Examorelin
Evidence Grade C — Moderate human evidence. 288 published studies, 168 human. 0 registered clinical trials.
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.
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.
No trials registered on ClinicalTrials.gov for this compound.
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.
Somatropin has been available since the mid-1980s and is one of the most established peptide therapies. It is sold under numerous brand names including Genotropin, Humatrope, Norditropin, and Omnitrope (the first biosimilar approved in the US, 2006). Approved indications include childhood and adult growth hormone deficiency, Turner syndrome, children born small for gestational age, Prader-Willi syndrome, idiopathic short stature, and short stature from chronic kidney disease. Daily injection has been the main burden of somatropin therapy, particularly for paediatric patients who may require years of treatment. This has driven the development of once-weekly alternatives (somatrogon and somapacitan), which are gradually changing the treatment landscape. Annual treatment costs remain substantial, and concerns about misuse in anti-ageing and performance enhancement contexts are ongoing.
Tesamorelin is marketed as Egrifta SV (approved November 2010) for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. In clinical trials, it reduced visceral fat by approximately 15% compared to a 5% increase with placebo, and this reduction was sustained with continued treatment. Tesamorelin occupies a unique niche — it is the only approved GHRH analogue and the only medication specifically approved for HIV-associated lipodystrophy. Beyond its approved indication, it has attracted research interest for potential effects on liver fat, cognitive function, and peripheral neuropathy. Fat reduction reverses when treatment stops, and it is not approved for general weight loss or body composition purposes.
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.
