Tesamorelin: Scientific Profile
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Tesamorelin: a 44-amino-acid synthetic GHRH analog and GH secretagogue, approved by the FDA. With an N-terminal trans-3-hexenoyl stabilizer that confers resistance to DPP-IV. For research use only (RUO).
Tesamorelin (tesamorelin; CAS 218949-48-5) is a synthetic analog of growth hormone-releasing factor/hormone (GHRH), a 44-amino-acid peptide corresponding to human GHRH (1-44) with a trans-3-hexenoyl stabilizer at the N-terminus that confers resistance to dipeptidyl peptidase IV (DPP-IV/DPP-4) and prolongs its half-life. As a GH secretagogue, it acts as an agonist of the GHRH receptor (GHRHR) on the somatotrophs of the anterior pituitary, stimulating endogenous pulsatile secretion of growth hormone and signaling of the GH/IGF-1 axis. It has been investigated for its effect on the reduction of visceral adipose tissue. Safety note for its interpretation in research: the FDA label warns that treatment may produce glucose intolerance or diabetes mellitus, so glycemic status should be evaluated and monitored. Pivotal reference: Falutz J et al., N Engl J Med 2007;357(23):2359-70 (PMID 18057338). Reagent intended exclusively for in vitro and preclinical research (RUO).
Mechanism of action
Tesamorelin binds to the GHRH receptor in the anterior pituitary, stimulating the synthesis and secretion of GH in a pulsatile manner, similar to the natural physiological pattern.
Mechanism summary
Synthetic analog of GHRH (1-44) with a DPP-IV-resistant N-terminal trans-3-hexenoyl stabilizer. It agonizes the GHRH receptor (GHRHR) on somatotrophs of the anterior pituitary and stimulates the endogenous pulsatile secretion of GH, modulating the GH/IGF-1 axis.
Clinical Studies (7)
- Tesamorelin reduces visceral adipose tissue (Falutz J, et al. · New England Journal of Medicine · 2007) — Clinical study of tesamorelin for reduction of visceral fat. PMID 18057338.
- Efficacy and safety of tesamorelin in people with HIV on integrase inhibitors. (Russo SC, et al. · AIDS · 2024) PMID 38905488.
- Body composition, hepatic fat, metabolic, and safety outcomes of Tesamorelin, a GHRH analogue, in HIV-associated lipodystrophy: A meta-analysis of randomized controlled trials. (Badran AS, et al. · Obes Res Clin Pract · 2026) PMID 41545261.
- Population pharmacokinetic analysis of tesamorelin in HIV-infected patients and healthy subjects. (González-Sales M, et al. · Clin Pharmacokinet · 2015) PMID 25358450.
- Effects of Tesamorelin on Neurocognitive Impairment in Persons With HIV and Abdominal Obesity. (Ellis RJ, et al. · J Infect Dis · 2025) PMID 39813152.
- A placebo-controlled, dose-ranging study of a growth hormone releasing factor in HIV-infected patients with abdominal fat accumulation (Falutz, et al. · AIDS · 2005) PMID 16052083.
- Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy (Dhillon, et al. · Drugs · 2011) PMID 21668043.
Warnings
Tesamorelin is a research-use-only (RUO) compound; the following warnings and handling considerations apply to its laboratory use:
- FDA-approved for HIV lipodystrophy
- FDA label: it may produce glucose intolerance or diabetes mellitus; it requires monitoring of glycemic status
- Hypersensitivity to the compound
- Active malignancy
- Pregnancy
Technical data
- CAS
- 218949-48-5
- Molecular formula
- C221H366N72O67S
- Molecular weight
- 5135.89 Da
- Compound type
- peptide
- Storage
- -20 °C liofilizado; 2-8 °C reconstituido
- Shelf life (lyophilized)
- 24 months
- Shelf life (reconstituted)
- 30 days refrigerated
- Light-sensitive
- Sí
Available for research
Tesamorelin is available as a research reagent (RUO):
Frequently asked questions about Tesamorelin
What is Tesamorelin?
Tesamorelin: synthetic 44-amino-acid GHRH analogue and GH secretagogue, FDA approved. With a trans-3-hexenoyl N-terminal stabilizer that confers resistance to DPP-IV.
What is the mechanism of action of Tesamorelin?
Synthetic analog of GHRH (1-44) with a DPP-IV-resistant N-terminal trans-3-hexenoyl stabilizer. It agonizes the GHRH receptor (GHRHR) on somatotrophs of the anterior pituitary and stimulates the endogenous pulsatile secretion of GH, modulating the GH/IGF-1 axis.
What is Tesamorelin researched for?
In preclinical research, Tesamorelin is studied mainly in: Selective GH secretagogue; Reduction of visceral adipose tissue; FDA approved. Material for scientific research use only.
What are the chemical properties of Tesamorelin?
Molecular formula C221H366N72O67S; molecular weight 5135.89 Da; CAS number 218949-48-5.
How is Tesamorelin stored?
Condiciones de conservación: -20 °C liofilizado; 2-8 °C reconstituido; estabilidad liofilizado: 24 meses; una vez reconstituido: 30 días refrigerado; protéjase de la luz.
What routes of administration are studied for Tesamorelin?
In the research models the following are described: Subcutaneous. Use is exclusively for scientific research.