Tesamorelin is a synthetic analog of human growth hormone-releasing hormone, GHRH(1-44), carrying a trans-3-hexenoyl group on its N-terminus that researchers added to slow enzymatic degradation while preserving binding at the GHRH receptor.1 Among the GH-axis peptides it is unusual in having a substantial clinical evidence base: multiple randomized, double-blind, placebo-controlled trials have studied it, and it is an approved prescription drug (marketed as Egrifta) for HIV-associated lipodystrophy.13 The most consistently reported finding is a selective reduction in visceral adipose tissue.12 Material sold here is supplied strictly for in-vitro and laboratory research use and is not the approved pharmaceutical product; the data below describe what published studies reported, not directions for use.
Sequence & identity
Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH2 (N-terminal trans-3-hexenoyl) · C221H366N72O67S · 5135.86 g/mol
Structure and identity per PubChem CID 16137828 (InChIKey QBEPNUQJQWDYKU-BMGKTWPMSA-N).5
Mechanisms studied
Researchers describe tesamorelin as a GHRH-receptor agonist: it binds pituitary GHRH receptors and stimulates the synthesis and pulsatile release of endogenous growth hormone, which in turn raises circulating insulin-like growth factor 1 (IGF-1).14 Because it acts upstream on the hypothalamic-pituitary axis rather than supplying exogenous GH, investigators reported that GH secretion remained pulsatile and subject to negative feedback in healthy men.4 The N-terminal trans-3-hexenoyl modification was reported to confer resistance to degradation by dipeptidyl peptidase and other proteases relative to native GHRH.1 The reduction in visceral fat observed in trials is attributed to the lipolytic actions of the restored GH/IGF-1 axis.2
Dosing in the research literature
The figures below summarise regimens as reported in published research — they are not recommendations or directions for use.
| Source / model | Regimen reported | Notes |
|---|---|---|
| Falutz et al., N Engl J Med 2007 (phase III, HIV-associated lipodystrophy)1 | 2 mg administered subcutaneously once daily over a 26-week double-blind phase | Study-reported regimen, not a usage direction. Investigators reported a selective reduction in visceral adipose tissue (approximately 15% relative to placebo) with concurrent improvements in triglycerides and no significant deterioration in glucose tolerance over the primary phase. |
| Stanley et al., JAMA 2014 (liver fat in HIV)2 | 2 mg subcutaneously once daily for 6 months | Same study-reported dose. Net treatment effect on hepatic fat fraction was -2.9% lipid-to-water (P=0.003) and visceral fat -42 cm2 (P=0.005); fasting glucose rose transiently at 2 weeks (treatment effect 7 mg/dL, P=0.03) but the between-group difference was no longer significant by 6 months (P=0.56). |
| Stanley et al., J Clin Endocrinol Metab 2011 (healthy men, PK/PD)4 | Single and 2 mg-range subcutaneous doses used to characterize GH pulsatility | Pharmacology study, not a dosing recommendation. Reported a short plasma elimination half-life on the order of tens of minutes after subcutaneous administration. |
Effects observed in research
In HIV-infected adults with excess abdominal fat, randomized placebo-controlled trials reported that tesamorelin selectively reduced visceral adipose tissue (on the order of 15-18%) while sparing subcutaneous fat, and lowered triglycerides; investigators observed that these changes largely reversed when treatment was stopped.1 A separate randomized trial reported a reduction in hepatic fat fraction, with a net treatment effect of about -2.9% lipid-to-water (P=0.003).2 Across studies, IGF-1 rose as expected, and the most frequently reported adverse events were injection-site reactions and arthralgia; transient increases in fasting glucose were observed early but the between-group difference was generally reported to resolve over the treatment period.23 All of these are observations from the HIV-lipodystrophy population studied; effects in other contexts are not established. No statement here implies a benefit to any individual.
Strength of evidence
Grade A for the specific indication studied. Tesamorelin is supported by multiple randomized, double-blind, placebo-controlled phase III trials in HIV-associated lipodystrophy12 and is an FDA-approved drug (Egrifta), approved November 2010, for that narrow population.3 Evidence outside HIV-associated visceral adiposity (for example general body composition, cognition, or fatty liver disease in HIV-negative people) is far more limited and should be regarded as exploratory.2 The published safety database is largely confined to the studied population, and long-term outcomes in other groups are not established. Material offered here is for laboratory research use only and is not the approved medicine.
Reconstitution & storage
Reconstitute with bacteriostatic water for laboratory handling. Store lyophilised material frozen and reconstituted material refrigerated. Use Peptigo’s reconstitution calculator and storage cheat sheet for working figures.
References
- Falutz J, Allas S, Blot K, et al. Metabolic effects of a growth hormone-releasing factor in patients with HIV. N Engl J Med. 2007;357(23):2359-2370. doi:10.1056/NEJMoa072375. https://www.nejm.org/doi/full/10.1056/NEJMoa072375
- Stanley TL, Feldpausch MN, Oh J, et al. Effect of tesamorelin on visceral fat and liver fat in HIV-infected patients with abdominal fat accumulation: a randomized clinical trial. JAMA. 2014;312(4):380-389. doi:10.1001/jama.2014.8334. https://pmc.ncbi.nlm.nih.gov/articles/PMC4363137/
- U.S. Food and Drug Administration. EGRIFTA (tesamorelin for injection) prescribing information; original approval November 10, 2010. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022505s012s013lbl.pdf
- Stanley TL, Chen CY, Branch KL, Makimura H, Grinspoon SK. Effects of a growth hormone-releasing hormone analog on endogenous GH pulsatility and insulin sensitivity in healthy men. J Clin Endocrinol Metab. 2011;96(1):150-158. doi:10.1210/jc.2010-1587. https://pmc.ncbi.nlm.nih.gov/articles/PMC3038486/
- National Center for Biotechnology Information. PubChem Compound Summary for CID 16137828, Tesamorelin. https://pubchem.ncbi.nlm.nih.gov/compound/16137828