Ipamorelin
Growth hormone secretagogue (ghrelin receptor agonist)
Status
Not approved
Never approved; development for postoperative ileus ended after a negative phase 2 trial, FDA's compounding advisory committee voted 12-0 (one abstention) in October 2024 against adding it to the 503A bulks list, and it remains on FDA's 503B Category 2 list of substances raising significant safety risks.
Evidence
Preliminary
Human data are limited to a pharmacokinetic study in healthy men and one small phase 2 trial that missed its main endpoint.
In sport
WADAProhibited (WADA)
Ipamorelin is a small synthetic peptide that mimics the hunger hormone ghrelin to trigger growth hormone release. Developed by Novo Nordisk and later tested for bowel recovery after surgery, it was never approved and is sold online as a research chemical.
Structure
5 residuesPoint at a bead, or focus the chain and use the arrow keys, to name it. Pick a chemistry to highlight it.
D-form (mirror image), shown in lower case
Sequence as text
H-Aib-H-D-2Nal-D-Phe-K-NH2
What it is used for
- Postoperative ileus (slow return of bowel function) after bowel surgery (studied)
- Growth hormone deficiency, the use proposed for compounding (claimed, unproven)
- Muscle gain, fat loss, sleep or anti-ageing (claimed, unproven)
How it works
Ipamorelin activates the growth hormone secretagogue receptor (the ghrelin receptor) in the pituitary and hypothalamus, producing a single short burst of growth hormone. In animal studies it was notably selective: unlike GHRP-6 and GHRP-2, it did not raise ACTH or cortisol even at doses far above those needed for growth hormone release, and it did not change other pituitary hormones. Ghrelin receptor activation also stimulates gut movement, which is why it was tested for postoperative ileus.
How strong the evidence is
Preliminary
Raun and colleagues (1998) described its potency and selectivity in rat and pig studies. In healthy men given intravenous infusions, it produced a single growth hormone peak about 40 minutes later and had a terminal half-life of about 2 hours (Gobburu 1999). A phase 2 randomized trial in 117 bowel resection patients found no significant difference from placebo in time to first tolerated meal (25.3 versus 32.6 hours, p = 0.15), and development was discontinued (Beck 2014). FDA's 2024 review found no data supporting effectiveness for growth hormone deficiency.
Risks and side effects
- Two deaths from surgical complications occurred in ipamorelin-treated patients in the ileus trial; FDA could not rule out a link
- Higher rates of low potassium and high blood sugar were reported with ipamorelin in that trial
- Immunogenicity and impurity risks from its unnatural amino acids flagged by FDA
- Research-chemical products are unregulated and of uncertain purity
- Prohibited in sport at all times (WADA S2)
Regulatory status
Status by country
| Jurisdiction | Status | Source |
|---|---|---|
| USUnited States | No authorised medicine | Source 5 |
| EUEuropean Union | No authorised medicine | Source 9 |
| UKUnited Kingdom | No authorised medicine | Source 10 |
| AUAustralia | No authorised medicine | Source 11 |
| CACanada | No authorised medicine | Source 12 |
Timeline
Articles about Ipamorelin
Sources
- 01Ipamorelin (CID 9831659)(opens the source in a new tab)
- 02Ipamorelin, the first selective growth hormone secretagogue(opens the source in a new tab)
- 03Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers(opens the source in a new tab)
- 04Prospective, randomized, controlled, proof-of-concept study of the ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients(opens the source in a new tab)
- 05FDA Briefing Document: ipamorelin, Pharmacy Compounding Advisory Committee, October 29, 2024(opens the source in a new tab)
- 06Pharmacy Compounding Advisory Committee meeting, October 29, 2024: minutes(opens the source in a new tab)
- 07Safety Risks Associated with Certain Bulk Drug Substances Nominated for Use in Compounding (Category 2)(opens the source in a new tab)
- 08World Anti-Doping Code International Standard: Prohibited List 2026(opens the source in a new tab)
- 09Find medicine: centrally authorised medicines(opens the source in a new tab)
- 10MHRA Products: active substances beginning with I(opens the source in a new tab)
- 11Australian Register of Therapeutic Goods (ARTG)(opens the source in a new tab)
- 12Think twice before injecting peptides bought online: unauthorized products can seriously harm you(opens the source in a new tab)
Educational information, not medical advice. Talk to a licensed clinician before starting, stopping or changing any medicine.