoyl modification [6].","Current FDA status: tesamorelin is an approved, marketed product [6]; sermorelin's GEREF applications are listed as discontinued, although US FDA found they were not withdrawn for safety- or efficacy-related reasons [4, 5].","Approved use: sermorelin was studied for growth hormone deficiency in children [1, 2], whereas tesamorelin is indicated for excess abdominal fat in adults with HIV and lipodystrophy [6].","Half-life: about 4 minutes for GHRH(1-29)-NH2 in healthy men [3] versus about 11 minutes for tesamorelin in healthy subjects [6], measured by different routes and methods."],"faqs":[{"q":"Is sermorelin US FDA-approved?","a":"Sermorelin was approved as GEREF, but both GEREF applications are listed as discontinued in Drugs@FDA [4]. In 2013 the US FDA determined GEREF was not withdrawn from sale for safety- or efficacy-related reasons [5]."},{"q":"Is tesamorelin the same as sermorelin?","a":"No. Both are GHRH analogues, but sermorelin is a 29-amino-acid fragment while tesamorelin is the full 44-amino-acid sequence with a hexenoyl group added [1, 6]."},{"q":"Can sermorelin and tesamorelin be compared directly?","a":"Not on current evidence: no head-to-head trial was located, and they were tested in different populations for different outcomes [2, 7]."},{"q":"Are sermorelin and tesamorelin banned in sport?","a":"Yes. WADA's 2026 List names both under S2.2.4 as GHRH analogues, prohibited at all times [11]."}],"intro":"Sermorelin and tesamorelin are both synthetic analogues of growth hormone-releasing hormone (GHRH) that stimulate the pituitary to release growth hormone [1, 6]. Sermorelin is the 29-amino-acid N-terminal fragment of GHRH; it was US FDA-approved as GEREF, and both GEREF applications are now listed as discontinued [1, 4]. Tesamorelin is the full 44-amino-acid GHRH sequence with an added hexenoyl group, and it is US FDA-approved (first in 2010) for reducing excess abdominal fat in adults with HIV and lipodystrophy [6]. The two were developed for different conditions and have not been compared in a head-to-head trial in the sources reviewed [1, 7].","last_reviewed":"2026-10-24","limited":"No head-to-head trial of sermorelin and tesamorelin was located. Their main trials enrolled different populations (children with growth hormone deficiency versus adults with HIV-associated abdominal fat) and measured different outcomes (height velocity versus visceral fat), so results cannot be compared directly [2, 7]. The half-life figures come from different routes and study designs [3, 6]. Much of the sermorelin evidence predates modern trial reporting standards [1, 2].","published":true,"slug":"sermorelin-vs-tesamorelin","table":[{"field":"Class","a":"GHRH analogue [1]","b":"GHRH analogue (growth hormone-releasing factor analogue) [6]"},{"field":"Origin and structure","a":"29-amino-acid analogue of human GHRH, described as the shortest synthetic peptide with the full biological activity of GHRH [1]","b":"The 44-amino-acid sequence of human GRF with a trans-3-hexenoyl group attached at the N-terminal tyrosine [6]"},{"field":"Proposed mechanism","a":"Stimulates growth hormone secretion from the anterior pituitary [1]","b":"Binds and stimulates human GRF receptors with potency similar to endogenous GRF, causing pulsatile release of endogenous growth hormone [6]"},{"field":"Half-life","a":"Disappearance half-time of about 4 minutes for GHRH(1-29)-NH2 during administration in 10 healthy men [3]","b":"About 11 minutes in healthy subjects after administration, per the US label [6]"},{"field":"Highest human trial phase","a":"US FDA-approved product for HIV-associated abdominal fat (Egrifta); pivotal data include a 110-child multicentre open-label study in growth hormone deficiency [2, 4]","b":"US FDA-approved product for HIV-associated abdominal fat (Egrifta); two phase 3 placebo-controlled trials in HIV-associated abdominal fat [6, 8]"},{"field":"FDA status","a":"Approved as GEREF (NDA 019863, 1990; NDA 020443, 1997); both listed as discontinued in Drugs@FDA as of 24 October 2026 [4]. In 2013 US FDA determined that GEREF was not withdrawn from sale for safety- or efficacy-related reasons [5]","b":"US FDA-approved (initial US approval 2010); EGRIFTA WR label revised 03/2025 [6]"},{"field":"Published human outcomes","a":"In growth hormone-deficient children, mean height velocity rose in an open-label study [2]; a review notes increases were smaller than with somatropin [1]","b":"In a 412-patient phase 3 trial, visceral fat fell by 15.2% versus a 5.0% rise with placebo [7]; a 61-patient trial reported reduced liver fat in HIV with NAFLD [9]"},{"field":"Safety signals","a":"No adverse biochemical or hormonal changes, and no change in fasting glucose, were reported in the 110-child study [2]","b":"Label warnings include neoplasm risk, elevated IGF-1, fluid retention, glucose intolerance, hypersensitivity and increased mortality in acute critical illness [6]"},{"field":"WADA status","a":"Named under S2.2.4 (GHRH analogues); prohibited at all times (2026 List) [11]","b":"Named under S2.2.4 (GHRH analogues); prohibited at all times (2026 List) [11]"},{"field":"Who funded the evidence","a":"The paediatric efficacy study was run by the Geref International Study Group [2]; GEREF applications were held by EMD Serono [4]","b":"Phase 3 registration sponsored by Theratechnologies [10]; later liver-fat trials funded by the US NIH [9]"}],"title":"Sermorelin vs Tesamorelin","verdict":["Structure: sermorelin is a 29-residue GHRH fragment; tesamorelin is full-length 44-residue GHRH with a hexenoyl group [1, 6].","Approval: tesamorelin is US FDA-approved and marketed; sermorelin's GEREF approvals are listed as discontinued (as of October 2026) [4, 6].","Use studied: sermorelin in children with growth hormone deficiency; tesamorelin in adults with HIV-associated abdominal fat [2, 7]."],"id":"6add5a5a2fbcef8b86245eab","created_date":"2026-10-25T01:24:42.962000","updated_date":"2026-10-25T01:24:42.962000"},{"a":"tesamorelin","b":"ipamorelin","differences":["Receptor target: tesamorelin acts on GRF (GHRH) receptors, while ipamorelin acts through a GHRP-like (ghrelin-type) receptor [1, 6].","Approval: tesamorelin is US FDA-approved for one HIV-related indication; ipamorelin is not approved [1, 9].","Evidence base: tesamorelin has phase 3 data in more than 800 patients, while ipamorelin has one small phase 2 trial that did not meet its endpoints [4, 8].","Half-life: minutes for tesamorelin versus about 2 hours for ipamorelin in healthy subjects [1, 7].","Both are prohibited in sport under WADA class S2.2.4 [11]."],"faqs":[{"a":"No. Tesamorelin is a GRF (GHRH) analog, while ipamorelin is a GH secretagogue acting through a GHRP-like receptor [1, 6].","q":"Do tesamorelin and ipamorelin act on the same receptor?"},{"a":"Yes, since 2010, for reduction of excess abdominal fat in HIV-infected adults with lipodystrophy [1, 10].","q":"Is tesamorelin US FDA-approved?"},{"a":"Its phase 2 postoperative ileus trial showed no significant differences from placebo in efficacy analyses [8].","q":"Have studies shown results for tesamorelin or ipamorelin?"},{"a":"Tesamorelin's mean elimination half-life was 8-11 minutes and ipamorelin's terminal half-life was about 2 hours in healthy subjects [1, 2, 7].","q":"How do their half-lives compare?"},{"a":"Both are named under S2.2.4 of WADA's 2026 List [11].","q":"Are they prohibited in sport?"}],"intro":"Tesamorelin and ipamorelin both raise growth hormone, but through different receptors: tesamorelin is a GHRH analog and ipamorelin is a GH secretagogue acting through a GHRP-like receptor [1, 6]. Tesamorelin is US FDA-approved for one indication in HIV-associated lipodystrophy, while ipamorelin has no approval and its one efficacy trial did not show improvement over placebo [1, 8, 10]. This page compares their pharmacology, evidence and regulatory status as of 22 October 2026.","last_reviewed":"2026-10-22","limited":"No head-to-head study of tesamorelin and ipamorelin was identified. Tesamorelin's evidence comes from trials in HIV-associated lipodystrophy, and its label covers only that use [1, 3, 4]. Ipamorelin's human data are a pharmacokinetic study in healthy men and one small proof-of-concept trial in surgical patients [7, 8]. The label notes that the effects of prolonged IGF-1 elevation are unknown [1].","published":true,"slug":"tesamorelin-vs-ipamorelin","table":[{"a":"GHRH (GRF) analog [1]","b":"GH secretagogue (GHRP-like pentapeptide) [6]","field":"Class"},{"a":"44-amino-acid human GRF sequence with an N-terminal hexenoyl group, as an acetate salt [1]","b":"Synthetic pentapeptide from Novo Nordisk's GH secretagogue program [6]","field":"Origin and structure"},{"a":"Binds and stimulates GRF receptors, increasing GH and then IGF-1 [1]","b":"Releases GH through a GHRP-like receptor [6]","field":"Proposed mechanism"},{"a":"Mean elimination half-life of 11 minutes (Egrifta WR) and 8 minutes (Egrifta SV) in healthy subjects [1, 2]","b":"Terminal half-life of about 2 hours in healthy men [7]","field":"Half-life"},{"a":"Phase 3 randomized trials [3, 4]","b":"Phase 2 randomized trial [8]","field":"Highest human trial phase"},{"a":"Approved (2010) for reduction of excess abdominal fat in HIV-infected adults with lipodystrophy [1, 10]","b":"Not approved; US FDA proposed in 2024 not to add it to the 503A bulks list [9]","field":"FDA status"},{"a":"In a 412-patient trial, visceral fat fell 15.2% versus a 5.0% rise with placebo [3]","b":"In 117 patients after bowel resection, no significant difference from placebo on efficacy endpoints [8]","field":"Published human outcomes"},{"a":"Label warnings include elevated IGF-1, fluid retention, glucose intolerance and hypersensitivity [1]","b":"FDA noted more hypokalemia, insomnia and hyperglycemia in the ipamorelin arm of the ileus trial [9]","field":"Safety signals"},{"a":"Named under S2.2.4 as a GHRH analog; prohibited at all times [11]","b":"Named under S2.2.4 as a GH secretagogue; prohibited at all times [11]","field":"WADA status"},{"a":"Large randomized phase 3 trials in a specific population [3, 4]","b":"Animal pharmacology, a PK study and one small phase 2 trial [6, 7, 8]","field":"Evidence level"}],"title":"Tesamorelin vs ipamorelin","verdict":["Approval: Tesamorelin is US FDA-approved (2010) for one HIV-related lipodystrophy indication; ipamorelin is not approved [1, 9].","Human evidence: Tesamorelin has phase 3 data in more than 800 patients; ipamorelin has one small phase 2 trial that did not meet its endpoints [4, 8].","Mechanism: Tesamorelin acts on GRF (GHRH) receptors; ipamorelin acts through a GHRP-like (ghrelin-type) receptor [1, 6]."],"id":"6adaa234c03613717e7bdcd2","created_date":"2026-10-22T23:54:28.477000","updated_date":"2026-10-25T01:05:38.112000"},{"a":"sermorelin","b":"cjc-1295-no-dac","differences":["Approval history: sermorelin was US FDA-approved as Geref until 2009, while CJC-1295 without DAC has never been US FDA-approved [1, 7].","Human data: sermorelin has published pediatric and diagnostic studies, while FDA identified no human data for CJC-1295 without DAC [3, 4, 7].","Structure: CJC-1295 is described as a tetrasubstituted form of hGRF(1-29), while sermorelin is described as a 29-amino-acid analog of GHRH [3, 5].","Naming risk: FDA notes that 'CJC-1295' is used for both DAC and non-DAC structures, which complicates identification [7].","Both are covered by WADA's S2.2.4 class of GHRH analogs [10]."],"faqs":[{"a":"No. Both are based on GHRH(1-29), but CJC-1295 is a substituted version of that sequence [3, 5].","q":"Are sermorelin and CJC-1295 without DAC the same molecule?"},{"a":"Yes. Geref was approved in 1990 and 1997 and withdrawn established 2009 after discontinuation by the sponsor; US FDA determined in 2013 that this was not for safety or efficacy reasons [1].","q":"Was sermorelin ever US FDA-approved?"},{"a":"FDA's 2024 review found no nonclinical or clinical data to assess its safety and efficacy [7].","q":"Is there human research on CJC-1295 without DAC?"},{"a":"No data specific to the non-DAC form were identified; the DAC group is the feature that binds albumin and extends half-life [5, 7].","q":"Does CJC-1295 without DAC last as long as the DAC form?"},{"a":"Sermorelin and CJC-1295 are both named as GHRH analogs under S2.2.4 of WADA's 2026 List [10].","q":"Are they prohibited in sport?"}],"intro":"Sermorelin and CJC-1295 without DAC are both analogs of the first 29 residues of human growth hormone-releasing hormone (GHRH) [3, 7]. Sermorelin was once an US FDA-approved product (Geref) with published pediatric data, while US FDA found no nonclinical or clinical data to assess the safety and efficacy of CJC-1295 without DAC [1, 7]. Without the drug affinity complex, CJC-1295 lacks the albumin-binding group that gives the DAC form its multi-day half-life [5, 7].","last_reviewed":"2026-10-22","limited":"No head-to-head study of sermorelin and CJC-1295 without DAC was identified. Sermorelin's clinical evidence dates mainly from the 1990s and is open-label without placebo control [3, 4]. For CJC-1295 without DAC, US FDA found no nonclinical or clinical data, so its pharmacology, half-life and safety are not established [7]. Data from the DAC form should not be read across to the non-DAC peptide [7].","published":true,"slug":"sermorelin-vs-cjc-1295-no-dac","table":[{"a":"GHRH analog [3]","b":"GHRH analog [7]","field":"Class"},{"a":"29-amino-acid analog of human GHRH, the shortest synthetic peptide with full GHRH activity [3]","b":"Substituted form of hGRF(1-29) without the C-terminal maleimidopropionamide-lysine (DAC) group [5, 7]","field":"Origin and structure"},{"a":"Stimulates GH secretion from the anterior pituitary [3]","b":"Expected to act at the GHRH receptor, but US FDA found no nonclinical studies establishing its activity [7]","field":"Proposed mechanism"},{"a":"Not identified in the primary sources reviewed","b":"No data specific to this form were identified [7]","field":"Half-life"},{"a":"Multicenter open-label pediatric study (110 children) supporting a former approval [4]","b":"No human studies identified [7]","field":"Highest human trial phase"},{"a":"Geref approvals (1990, 1997) withdrawn established 2009 after sponsor discontinuation, not for safety or efficacy reasons; no current product [1, 2]","b":"Not approved; US FDA proposed in 2024 that it not be added to the 503A bulks list; no DailyMed label [7, 9]","field":"FDA status"},{"a":"Mean height velocity rose from 4.1 to 8.0 cm/yr in GH-deficient children [4]","b":"None identified [7]","field":"Published human outcomes"},{"a":"FDA's 2013 review of postmarketing data concluded Geref was not withdrawn for safety reasons [1]","b":"FDA cites immunogenicity and characterization concerns for CJC-1295 substances [7, 8]","field":"Safety signals"},{"a":"Named under S2.2.4 as a GHRH analog; prohibited at all times [10]","b":"CJC-1295 named under S2.2.4 as a GHRH analog; prohibited at all times [10]","field":"WADA status"},{"a":"Human pediatric open-label and diagnostic data [3, 4]","b":"No direct evidence; regulatory review only [7]","field":"Evidence level"}],"title":"Sermorelin vs CJC-1295 (no DAC)","verdict":["Approval: Sermorelin was US FDA-approved as Geref until a 2009 withdrawal for non-safety reasons; CJC-1295 without DAC has never been US FDA-approved [1, 7].","Human evidence: Sermorelin has published pediatric and diagnostic studies; FDA identified no human data for CJC-1295 without DAC [3, 4, 7].","Mechanism: Both are GHRH(1-29) analogs; CJC-1295 is a tetrasubstituted form, and US FDA found no nonclinical studies establishing its activity [3, 5, 7]."],"id":"6adaa234c03613717e7bdcd1","created_date":"2026-10-22T23:54:28.477000","updated_date":"2026-10-25T01:05:37.073000"},{"a":"ipamorelin","b":"ghrp-6","differences":["Stress-axis effects: in swine, GHRP-6 raised ACTH and cortisol while ipamorelin did not beyond GHRH levels (animal data) [1].","Size: ipamorelin is a pentapeptide and GHRP-6 a hexapeptide [1, 5].","Clinical development: ipamorelin reached a phase 2 efficacy trial, which did not meet its endpoints, whereas GHRP-6 human data are mainly diagnostic and physiology studies [3, 6].","Pharmacokinetics: a human terminal half-life of about 2 hours is reported for ipamorelin; none was found for GHRP-6 [2].","FDA compounding categories differ: ipamorelin is on the 503B category 2 list, and GHRP-6 is in 503A category 3 [10, 11]."],"faqs":[{"a":"Both are GH secretagogues; ipamorelin acts through a GHRP-like receptor and GHRP-6 through the GH secretagogue receptor, whose natural ligand is ghrelin [1, 7, 8].","q":"Do ipamorelin and GHRP-6 act on the same receptor?"},{"a":"In swine, ipamorelin did not raise ACTH or cortisol beyond GHRH levels, while GHRP-6 did; this is animal data [1].","q":"Is ipamorelin more selective than GHRP-6?"},{"a":"Ipamorelin was tested in a phase 2 postoperative ileus trial that showed no significant difference from placebo [3]. GHRP-6 has been used in diagnostic GH testing [6].","q":"Has either been tested in a clinical trial?"},{"a":"Neither is approved; US FDA proposed not adding ipamorelin to the 503A bulks list and places GHRP-6 in 503A category 3 [4, 11].","q":"What is their FDA status?"},{"a":"Both are named under S2.2.4 of WADA's 2026 List and are prohibited at all times [12].","q":"Are they prohibited in sport?"}],"intro":"Ipamorelin and GHRP-6 are synthetic growth hormone secretagogues that act through the ghrelin (GH secretagogue) receptor system [1, 7, 8]. They were compared directly in animal pharmacology, where ipamorelin released GH without the ACTH and cortisol rise seen with GHRP-6 [1]. Neither is approved by the US FDA, and both are named on WADA's 2026 Prohibited List [4, 11, 12].","last_reviewed":"2026-10-22","limited":"The only direct comparison identified is animal pharmacology in rats and swine [1]. Human data for GHRP-6 are small, short physiology and diagnostic studies, and the single ipamorelin efficacy trial was a small proof-of-concept study in a surgical population that did not show improvement over placebo [3, 5, 6]. Long-term human safety data were not identified for either compound.","published":true,"slug":"ipamorelin-vs-ghrp-6","table":[{"a":"Pentapeptide GH secretagogue [1]","b":"Hexapeptide GH-releasing peptide [5]","field":"Class"},{"a":"Synthetic pentapeptide from Novo Nordisk's GH secretagogue program [1]","b":"Synthetic hexapeptide His-D-Trp-Ala-Trp-D-Phe-Lys-NH2 [5]","field":"Origin and structure"},{"a":"Releases GH through a GHRP-like receptor [1]","b":"Acts on the GH secretagogue receptor, whose endogenous ligand is ghrelin [7, 8]","field":"Proposed mechanism"},{"a":"Terminal half-life of about 2 hours in healthy men [2]","b":"Not identified in the sources reviewed","field":"Half-life"},{"a":"Phase 2 randomized trial in postoperative ileus (117 enrolled) [3]","b":"Small physiology and diagnostic-test studies [5, 6]","field":"Highest human trial phase"},{"a":"Not approved; US FDA proposed in 2024 not to add it to the 503A bulks list; on FDA's 503B category 2 list [4, 10]","b":"Not approved; listed in 503A category 3 (nominated without adequate support) [11]","field":"FDA status"},{"a":"No significant difference from placebo in time to first tolerated meal (25.3 versus 32.6 hours, p = 0.15) [3]","b":"As a GH provocation test in 49 patients, GHRP-6 alone was highly specific but less sensitive than the insulin tolerance test [6]","field":"Published human outcomes"},{"a":"FDA noted more hypokalemia, insomnia and hyperglycemia and deaths of unclear relationship in the ipamorelin arm of the ileus trial [4]","b":"Slight rises in prolactin and cortisol after use in 6 healthy men [5]","field":"Safety signals"},{"a":"Named under S2.2.4 as a GH secretagogue; prohibited at all times [12]","b":"Named under S2.2.4 as a GH-releasing peptide; prohibited at all times [12]","field":"WADA status"},{"a":"Animal pharmacology, a human PK study and one phase 2 trial [1, 2, 3]","b":"Small human endocrine and diagnostic studies plus cell data [5, 6, 9]","field":"Evidence level"}],"title":"Ipamorelin vs GHRP-6","verdict":["Approval: Neither is US FDA-approved; ipamorelin is on the 503B category 2 list and GHRP-6 is in 503A category 3 [4, 10, 11].","Human evidence: Ipamorelin reached a phase 2 trial that did not meet its endpoints; GHRP-6 human data are mainly diagnostic and physiology studies [3, 6].","Mechanism: Both act via the ghrelin receptor system; in swine, GHRP-6 raised ACTH and cortisol while ipamorelin did not beyond GHRH levels [1, 7, 8]."],"id":"6adaa1f7dec8cf73bd0f6281","created_date":"2026-10-22T23:53:27.146000","updated_date":"2026-10-25T01:05:35.370000"},{"a":"ghrp-2","b":"ghrp-6","differences":["Potency and efficacy: in swine, GHRP-2 showed higher potency but lower maximal efficacy than GHRP-6 for GH release (animal data) [2].","Stress-axis effects: both raised ACTH and cortisol in swine [2]; in humans, GHRP-6 raised ACTH and cortisol [5] and the ACTH response to GHRP-2 is used as a diagnostic readout [4].","Appetite: increased food intake has been documented in a small human study of GHRP-2 [3]. No equivalent human feeding study of GHRP-6 was identified.","Clinical-trial evidence: GHRP-6 appears in a phase 3 combination trial with EGF in stroke that missed its primary endpoint [8], whereas GHRP-2 is documented mainly as a diagnostic test in humans [4].","FDA-cited concerns differ: for GHRP-2, serious adverse event reports of unestablished causality; for GHRP-6, effects on cortisol and blood glucose [9].","Both are named in WADA class S2.2.4 and are prohibited at all times [10]."],"faqs":[{"q":"Do GHRP-2 and GHRP-6 act on the same receptor?","a":"Both are described as synthetic agonists of the ghrelin (GH secretagogue) receptor and are thought to share receptor and cellular mechanisms [1, 3]."},{"q":"Have they been compared directly?","a":"In swine (animal data), GHRP-2 had higher potency but lower efficacy than GHRP-6 for GH release, and both raised ACTH and cortisol [2]. No head-to-head human trial was identified."},{"q":"Has GHRP-6 been tested in a clinical trial?","a":"A 2026 phase 3 trial tested EGF combined with GHRP-6 in acute ischemic stroke and missed its primary endpoint; a subgroup analysis in severe stroke was exploratory [8]."},{"q":"What does the FDA say about them?","a":"The US FDA lists both among bulk substances for compounding that may present significant safety risks, citing serious adverse event reports of unestablished causality for GHRP-2 and cortisol and blood-glucose effects for GHRP-6 [9]."},{"q":"Are they prohibited in sport?","a":"WADA's 2026 Prohibited List names GHRP-2 (pralmorelin) and GHRP-6 under S2.2.4, and both are prohibited at all times [10]."}],"intro":"GHRP-2 and GHRP-6 are synthetic growth hormone-releasing peptides from the same pharmacological family; both are thought to act through the growth hormone secretagogue (ghrelin) receptor [1, 3]. They differ in potency and efficacy in animal pharmacology, in the human and animal studies available, and in the concerns the US FDA lists for each [2, 9]. Neither is an approved medicine in the sources reviewed, and both are named on WADA's 2026 Prohibited List [9, 10].","last_reviewed":"2026-10-22","limited":"Evidence for both compounds is limited [2, 8]. No head-to-head human trial was identified, and the direct comparisons available are animal pharmacology [2]. The human GHRP-2 and GHRP-6 studies are small physiology or diagnostic studies, and the only trial of GHRP-6 in patients tested a combination product [3, 4, 5, 8]. No half-life figure for either compound was found in the sources reviewed. The FDA notes that causality for the adverse event reports it cites for GHRP-2 has not been established [9].","published":true,"slug":"ghrp-2-vs-ghrp-6","table":[{"field":"Class","a":"Synthetic GH-releasing peptide; ghrelin-receptor agonist [3]","b":"Synthetic GH-releasing hexapeptide that acts on the ghrelin-receptor system [1, 8]"},{"field":"Origin and structure","a":"Unnatural (synthetic) GHRP; the FDA notes it contains an unnatural amino acid that complicates characterization [1, 9]","b":"Unnatural (synthetic) GHRP [1]"},{"field":"Proposed mechanism","a":"Binds the GH secretagogue receptor, stimulating GH release and, in humans, appetite [3]","b":"Stimulates GH release; like ghrelin, it also raised ACTH and cortisol in human studies [5]"},{"field":"Half-life","a":"Not identified in the sources reviewed","b":"Not identified in the sources reviewed"},{"field":"Highest human trial phase","a":"Small physiology studies and diagnostic-test studies in humans [3, 4]","b":"Small physiology studies; as a component of a combination with EGF, a phase 3 open-label stroke trial [5, 8]"},{"field":"FDA status","a":"Listed by the FDA among bulk substances for compounding that may present significant safety risks (injectable and nasal routes) [9]","b":"Listed on the same FDA page, with limited safety information [9]"},{"field":"Published human outcomes","a":"In 7 lean men, intake at a buffet meal was 35.9% higher during administration than with saline, and serum GH rose [3]. In 36 patients, the ACTH response in a GHRP-2 test helped identify secondary adrenal insufficiency [4]","b":"In 9 adults with type 1 diabetes and 9 controls, GHRP-6 released GH, ACTH and cortisol, with responses similar between groups and a smaller GH response than ghrelin [5]. In a phase 3 stroke trial of EGF plus GHRP-6 (188 patients), the primary endpoint was missed [8]"},{"field":"Safety signals","a":"FDA is aware of reports of increased insulin requirement, death of critically ill study subjects, infection and pancreatitis, though causality has not been established [9]","b":"FDA cites potential effects on cortisol and increased blood glucose from decreased insulin sensitivity [9]"},{"field":"WADA status","a":"Named under S2.2.4 as GHRP-2 (pralmorelin); prohibited at all times [10]","b":"Named under S2.2.4 as GHRP-6; prohibited at all times [10]"},{"field":"Evidence level","a":"Small human physiology studies plus animal and cell data [3, 4, 6]","b":"Small human physiology studies, a combination-product trial and animal data [5, 7, 8]"}],"title":"GHRP-2 vs GHRP-6","verdict":["Approval: Neither is an approved medicine in the sources reviewed; US FDA lists both among compounding substances that may present significant safety risks [9].","Human evidence: GHRP-2 is documented mainly as a diagnostic test; GHRP-6 appears in a phase 3 combination stroke trial with EGF that missed its primary endpoint [4, 8].","Mechanism: Both act via the ghrelin receptor; in swine, GHRP-2 showed higher potency but lower maximal GH efficacy than GHRP-6 [1, 2, 3]."],"id":"6ada7efce46e66bc14222ba2","created_date":"2026-10-22T21:24:12.387000","updated_date":"2026-10-25T01:05:35.070000"}],"Article?q=%7B%22topic%22%3A%22Questions%22%2C%22compounds%22%3A%7B%22%24in%22%3A%5B%22tesamorelin%22%2C%22sermorelin%22%2C%22cjc-1295-no-dac%22%2C%22ipamorelin%22%2C%22ghrp-2%22%2C%22ghrp-6%22%5D%7D%7D":[{"compounds":["tesamorelin"],"faqs":[],"intro":"Tesamorelin is a growth hormone-releasing factor analog, US FDA-approved only for excess abdominal fat in adults with HIV-related lipodystrophy [1, 2]. Almost all human evidence comes from that group, so label figures below do not extend to other uses [1, 3].","kind":"blog","known":["In two phase 3 trials in adults with HIV, visceral fat changed by -27 and -21 cm2 versus +4 and 0 cm2 with placebo [1].","Visceral fat returned in people switched to placebo after week 26 [1].","Tesamorelin raises IGF-1; 47% of treated patients had IGF-1 above 2 standard deviation scores [1].","New HbA1c of 6.5% or higher occurred in 5% versus 1% with placebo [1].","Small randomized trials in people with HIV reported lower liver fat than placebo [5, 6]."],"published":true,"slug":"tesamorelin-questions-answered","title":"Tesamorelin: Dosage, Side Effects, Results and Legality, Answered","topic":"Questions","unknown":["Long-term cardiovascular safety, which the labels say has not been established.","The effects of prolonged IGF-1 elevation.","Efficacy and safety outside HIV-associated lipodystrophy, including in healthy adults or athletes.","Use in people over 65, in children, and in kidney or liver impairment.","Effects of combining tesamorelin with other growth hormone secretagogues or with incretin drugs."],"id":"6add3bf5868d820382afa034","created_date":"2026-10-24T23:15:01.692000","updated_date":"2026-10-24T23:34:04.098000"},{"compounds":["sermorelin"],"faqs":[],"intro":"Sermorelin is a 29-amino-acid GHRH analog once US FDA-approved as Geref for children with growth hormone deficiency, then discontinued by its maker [1, 2]. It has no current approval anywhere, and its human evidence is mostly older pediatric and diagnostic studies, not adult wellness use [1, 3].","kind":"blog","known":["Geref was approved in 1990 and 1997, discontinued by its sponsor in 2008, and withdrawn established 2009 [1].","US FDA determined in 2013 that Geref was not withdrawn for reasons of safety or efficacy [1].","In 110 children with growth hormone deficiency, mean growth rate rose from 4.1 to 7.2 cm a year, without a placebo group [3].","Transient facial flushing and pain at the administration area were among the most common reactions in children [2].","Sermorelin is prohibited at all times in sport under WADA's S2 category [5]."],"published":true,"slug":"sermorelin-questions-answered","title":"Sermorelin: FDA Status, Side Effects and Evidence, Answered","topic":"Questions","unknown":["Any effect on muscle, fat, testosterone or aging in adults; no controlled adult trial was identified.","Effect on final adult height in treated children.","Frequencies of adverse events and elimination half-life, which were not found in the sources reviewed.","Long-term safety, including cancer risk.","Whether products sold in other forms deliver any active peptide."],"id":"6add3bf35c6258e9859fedfa","created_date":"2026-10-24T23:14:59.792000","updated_date":"2026-10-24T23:33:00.838000"},{"compounds":["cjc-1295-no-dac-ipamorelin","ipamorelin"],"faqs":[],"intro":"CJC-1295/ipamorelin is a combination of two unapproved growth hormone-releasing peptides; see our CJC-1295 (no DAC) + ipamorelin reference for the full record. The key fact: no study has tested the combination, and the human CJC-1295 trials used a different molecule, the DAC form [2, 10].","kind":"blog","known":["Ipamorelin released growth hormone in rat cells, rats and pigs, and in pigs did not raise cortisol beyond the GHRH response [3].","In healthy men, ipamorelin produced a single growth hormone peak and had a terminal half-life of about 2 hours [4].","In a phase 2 trial after bowel surgery, ipamorelin did not differ from placebo on efficacy endpoints [5].","The DAC form of CJC-1295 raised growth hormone and IGF-1 for several days in healthy adults; the no-DAC form was not studied [2].","Both peptides are prohibited at all times under WADA section S2.2.4 [9]."],"published":true,"slug":"cjc-1295-no-dac-ipamorelin-questions-answered","title":"CJC-1295/Ipamorelin: Side Effects, Evidence and Legality, Answered","topic":"Questions","unknown":["Whether the combination differs from either peptide alone on any outcome, in animals or humans.","Human pharmacokinetics of the no-DAC GRF(1-29) component.","Stability and compatibility of the two peptides mixed in one vial.","Long-term safety, glucose effects and immunogenicity of the mixture.","Any effect on body fat, muscle, sleep or height in people."],"id":"6add3becacf447ae7e4a174a","created_date":"2026-10-24T23:14:52.248000","updated_date":"2026-10-24T23:34:02.822000"}]}}