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Ipamorelin

Grade C: Preliminary or limited human evidence

TL;DR: Ipamorelin is a synthetic pentapeptide growth hormone secretagogue that stimulates GH release by acting as a selective ghrelin receptor agonist. Only small human studies have been completed, including a pharmacokinetic characterization in healthy volunteers and at least one efficacy trial that did not demonstrate a positive therapeutic outcome. No positive human RCT supporting a clinical indication has been published. Animal studies confirm GH release, longitudinal bone growth effects, and glucocorticoid-attenuating properties, but these findings have not translated into demonstrated human benefit. The evidence base is insufficient to establish efficacy for any therapeutic use in humans.

Key Takeaways

  • Grade C: Preliminary or limited human evidence
  • Not FDA approved: Not FDA-approved for any indication; banned from both 503A and 503B compounding as of April 2026.
  • Compounding: The FDA placed Ipamorelin in Category 2 of its interim 503A/503B bulk-substances policy, the list of substances it has identified as presenting potential significant safety risks, so it is not eligible for routine pharmacy compounding.
Ipamorelin chemical structure
Structure via PubChem CID 9831659

Mechanism

Ipamorelin binds selectively to the growth hormone secretagogue receptor (GHSR-1a), stimulating pulsatile GH release from the pituitary without substantially affecting cortisol or prolactin at tested doses.

Evidence

Ipamorelin is a synthetic pentapeptide growth hormone secretagogue that stimulates GH release by acting as a selective ghrelin receptor agonist. Only small human studies have been completed, including a pharmacokinetic characterization in healthy volunteers and at least one efficacy trial that did not demonstrate a positive therapeutic outcome. No positive human RCT supporting a clinical indication has been published. Animal studies confirm GH release, longitudinal bone growth effects, and glucocorticoid-attenuating properties, but these findings have not translated into demonstrated human benefit. The evidence base is insufficient to establish efficacy for any therapeutic use in humans.

Safety and risks

Human safety data for ipamorelin is limited; the available studies were not designed primarily to characterize safety. GH secretagogues as a class elevate insulin-like growth factor 1 (IGF-1), and sustained IGF-1 elevation carries theoretical risks including promotion of tissue growth in unintended compartments. Injection site reactions are expected with subcutaneous use. Long-term safety in humans has not been studied. Following the 2024 PCAC vote against 503A inclusion, ipamorelin is not eligible for routine pharmacy compounding, so clinics offering it as a subscription product are operating outside current federal compounding policy. The compound should be considered to have limited human safety data.

Interactions

Concurrent use with other GH-axis modulators (GHRH analogs, other secretagogues, exogenous GH) is expected to produce additive IGF-1 elevation; interaction data in humans is absent.

Federal compounding status

503A/503B Category 2: significant safety risk as of 2023.

The FDA placed this substance (503B) in Category 2 of its interim bulk-substances policy, the list it has identified as presenting potential significant safety risks, so it is not eligible for routine pharmacy compounding. FDA source

Federal status only, from public FDA records. State pharmacy-board rules vary and are not covered here. This is regulatory reporting, not legal advice. All compounds.

Compounding legality

The FDA placed Ipamorelin in Category 2 of its interim 503A/503B bulk-substances policy, the list of substances it has identified as presenting potential significant safety risks, so it is not eligible for routine pharmacy compounding.

Sources

  1. The growth hormone secretagogue receptor 1a agonists, anamorelin and ipamorelin, inhibit cisplatin-induced weight loss in ferrets: Anamorelin also exhibits anti-emetic effects via a central mechanism. (2024) other
  2. Ipamorelin, the first selective growth hormone secretagogue. (1998) other
  3. Ipamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats. (1999) other
  4. Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers. (1999) rct
  5. Pharmacokinetic evaluation of ipamorelin and other peptidyl growth hormone secretagogues with emphasis on nasal absorption. (1998) other
  6. Highly potent growth hormone secretagogues: hybrids of NN703 and ipamorelin. (2001) other
  7. Influence of chronic treatment with the growth hormone secretagogue Ipamorelin, in young female rats: somatotroph response in vitro. (2002) other
  8. The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats. (2001) other
  9. Determination of growth hormone releasing peptides metabolites in human urine after nasal administration of GHRP-1, GHRP-2, GHRP-6, Hexarelin, and Ipamorelin. (2015) other
  10. A new series of highly potent growth hormone-releasing peptides derived from ipamorelin. (1998) other
  11. Efficacy of ipamorelin, a novel ghrelin mimetic, in a rodent model of postoperative ileus. (2009) other
  12. The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats. (2000) other
  13. Mechanism of ipamorelin-evoked insulin release from the pancreas of normal and diabetic rats. (2004) other

Ipamorelin is Not FDA approved. PeptideGrids presents evidence and regulatory status for informational purposes only. We do not sell, supply, source, or help anyone obtain this compound, and we provide no dosing or administration guidance. This is not medical advice; consult a licensed clinician. Full disclaimer.

Last reviewed June 1, 2026 by PeptideGrids editorial team (independently audited).