Ipamorelin
/ Pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) ghrelin / GHS-R1a receptor agonistTerms in this page you can click for a plain-English popup: , , , , , , , .
Helsinn/Ipsen Phase 2b in postoperative ileus missed its primary endpoint (2012). No approved indications. 503A Category 2.
Ipamorelin is a pentapeptide ghrelin/GHS-R1a receptor agonist (growth hormone secretagogue). It is selective for GH release with minimal effect on ACTH, cortisol, or prolactin — distinguishing it from older GHRPs such as GHRP-6 and hexarelin. Short half-life of approximately 2 hours.
No approvals. Helsinn/Ipsen developed ipamorelin for postoperative ileus through Phase 2b; program discontinued in 2012 after the trial missed its primary endpoint. Published human data is limited to single-dose Phase 1 PK/PD characterization.
Generally mild in trials: flushing, headache, transient hyperglycemia at higher doses. No cortisol or prolactin elevation. Long-term human data absent.
Regulatory status
- FDA status:
- Not FDA-approved
- Compounding:
- 503A Category 2 — do-not-compound pending review
FDA’s 2023 503A bulk drug substance evaluation placed ipamorelin in Category 2 — not on the positive bulk list. Multiple FDA warning letters (2023-2024) have been issued to compounders selling ipamorelin and CJC-1295/ipamorelin blends. The CJC-1295 + ipamorelin combination is the most commonly compounded regimen in the category but has no published clinical trials of the combination.