Tesamorelin

Tesamorelin is a 44-amino acid synthetic analogue of endogenous growth hormone-releasing hormone (GHRH) in which the N-terminal tyrosine carries a covalently attached trans-3-hexenoic acid group. This modification shields the peptide from dipeptidyl peptidase IV (DPP-IV) cleavage, extending its functional half-life compared to native GHRH while preserving the ability to bind and activate the pituitary GHRH receptor. Tesamorelin is the first and, as of 2026, only FDA-approved pharmacological treatment for HIV-associated lipodystrophy — specifically the excess visceral abdominal fat accumulation seen in HIV-infected adults on antiretroviral therapy. It was approved in 2010 under the brand name Egrifta (NDA 022505), with subsequent formulations Egrifta SV (2019) and Egrifta WR (2025) improving convenience. The EMA did not grant European approval; a marketing application was withdrawn in 2011. Beyond its approved indication, tesamorelin has been studied in small randomized trials for HIV-associated non-alcoholic fatty liver disease (NAFLD), cognitive function in older adults and those with mild cognitive impairment, and visceral fat reduction in non-HIV obese adults with relative growth hormone deficiency. These applications remain investigational. As a growth hormone secretagogue, tesamorelin produces pulsatile GH release — considered more physiological than exogenous recombinant GH administration — and subsequently raises IGF-1. It is prohibited in competitive sport by WADA (S2 category). Outside its single FDA-approved indication, tesamorelin is available only for research use and is not validated for other human therapeutic applications.