Produktbeschreibung
What is Tesamorelin?
Tesamorelin (also known as TH9507, trade name EGRIFTA) is a synthetic analogue of human growth hormone releasing hormone (GHRH), consisting of 44 amino acids corresponding to the full sequence of endogenous GHRH with an additional N-terminal modification. The compound was developed by the Canadian company Theratechnologies Inc. and received FDA approval in 2010 as the first and only therapy specifically indicated for the reduction of excess abdominal fat in adults with HIV-related lipodystrophy.
Structurally, tesamorelin differs from native GHRH by the presence of a trans-3-hexene group attached to the tyrosine residue at the N-terminus of the molecule. This modification renders the peptide resistant to degradation by the enzyme dipeptidyl peptidase 4 (DPP-4), which rapidly inactivates native GHRH. As a result, tesamorelin has a much longer half-life and better bioavailability after subcutaneous administration. The molecular weight is approximately 5136 Da and the molecular formula is C₂₂₁H₃₆₆N₇₂O₆₇S.
The mechanism of action of tesamorelin involves binding to GHRH receptors on the somatotropes of the anterior pituitary, which stimulates the synthesis and pulsatile release of endogenous growth hormone (GH). Unlike direct administration of recombinant GH, pituitary stimulation by tesamorelin maintains the physiological pulsatile secretion pattern and is regulated by the IGF-1 feedback loop.
HIV-associated lipodystrophy, for which tesamorelin is indicated, is characterized by pathological accumulation of visceral adipose tissue (VAT) and loss of subcutaneous adipose tissue, occurring in patients receiving highly active antiretroviral therapy (HAART). This metabolic syndrome is associated with increased cardiovascular risk and significant deterioration in quality of life.
Mechanism of action
<pphysiological" approach by stimulating endogenous GH secretion while maintaining pulsatility and feedback. It is on the WADA prohibited substances list.
Research safety profile
General tolerability - Tesamorelin demonstrated an acceptable safety profile in clinical trials in over 900 patients.
Adverse reactions - Most frequently observed: hypersensitivity reactions, joint swelling and pain, pain in extremities, peripheral edema, muscle pain, injection site reactions.
IGF-1 elevation - Tesamorelin increases IGF-1 levels, and some patients had values above the upper limit of normal.
Regulatory status - FDA approved for the reduction of excess abdominal fat in adults with HIV-related lipodystrophy. Not approved by EMA.
Bibliography - latest scientific research
- Abdallah R et al. Body composition, hepatic fat, metabolic, and safety outcomes of Tesamorelin in HIV-associated lipodystrophy: A meta-analysis. Obes Med. 2025. ScienceDirect
- FDA. FDA Approves F8 Formulation of Tesamorelin. FDA News. March 2025. FDA
- Stanley TL et al. Effect of tesamorelin on visceral fat and liver fat in HIV-infected patients. JAMA. 2014;312(4):380-389. PubMed
- Makimura H et al. Growth hormone and tesamorelin in HIV-associated lipodystrophy. HIV AIDS (Auckl). 2011;3:65-76. PMC
- 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. PubMed
- Rochira V, Guaraldi G. Growth hormone deficiency and human immunodeficiency virus. Best Pract Res Clin Endocrinol Metab. 2017;31(1):91-111. PubMed
- Fourman LT et al. Effects of Tesamorelin on Hepatic Transcriptomic Signatures in HIV-Associated NAFLD. JCI Insight. 2020;5(17):e140134. PMC
- Lo J et al. Tesamorelin Decreases Muscle Fat and Increases Muscle Area in Adults with HIV. J Frailty Aging. 2019;8(4):201-206. PubMed
- Spooner LM, Olin JL. Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. Ann Pharmacother. 2012;46(2):240-247. PubMed
- Dhillon S. Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy. Drugs. 2011;71(8):1071-1091. PubMed
