Ipamorelin: The Complete Guide

Key Facts

Full name: Ipamorelin (NNC 26-0161)
Type: Synthetic pentapeptide growth hormone secretagogue
Origin: Developed by Novo Nordisk as a selective ghrelin receptor (GHS-R1a) agonist
Studied for: Growth hormone release, body composition, post-operative ileus, anti-aging
Administration: Subcutaneous injection
Common side effects: Generally well-tolerated — headache, lightheadedness, water retention
Safety alerts: Not FDA-approved; limited completed human clinical data
FDA status: Not approved for any indication

Overview

At a Glance

Ipamorelin is a selective growth hormone secretagogue that mimics ghrelin to stimulate GH release from the pituitary, without significantly affecting cortisol or prolactin. It's popular in anti-aging and peptide therapy clinics, often combined with CJC-1295. A few clinical trials exist — notably in post-surgical recovery — but it has no FDA approval for any indication. It is sold as a research chemical, and long-term safety data in humans is lacking.

Ipamorelin is a synthetic pentapeptide — a chain of five amino acids (Aib-His-D-2-Nal-D-Phe-Lys-NH₂) — that acts as a selective growth hormone secretagogue (GHS). It stimulates the pituitary gland to release growth hormone (GH) by binding to the ghrelin receptor (GHS-R1a), mimicking the action of the endogenous hunger hormone ghrelin. Ipamorelin was originally developed by Novo Nordisk in the 1990s as part of a research program to identify compounds that could stimulate GH release with fewer side effects than earlier growth hormone-releasing peptides (Raun et al., 1998).

What distinguishes ipamorelin from earlier growth hormone secretagogues — such as GHRP-2 and GHRP-6 — is its selectivity. While those peptides stimulate GH release effectively, they also significantly elevate cortisol, prolactin, and aldosterone levels. Ipamorelin produces a dose-dependent increase in GH with minimal to no effect on these other hormones at therapeutic doses (Raun et al., 1998). This selectivity profile has made it one of the most widely used growth hormone secretagogues in clinical and anti-aging medicine settings.

Ipamorelin reached Phase 2 clinical trials for post-operative ileus (delayed gut motility after abdominal surgery), conducted by Helsinn Therapeutics. While the compound demonstrated biological activity and GH-releasing properties in humans, the Phase 2b trial did not meet its primary endpoint for ileus, and development for that indication was discontinued (Beck et al., 2008). No further FDA-track clinical development has been pursued.

Despite the lack of FDA approval, ipamorelin has become one of the most commonly prescribed peptides through compounding pharmacies and anti-aging/regenerative medicine clinics. It is frequently used alone or in combination with CJC-1295 (a growth hormone-releasing hormone analog) to amplify GH output. Ipamorelin has no FDA-approved indication for any use.

Quick Facts

PropertyDetails
Molecular formulaC₃₈H₄₉N₉O₅
Amino acid sequenceAib-His-D-2-Nal-D-Phe-Lys-NH₂
Molecular weight~711.9 Da
Receptor targetGrowth hormone secretagogue receptor (GHS-R1a / ghrelin receptor)
Routes studiedSubcutaneous injection, intravenous
Human trialsPhase 2 for post-operative ileus (completed; did not advance)
FDA approvalNone
WADA statusProhibited (S2 — peptide hormones, growth factors)

This content is for informational purposes only and does not constitute medical advice. Always consult your healthcare provider.

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