Evidence Grade C — Moderate human evidence. 288 published studies, 168 human. 0 registered clinical trials.
Medically reviewed by a licensed medical professional
Hexarelin (examorelin) is a synthetic growth hormone secretagogue developed in Italy. Beyond its growth hormone effects, research has investigated potential heart-protective properties through a separate receptor (CD36). However, a fundamental problem emerged: the growth hormone response fades within weeks of repeated use (tachyphylaxis), which halted clinical development. It has no regulatory approval.
Hexarelin is also known by these brand and alternate names:
288 published studies: 168 human, 106 animal, 47 in-vitro, 22 reviews
Hexarelin has no marketing authorisation. A small Phase II study in growth hormone-deficient adults (12 patients) reported changes in cardiac function over 16 weeks. Significant growth hormone tachyphylaxis (loss of response) was observed within 4–16 weeks of repeated dosing, which limited clinical development.
No Phase III trials have been conducted. The growth hormone tachyphylaxis observed with hexarelin is a fundamental pharmacological limitation that distinguishes it from approved growth hormone therapies. Products available through unregulated channels lack pharmaceutical quality assurance.
Research suggests hexarelin activates both the ghrelin receptor (for growth hormone release) and the CD36 receptor on heart muscle cells and immune cells. The CD36 interaction has been investigated in preclinical cardiac studies. Like GHRP-2 and GHRP-6, it also stimulates cortisol and prolactin. A significant limitation observed in research is rapid loss of growth hormone response (tachyphylaxis) within weeks of repeated administration.
Research suggests a small Phase II study (12 patients) reported changes in cardiac function over 16 weeks, but the significant growth hormone tachyphylaxis observed — loss of response within 4-16 weeks of repeated dosing — is a fundamental limitation that distinguishes hexarelin from approved growth hormone therapies. The CD36 receptor interaction for heart protection is scientifically interesting but has not advanced beyond preclinical investigation. Like GHRP-2, hexarelin also stimulates cortisol and prolactin. It is prohibited by WADA. Products from unregulated channels lack pharmaceutical quality assurance.
PeptideTrace tracks 0 registered clinical trials for Hexarelin sourced from ClinicalTrials.gov.
No trials registered on ClinicalTrials.gov for this compound.
Hexarelin (examorelin) is a synthetic hexapeptide (His-D-2-MeTrp-Ala-Trp-D-Phe-Lys-NH2), MW ~887.04 Da. GHRP-6 with 2-methyl on D-Trp increasing potency ~2-fold. Most potent hexapeptide GH secretagogue. Unique direct cardioprotective effects independent of GH via CD36 binding. Developed by Europeptides/Aeterna Zentaris. Not approved. Half-life ~55-70 min. WADA-prohibited.
Research suggests GHS-R1a activation for GH release plus unique CD36 binding (Kd ~200 nM) on cardiomyocytes/macrophages. CD36 activates PPARgamma, reduces cardiac fibrosis, protects against ischemia-reperfusion. Also stimulates ACTH/cortisol/prolactin. Dual GHS-R1a/CD36 activity is unique among secretagogues.
No marketing authorization. Phase II cardiac (Bisi, JCEM 1999; N=12 GHD adults): hexarelin 400 mcg SC BID x16 weeks, LVEF 39.8% to 44.5% (P<0.05). In healthy volunteers: 1 mcg/kg IV peak GH ~60-120 ng/mL. Significant GH tachyphylaxis by 4-16 weeks limited development. No Phase III.
The information on this page is provided for educational and research reference purposes only. This is not medical advice. Always consult a qualified healthcare professional before making any health-related decisions.
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Somatrogon is marketed as Ngenla (approved June 2023) for paediatric growth hormone deficiency in children aged 3 years and older. In the pivotal trial, once-weekly somatrogon produced growth rates equivalent to daily somatropin injections (10.1 cm/year versus 9.8 cm/year), confirming that reducing injection frequency does not compromise growth outcomes. Ngenla represents a meaningful advance for paediatric patients and their families, reducing injections from 365 to 52 per year. Treatment adherence has been a persistent challenge with daily growth hormone, and weekly dosing is expected to improve long-term outcomes through better compliance. Somatrogon competes directly with somapacitan (Sogroya), the other approved weekly growth hormone, creating a new generation of less burdensome treatment options.
Somapacitan is marketed as Sogroya (approved August 2020 for adult growth hormone deficiency; expanded April 2023 to paediatric growth hormone deficiency in children aged 2.5 years and older). It is the first once-weekly growth hormone approved for both adult and paediatric patients. In adults, clinical trials showed improvements in body composition including reduced truncal fat. In children, growth rates were comparable to daily somatropin. The albumin-binding approach provides predictable drug levels with lower peak-to-trough variation than some other long-acting growth hormone technologies. Sogroya competes with somatrogon (Ngenla) in the growing once-weekly growth hormone market, with both products expected to gradually replace daily injections as the standard of care.
ACE-031 has no marketing authorisation. A Phase I trial in healthy women showed increased lean mass and decreased fat mass. A Phase II trial in DMD (24 patients) showed lean body mass increases but was discontinued due to bleeding-related safety concerns (epistaxis, telangiectasias, and gum bleeding), likely caused by inhibition of BMP-9/10 vascular signalling. ACE-031 is a large fusion protein (~90 kDa), not a peptide. Its clinical development was halted. The non-selective ligand-trapping profile — capturing beneficial vascular signalling molecules alongside the intended muscle-growth targets — illustrates the challenge of targeting the TGF-beta superfamily. Acceleron subsequently developed more selective agents.
This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before making decisions about your health.
