Peptides›GH secretagogue›Hexarelin

Hexarelin

/ Synthetic hexapeptide; potent ghrelin/GHS-R1a agonist; also CD36 ligand

TIER 3 · PreclinicalN = 0 · TESTING PENDINGLAST REVIEW 2026·04·20

ALIAS · HEX · Examorelin

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Research use onlyAny dose figures below describe what specific cited studies used, reported factually. Nothing on this page is guidance for human use.READ FIRST →

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§ A · Identity

Primary sequence— sequence not captured —

MW · —CLASS · Synthetic hexapeptide; potent ghrelin/GHS-R1a agonist; also CD36 ligandCATEGORY · GH secretagogue

Studied in small human trials for cardiac and GH-deficiency research. Not FDA-approved. Cardiac-tissue effects distinguish it from pure ghrelin mimetics.

§ B · Mechanism of action

Hexarelin is a synthetic hexapeptide GH-secretagogue with high affinity at GHS-R1a. It also binds the scavenger receptor CD36, which may contribute to cardioprotective effects reported in rodent cardiac-ischemia models.

§ C · Human clinical evidence

Small human trials in GH-deficient children and adults exist. No pivotal Phase 3 program. Proposed cardiac applications have not advanced to approval.

§ D · Primary literature

PubMed6426923Bowers CY et al. — On the in vitro and in vivo activity of a new synthetic hexapeptide that acts on the pituitary to specifically release growth hormone · Endocrinology · other-animalOriginal characterization of growth hormone-releasing peptides (GHRPs) including the hexapeptide lineage. Foundation for GHRP-2, GHRP-6, hexarelin, and subsequent ghrelin-mimetic development.Limitations: Preclinical; predates identification of ghrelin (1999) as the endogenous ligand for these receptor agonists.1984

§ F · Safety signal

Tachyphylaxis (decreased response with repeated dosing) has been reported. Cortisol and prolactin elevation. No long-term human safety data at chronic recreational doses.

§ H · Regulatory status

Regulatory status

FDA status:: Not FDA-approved

§ I · Notable gaps and controversies

CD36 binding differentiates hexarelin from purely GHS-R1a-selective agents but has not translated to any approved clinical indication. Tachyphylaxis is a recurring concern with chronic hexarelin administration.