Ipamorelin

Classification

Selective ghrelin / GHS-R1a agonist (research only)

Approval status

Research only · Not approved for human use

Research status

Investigational growth-hormone secretagogue. Not an approved chronic GH-axis medicine.

Molecular formula

Insufficient reliable evidence identified.

Molecular weight

Insufficient reliable evidence identified.

Sequence

Aib-His-D-2-Nal-D-Phe-Lys-NH2 (pentapeptide ghrelin-mimetic secretagogue)

Primary biological target

Ghrelin receptor (GHSR-1a) — proposed selective GH secretagogue

Half-life

Short (minutes to a few hours range in limited PK reports); insufficient standardised human PI data

Routes investigated

Intravenous (clinical pharmacology), Subcutaneous (research use reports)

Human evidence level

C — Limited or early human evidence

A research-only ghrelin-mimetic peptide formerly explored in medicine development. Not approved for anti-ageing or bodybuilding.

Synthetic pentapeptide developed as a ghrelin-receptor agonist with relative GH selectivity in early pharmacology.

Proposed mechanism

Proposed mechanism: ipamorelin stimulates the ghrelin receptor on pituitary somatotrophs, increasing GH release with less ACTH/cortisol and prolactin stimulation than some older GHRPs in experimental comparisons. Mechanism not yet fully established as a labelled therapy. Human programmes did not produce a registered product for anti-ageing or bodybuilding use.

GH pulse amplification in experimental settings — not an approved therapy.

• Growth-hormone secretion

  C · Limited or early human evidence

  Early human research has examined GH release after parenteral ipamorelin in clinical pharmacology settings.^[1]

Investigational findings are not proven clinical benefits unless an authority has labelled that indication.

Overall human evidence grade: C · Limited or early human evidence

Animal, cell and in-vitro findings are listed separately from human effects.

Well described as a GHS agonist in animals.

This section does not provide personalised medical dosing. Values are those reported in papers or protocols. Animal mg/kg doses are not converted to human doses.

Doses reported in human studies

1. Early ipamorelin GH-release pharmacology

   Dose: µg/kg range (paper-specific) µg/kg

   Route: Intravenous in foundational papers

   Frequency: Single or short repeated doses in experiments

   Duration: Acute

   Population: Human volunteers / limited clinical pharmacology

   Purpose: Characterise GH secretagogue activity

   ^[1]

Preclinical / animal study dosing

Insufficient reliable evidence identified.

Reliable population PK comparable to a registered weekly incretin was not identified.

Flushing, glucose or GH-axis effects are theoretically possible; a labelled AE table does not exist.

Unknowns. Grey-market vials are not pharmaceutical-grade evidence.

Contraindications. Not for human use.

Australia — TGA

Not approved as a GH secretagogue medicine.

United States — FDA

Not approved.

European Union — EMA

Not approved.

1. [1] Ipamorelin, the first selective growth hormone secretagogue

   Raun K et al. Ipamorelin, the first selective growth hormone secretagogue Eur J Endocrinol. 1998. PMID 9849822

   PMID 9849822