Ipamorelin is a synthetic pentapeptide and the first growth hormone secretagogue described as genuinely selective. Earlier compounds in this class stimulated growth hormone release but also raised cortisol, prolactin and adrenocorticotropic hormone; ipamorelin’s defining characteristic in the original pharmacology work was that it did not. This selectivity is the basis of its continued use in performance and longevity practice. Its formal clinical development took a different direction – it was investigated for postoperative ileus, reaching Phase III, where it did not meet its primary endpoint, and development ceased. It therefore holds no marketing authorisation for any indication. Practitioners should be clear that its endocrine pharmacology is well described while its clinical benefit for body composition or recovery has not been established in trials.
Active Compound: Ipamorelin
Permitted Claim GuidelinesA selective growth hormone secretagogue characterised in human clinical trials. Used under practitioner supervision with appropriate endocrine monitoring.
Mechanism of ActionBinds the growth hormone secretagogue receptor (GHS-R1a), the ghrelin receptor, on pituitary somatotrophs. Stimulates growth hormone release directly and reduces somatostatin inhibitory tone. Its receptor selectivity accounts for the absence of significant cortisol and prolactin elevation seen with less selective secretagogues.
Evidence Grade: B - Phase III human safety data; efficacy endpoint not met, different indication
Clinical Evidence BaseWell-characterised preclinical pharmacology establishing selectivity. Human Phase II and III trials in postoperative ileus demonstrated acceptable tolerability but did not meet efficacy endpoints. No controlled trials for body composition, recovery or ageing endpoints.
Literature & ReferencesRaun K et al. Eur J Endocrinol, 1998 - ipamorelin, the first selective growth hormone secretagogue. | Beck DE et al. Am J Surg, 2014 - Phase III evaluation in postoperative ileus. | Gobburu JV et al. Pharm Res, 1999 - pharmacokinetic-pharmacodynamic modelling of ipamorelin.
Safety & PrecautionsGenerally well tolerated in trials. Reported effects include injection-site reactions, headache, lightheadedness and increased appetite reflecting ghrelin-receptor activity. Sustained growth hormone elevation may produce fluid retention, arthralgia and reduced insulin sensitivity. Contraindicated where malignancy is present or suspected. IGF-1 and glucose monitoring is advised in continued use.
ContraindicationsActive or suspected malignancy; pregnancy and breastfeeding; proliferative diabetic retinopathy; acute critical illness; known hypersensitivity.
Storage & HandlingStore lyophilised vial at 2-8 C, protected from light.
Regulatory StatusNot authorised as a medicine in any major market. Prohibited in sport under the WADA Prohibited List (S2). Supplied only through appropriate professional, prescription-led channels.