Tesamorelin is a synthetic 44-amino-acid growth hormone-releasing factor (GHRF) analogue — a trans-3-hexenoyl-modified form of human GHRH(1-44) with extended pharmacokinetic stability. Studied in HIV-associated lipodystrophy clinical trials with reductions in visceral adipose tissue as the dominant published outcome.
Definition
Tesamorelin (TH9507) is a synthetic analogue of human growth hormone-releasing factor (also called growth hormone-releasing hormone, GHRH). The compound consists of the full 44-amino-acid GHRH sequence with an N-terminal trans-3-hexenoyl modification that confers resistance to dipeptidyl peptidase IV (DPP-IV) cleavage, the major route by which native GHRH is degraded in vivo. The N-terminal modification extends the plasma half-life sufficiently to support daily subcutaneous dosing while preserving the agonist activity of GHRH at the pituitary GHRH receptor on somatotroph cells.
Tesamorelin acts upstream of the growth hormone receptor: it stimulates endogenous GH release from the pituitary, which then signals through GH receptor on peripheral tissues to produce the downstream metabolic effects observed in clinical research. The compound is FDA-approved for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy, and is currently the only synthetic GHRH analogue with this approved clinical indication in the United States.
How tesamorelin is studied in peptide research
The clinical literature on tesamorelin centres on HIV-associated lipodystrophy, a body-composition complication of long-term antiretroviral therapy characterised by visceral adipose accumulation with associated metabolic risk. The pivotal Falutz trial published in the New England Journal of Medicine documented significant reductions in visceral adipose tissue with tesamorelin treatment in HIV-infected patients (PMID 18057338). Long-term safety and continued-efficacy extension data was published in subsequent Falutz reports (PMID 18690162, PMID 20101189). The pooled phase 3 analysis consolidated efficacy and safety findings across two multicentre placebo-controlled trials with safety-extension follow-up (PMID 20554713).
Secondary analyses extended the findings to inflammatory-marker improvements (PMID 21516030), metabolic-profile improvements in visceral-adiposity reducers (PMID 22495074), and liver-enzyme improvements correlating with visceral fat reduction (PMID 28832410). The drug-evaluation reviews provide overall integration of the clinical-development story (PMID 17086939, PMID 19243281, PMID 22298602).
Tesamorelin is supplied as research-grade lyophilised peptide for laboratory research applications. The clinical-trial framework summarised above is from FDA-approved indications and is not a research-supply use recommendation.
Related terms
- Growth hormone receptor
- Ipamorelin
- GHRH / growth hormone-releasing hormone
- GHRF / growth hormone-releasing factor
- CJC-1295 (long-acting GHRH analogue)
- Dipeptidyl peptidase IV (DPP-IV)
- Somatotroph
Where tesamorelin appears in the Ronin catalog
- Tesamorelin 10mg — single-compound vial, lyophilized white powder under inert gas
References
- Tomlinson B. Drug evaluation: tesamorelin, a synthetic human growth hormone releasing factor. Curr Opin Investig Drugs 2006;7(10):952-961. [PMID 17086939]
- Falutz J et al. Metabolic effects of a growth hormone-releasing factor in patients with HIV. N Engl J Med 2007;357(23):2359-2370. [PMID 18057338]
- Falutz J et al. Long-term safety and effects of tesamorelin, a growth hormone-releasing factor analogue, in HIV patients with abdominal fat accumulation. AIDS 2008;22(14):1719-1728. [PMID 18690162]
- Falutz J et al. Effects of tesamorelin (TH9507), a growth hormone-releasing factor analog, in HIV-infected patients with excess abdominal fat: a pooled analysis of two multicenter, double-blind placebo-controlled phase 3 trials with safety extension data. J Clin Endocrinol Metab 2010;95(9):4291-4304. [PMID 20554713]
- Stanley TL et al. Effects of tesamorelin on inflammatory markers in HIV patients with excess abdominal fat: relationship with visceral adipose reduction. AIDS 2011;25(10):1281-1288. [PMID 21516030]
- Spooner LM, Olin JL. Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. Ann Pharmacother 2012;46(2):240-247. [PMID 22298602]
Glossary entries describe research-context use of peptide-research terminology. They do not constitute medical, veterinary, or clinical advice. Tesamorelin is sold strictly as a research-grade reagent for laboratory and bench research applications.