Peptide

Hexarelin

Hexarelin

Evidence TierCWADA PROHIBITED

tuneTypical Dose

0.5-1.0 µg/kg

watchEffect Window

Minutes-hours (acute hormonal), weeks-months in selected pediatric protocols

lockCompliance

WADA PROHIBITED

Overview

Clinical Summary

Hexarelin is a potent growth hormone releasing peptide acting through ghrelin receptors. It is used to raise growth hormone and IGF-1, with interest in body composition and recovery claims.

Studies show strong stimulation of growth hormone and increases in IGF-1, which supported historical research in frailty and cardiac contexts. Controlled evidence for improved strength or fat loss in healthy users is limited. Minority effects include appetite changes, altered glucose handling, and worse deep sleep during nocturnal dosing. Safety data for long-term use outside clinical research are limited, complicating benefit assessment.

Ghrelin-receptor pathway GH secretagogue with pituitary-hypothalamic activation and measurable HPA-axis spillover.

Outcomes

What This Is Expected To Influence

Primary Outcomes

  • GH pulse amplification (acute)
  • ACTH/cortisol/prolactin axis activation

Secondary Outcomes

  • Sleep architecture changes
  • GH reserve diagnostic utility
  • Pediatric IGF-I and growth velocity context

Safety

Contraindications and Interactions

Contraindications

  • Pregnancy
  • Breastfeeding
  • Known pituitary-hypothalamic pathology without specialist oversight
  • Uncontrolled endocrine/cortisol instability

Side effects

  • Water retention
  • Cortisol increase
  • Tiredness
  • Joint stiffness

Interactions

  • Other GH secretagogues
  • GH/IGF-acting compounds
  • HPA-axis stimulators

Avoid if

  • Competitive athletes without compliance review
  • Active endocrine disorder without specialist supervision
  • Cortisol/HPA-axis sensitive medical conditions

Evidence

Study-level References

hexarelin-SRC-001Randomized, placebo-controlled clinical trial
Sourceopen_in_new

PMID: 9156035, DOI: 10.1046/j.1365-2265.1997.1240940.x

Population: Healthy male adults

Dose protocol: IV bolus 0.5-2.0 µg/kg

Key findings: Acute GH rise was dose-responsive with early peak and return toward baseline over hours.

Notes: Strongest support for acute biomarker-level pharmacodynamics.

Paper content

Acute GH rise was dose-responsive with early peak and return toward baseline over hours.

hexarelin-SRC-002Randomized controlled hormonal challenge study
Sourceopen_in_new

PMID: 8954038, DOI: 10.1210/jcem.81.12.8954038

Population: Healthy adult men

Dose protocol: IV 0.0-1.0 µg/kg. Plus GHRH 1.0 µg/kg with or without 0.125 µg/kg.

Key findings: Dose-response behavior for GH/PRL/cortisol with plateau-like GH response near 1.0 µg/kg and notable coadministration interactions.

Notes: Useful for axis signal interpretation, not long-horizon efficacy.

Paper content

Dose-response behavior for GH/PRL/cortisol with plateau-like GH response near 1.0 µg/kg and notable coadministration interactions.

hexarelin-SRC-003Controlled physiological challenge trial
Sourceopen_in_new

PMID: 9437229, DOI: 10.1530/eje.0.1370635

Population: Prepubertal children, pubertal children, adults, elderly adults

Dose protocol: IV up to 2.0 µg/kg

Key findings: GH, PRL, ACTH, and cortisol responses varied with age.

Notes: Supports phenotype-stratified interpretation.

Paper content

GH, PRL, ACTH, and cortisol responses varied with age.

hexarelin-SRC-004Randomized, double-blind clinical trial
Sourceopen_in_new

PMID: 10404825, DOI: 10.1210/jcem.84.7.5811

Population: Healthy young male volunteers

Dose protocol: IV hexarelin with CRH/desmopressin interaction paradigms

Key findings: Demonstrated GH secretagogue effects on pituitary-adrenal activation with hypothalamic AVP/CRH pathway involvement.

Notes: Mechanistic insight for safety/performance interpretation.

Paper content

Demonstrated GH secretagogue effects on pituitary-adrenal activation with hypothalamic AVP/CRH pathway involvement.

hexarelin-SRC-005Clinical safety/physiology study
Sourceopen_in_new

PMID: 10341859, DOI: 10.1046/j.1365-2265.1999.00609.x

Population: Healthy adults

Dose protocol: Acute and repeated exposure paradigms

Key findings: Confirmed recurrent ACTH/cortisol/PRL stimulation concerns during exposure with caution around prolonged use.

Notes: Supports concern for repeated endocrine perturbation in longer exposure.

Paper content

Confirmed recurrent ACTH/cortisol/PRL stimulation concerns during exposure with caution around prolonged use.

hexarelin-SRC-006Controlled repeated-stimulation study
Sourceopen_in_new

PMID: 8719303, DOI: 10.1007/BF03349794

Population: Healthy adults

Dose protocol: 1 µg/kg IV sequential stimulation over 120-minute spacing

Key findings: Second GH responses declined in repeat paradigms, with less attenuation than repeated GHRH alone.

Notes: Supports adaptive response/attenuation concerns in repeated dosing.

Paper content

Second GH responses declined in repeat paradigms, with less attenuation than repeated GHRH alone.

hexarelin-SRC-007Randomized crossover diagnostic protocol study
Sourceopen_in_new

PMID: 8977750, DOI: 10.1046/j.1365-2265.1996.00841.x

Population: Adult volunteers

Dose protocol: GHRH 1.0 µg/kg IV, hexarelin 1.0 µg/kg IV with 120-min separation

Key findings: Sequential protocol improved characterization of GH reserve with low false-negative behavior.

Notes: Diagnostic, not therapeutic outcome oriented.

Paper content

Sequential protocol improved characterization of GH reserve with low false-negative behavior.

hexarelin-SRC-008Clinical treatment-duration study
Sourceopen_in_new

Laron Z et al. 1995. "Intranasal administration of the GHRP hexarelin accelerates growth in short children." Clin Endocrinol (Oxf). 43(5):631-635. PMID: 8548949. DOI: 10.1111/j.1365-2265.1995.tb02929.x.

Population: Prepubertal short children

Dose protocol: Intranasal 60 µg/kg three times/day, up to 8 months

Key findings: IGF-I increased and growth velocity improved in this pediatric protocol.

Notes: Not directly transferable to healthy-adult enhancement use.

Paper content

IGF-I increased and growth velocity improved in this pediatric protocol.

hexarelin-SRC-009Pediatric endocrine response trial with reproducibility and sex-steroid effect assessment
Sourceopen_in_new

Loche S et al. 1997. "The growth hormone response to hexarelin in children: reproducibility and effect of sex steroids." J Clin Endocrinol Metab. 82(3):861-864. PMID: 9062497. DOI: 10.1210/jcem.82.3.3795.

Population: Short normal children

Dose protocol: IV hexarelin 2.0 µg/kg

Key findings: Reproducible GH responses with increased sensitivity after sex-steroid priming.

Notes: Supports pediatric phenotype/context dependence rather than broad adult claims.

Paper content

Reproducible GH responses with increased sensitivity after sex-steroid priming.

hexarelin-SRC-010Controlled clinical sleep-endocrine study
Sourceopen_in_new

Frieboes RM et al. 2004. "Hexarelin decreases slow-wave sleep and stimulates the secretion of GH, ACTH, cortisol and prolactin during sleep in healthy volunteers." Psychoneuroendocrinology. 29(7):851-860. PMID: 15177700. DOI: 10.1016/S0306-4530(03)00152-5.

Population: Healthy young volunteers

Dose protocol: 4 × 50 µg across one night

Key findings: Lower stage-4/slow-wave measures with concurrent endocrine increases.

Notes: Small sample. No long-horizon performance findings.

Paper content

Lower stage-4/slow-wave measures with concurrent endocrine increases.

hexarelin-SRC-011Randomized crossover physiology study
Sourceopen_in_new

Benso A et al. 2002. "Impact of two or three daily subcutaneous injections of hexarelin, a synthetic growth hormone (GH) secretagogue, on 24-h GH, prolactin, adrenocorticotropin and cortisol secretion in humans." Eur J Endocrinol. 146(3):310-316. PMID: 11888836. DOI: 10.1530/eje.0.1460310.

Population: Healthy volunteers

Dose protocol: SC hexarelin 1.5 µg/kg, 2-3 injections/day, 24-h monitoring

Key findings: 24-h GH secretion increased. Endocrine profiles changed with repeated administration and showed response adaptation.

Notes: Supports repeated-dose signal-shape behavior more than clinical outcome efficacy.

Paper content

24-h GH secretion increased; endocrine profiles changed with repeated administration and showed response adaptation.

hexarelin-SRC-012Policy/standards documentation
Sourceopen_in_new

WADA Prohibited List, S2.2.4 GH secretagogues and GH-releasing peptides; https: //www.wada-ama.org/what-is-prohibited

Population: Competitive athlete governance framework

Dose protocol: N/A

Key findings: GH-releasing factors/secretagogues are prohibited-class compounds under WADA S2.

Notes: Governance reference only. Not a clinical efficacy source.

Paper content

GH-releasing factors/secretagogues are prohibited-class compounds under WADA S2.