Tesamorelin
Stabilized growth hormone-releasing hormone analog approved for HIV lipodystrophy.
Also known as: Egrifta, TH9507
Tesamorelin is a modified version of growth hormone-releasing hormone (GHRH) designed for improved stability in circulation. It is approved by the FDA as Egrifta for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy, making it one of the few approved GHRH-based therapeutics.
Key facts
- Class
- Growth hormone-releasing hormone (GHRH) analog
- Originator
- Theratechnologies
- Regulatory status
- FDA approved as Egrifta (2010) for HIV-associated lipodystrophy
- Structure
- 44 amino acid peptide (based on human GHRH 1-44) with trans-3-hexenoic acid modification
- Administration
- Daily subcutaneous injection in approved use
What is tesamorelin?
Tesamorelin is a synthetic analog of the first 44 amino acids of human growth hormone-releasing hormone. A trans-3-hexenoic acid group attached to the N-terminus protects the peptide from degradation by dipeptidyl peptidase-4 (DPP-4), the same enzyme that degrades native GLP-1.
The compound was developed by the Canadian biotech Theratechnologies and received FDA approval in November 2010 as Egrifta for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy, a specific clinical population with abnormal fat redistribution.
Mechanism of action
Tesamorelin binds the GHRH receptor on pituitary somatotrophs and stimulates release of growth hormone, which in turn stimulates hepatic production of insulin-like growth factor 1 (IGF-1). Because the stimulation acts through the normal GHRH pathway, growth hormone release remains pulsatile and subject to physiologic feedback from IGF-1 and somatostatin.
- •Binds the pituitary GHRH receptor, stimulating release of endogenous growth hormone
- •Growth hormone in turn stimulates hepatic IGF-1 production
- •Release pattern remains pulsatile and subject to negative feedback
- •Modification at the N-terminus protects the peptide from DPP-4 degradation
Clinical trial history
Tesamorelin was studied in two large phase 3 trials in HIV-infected adults with excess abdominal fat. Results were published in NEJM in 2007 and AIDS in 2010. The trials reported significant reductions in visceral adipose tissue on CT imaging after 26 weeks of daily subcutaneous administration compared with placebo.
Additional research has examined tesamorelin in other contexts, including nonalcoholic fatty liver disease and mild cognitive impairment. These studies are smaller and do not carry the same regulatory approval as the HIV lipodystrophy indication.
Safety and regulatory context
The Egrifta prescribing information lists injection site reactions, arthralgia, peripheral edema, and glucose intolerance as commonly reported adverse events. The label notes that growth hormone axis activation may affect glucose metabolism and advises monitoring in patients with diabetes or prediabetes.
Tesamorelin is a prescription medication in the United States with a specific approved indication. Material sold as research tesamorelin outside of this indication is intended for laboratory use only and is not cleared for off-label human administration.
Research sourcing
Tesamorelin is listed by our research partner, GLP1 Research Lab, which supplies lyophilized peptides for laboratory use. Listings include product identifiers relevant to research documentation.
View Tesamorelin listing at GLP1 Research LabAffiliate partnership. Metabolic Playbook may earn a commission on purchases made through this link at no additional cost to the researcher.