Hexarelin
unknown riskAlso: Examorelin · EP-23905
Hexarelin is a synthetic GHRP-6 analog with potent GH-releasing activity. It also has direct cardiac effects independent of GH — including cardioprotection and cardiac remodeling — through CD36 receptor activation.
Reported Benefits
GH Release
Potent GH secretagogue with dose-dependent response in human studies.
Cardioprotection
Animal and limited human data show cardioprotective effects via CD36 mechanism.
Angiogenesis
Promotes coronary angiogenesis in animal models independent of GH.
Mechanism of Action
Hexarelin activates both the ghrelin/GHSR receptor (triggering GH release) and the scavenger receptor CD36. CD36 activation in cardiac tissue mediates direct cardioprotective effects including reduced cardiac cell apoptosis, improved cardiac remodeling after ischemia, and coronary angiogenesis.
Key Clinical Studies
Loche S et al. (1995)
pharmacodynamic · 24 children with GH deficiency
Potent GH release comparable to GHRH
Locatelli V et al. (2010)
review · Review
Cardiovascular effects of hexarelin independent of GH
Overview
Hexarelin is distinguished from other GHRPs by its additional direct cardiac mechanism through CD36 receptor activation — making it potentially useful in cardiac rehabilitation contexts beyond pure GH secretagogue applications.
Cardiac Mechanism
The CD36 receptor pathway is separate from GHSR and operates independently of GH. In animal myocardial infarction models, hexarelin reduces infarct size, improves contractility, and promotes coronary angiogenesis. This mechanism has attracted interest from cardiovascular researchers, though human cardiac trial data remains limited.
Desensitization Profile
Unlike ipamorelin (which shows minimal desensitization), hexarelin’s GHSR agonism is associated with receptor desensitization with daily use. Cycling protocols (5 days on, 2 days off, or intermittent schedules) are commonly used to mitigate this effect.
Research Status
Hexarelin has completed Phase 2 trials for GH deficiency and cardiac applications but has not advanced to Phase 3. This leaves it in a research-only classification despite reasonable human data.
Regulatory Status
Research OnlyNot FDA-approved; Phase 2 trials conducted but no regulatory approval
Safety Profile
Side Effects
- •Water retention
- •Cortisol elevation (more than ipamorelin)
- •Prolactin increase
- •Desensitization with daily dosing
Contraindications
- •Active malignancy
- •Pregnancy
- •Congestive heart failure (paradoxically, due to uncertain cardiac effects)
Drug Interactions
- •Glucocorticoids
- •Somatostatin analogs
Primary Uses
Related Peptides
Weekly Briefing
Regulatory updates + new study breakdowns.
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