Hexarelin 6mg: Experimental Growth Hormone Secretagogue
Hexarelin is a synthetic growth hormone-releasing peptide (GHRP) that stimulates growth hormone (GH) release through specific receptors in the pituitary and hypothalamus, but it is NOT FDA-approved for any clinical indication and should not be used in routine medical practice. 1, 2
Pharmacological Profile
Mechanism of Action:
- Hexarelin binds to and activates the growth hormone secretagogue receptor (GHSR) in both the brain and peripheral tissues, including the heart and blood vessels 3
- It also binds to the non-GHSR receptor CD36 in cardiac tissue, which mediates potential cardioprotective effects 3
- The compound is chemically more stable than natural ghrelin and functionally more potent as a GH secretagogue 3
Hormonal Effects Beyond GH:
- Hexarelin stimulates prolactin (PRL) release at levels similar across all age groups (approximately 500-600 μg*min/L) 1
- It possesses significant ACTH and cortisol-releasing activity comparable to corticotropin-releasing hormone (CRH), with ACTH responses ranging from 1,200-2,250 pg*min/mL depending on age 1, 4
- The ACTH-releasing effect appears independent of both CRH and vasopressin pathways, as hexarelin shows no synergistic interaction with these neurohormones 4
Age-Dependent GH Response Patterns
The GH response to hexarelin varies dramatically with age:
- Prepubertal children: moderate response (approximately 770 μg*min/L) 1
- Pubertal adolescents: peak response (approximately 1,960 μg*min/L, 2.5-fold higher than prepubertal) 1
- Young adults: sustained high response (approximately 1,830 μg*min/L, similar to pubertal) 1
- Elderly adults: reduced response (approximately 950 μg*min/L, returning to prepubertal levels) 1
Dosing Information from Research Studies
Experimental doses studied in humans:
- The maximal effective dose studied was 2.0 μg/kg intravenously, which translates to approximately 140 μg for a 70 kg adult 1, 4
- A 6mg dose would represent approximately 85 μg/kg for a 70 kg person—over 40 times the studied maximal effective dose 1
- In animal studies, subcutaneous administration produced longer-lasting GH release than intravenous administration 2
Repeated dosing effects:
- A second bolus of hexarelin administered 60-120 minutes after the first produces significant additional GH secretion, but with reduced peak secretion rates when given at 120 minutes (P=0.03) 5
- The synergistic effect observed when hexarelin is combined with GHRH is lost upon repeated administration 5
Critical Safety and Regulatory Considerations
This compound lacks FDA approval and clinical safety data:
- No evidence exists in the provided literature regarding the safety, efficacy, or appropriate use of a 6mg dose in humans
- The cardiovascular effects through CD36 receptors are incompletely characterized and may pose unknown risks 3
- The simultaneous stimulation of ACTH/cortisol could lead to hypercortisolism with chronic use 1, 4
Common pitfall: Hexarelin is sometimes marketed through non-medical channels as a "research peptide" or performance-enhancing substance. Clinicians should not prescribe this compound, as it has no established therapeutic indication, no FDA approval, and no safety data at the 6mg dose level.
If a patient presents requesting or using hexarelin, counsel them that this represents use of an unapproved experimental compound with unknown risks, and redirect them toward evidence-based, FDA-approved treatments for their underlying condition (whether growth hormone deficiency, aging-related concerns, or athletic performance enhancement).