What Is Tesamorelin?
Quick Answer
Tesamorelin (TH9507) is a synthetic 44-amino acid analog of endogenous GHRH with a molecular weight of 5135.9 Da. It was developed by Theratechnologies Inc. to overcome the inherent instability of native GHRH, which has a half-life of only 3–8 minutes due to rapid cleavage by DPP-4. [1] [2] Key Stru...
Tesamorelin (TH9507) is a synthetic 44-amino acid analog of endogenous GHRH with a molecular weight of 5135.9 Da. It was developed by Theratechnologies Inc. to overcome the inherent instability of native GHRH, which has a half-life of only 3–8 minutes due to rapid cleavage by DPP-4. [1] [2]
Key Structural Feature: A trans-3-hexenoic acid group is anchored to the N-terminal tyrosine (Tyr1), rendering the peptide resistant to DPP-4 degradation and extending the half-life to approximately 26–38 minutes. C-terminal is amidated (-NH₂). [3]
Regulatory Status:
- FDA: Approved as Egrifta SV / Egrifta WR for HIV-associated lipodystrophy (excess abdominal fat reduction). NOT indicated for weight loss. [4]
- EMA: Application withdrawn; not marketed in the EU. [6]
- WADA: Prohibited (S2 — Peptide Hormones, Growth Factors). [5]
Developer: Theratechnologies Inc. (Montreal, Canada) — originally designated TH9507.
Pharmacokinetic Highlights:
- Bioavailability: <4% (subcutaneous)
- Half-Life: ~26–38 min (SC); ~11 min (1.28 mg WR formulation)
- Route: Subcutaneous injection (abdomen)
- Standard Dose: 2 mg SC daily (Egrifta SV); 1.28 mg SC daily (Egrifta WR, bioequivalent)
- Pulsatility: Preserves natural pulsatile GH secretion (unlike rhGH)
References
- Falutz J, Allas S, Kotler D, et al. A placebo-controlled, dose-ranging study of a growth hormone releasing factor in HIV-infected study subjects with abdominal fat accumulation. AIDS, 19(12), 1279-87, 2005.
- Ferdinandi ES, Brazeau P, High K, et al. Non-clinical pharmacology and tolerability evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic Clin Pharmacol Toxicol, 100(1), 49-58, 2007.
- Falutz J, Allas S, Blot K, et al. Metabolic effects of a growth hormone-releasing factor in study subjects with HIV. N Engl J Med, 357(23), 2359-70, 2007.
- Falutz J, Mamputu JC, Potvin D, et al. Effects of tesamorelin (TH9507) in HIV-infected study subjects with excess abdominal fat: pooled analysis of two Phase 3 trials. J Clin Endocrinol Metab, 95(9), 4291-304, 2010.
- Wang Y, Tomlinson B. Tesamorelin, a human growth hormone releasing factor analogue. Expert Opin Investig Drugs, 18(3), 303-10, 2009.
- Grunfeld C, Dritselis A, Kirkpatrick P. Tesamorelin. Nat Rev compound Discov, 10(2), 95-6, 2011.
- 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, 96(1), 150-8, 2011.
- Dhillon S. Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy. Drugs, 71(8), 1071-91, 2011.
- Spooner LM, Olin JL. Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. Ann Pharmacother, 46(2), 240-7, 2012.
- Stanley TL, Falutz J, Marsolais C, et al. Reduction in visceral adiposity is associated with an improved metabolic profile in HIV-infected study subjects receiving tesamorelin. Clin Infect Dis, 54(11), 1642-51, 2012.
- Stanley TL, Fourman LT, Feldpausch MN, et al. Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial. Lancet HIV, 6(12), e821-e830, 2019.
- Adrian S, Scherzinger A, Sanyal A, et al. The Growth Hormone Releasing Hormone Analogue, Tesamorelin, Decreases Muscle Fat and Increases Muscle Area in Adults with HIV. J Frailty Aging, 8(3), 154-159, 2019.
- Baker LD, Barsness SM, Borson S, et al. Effects of Growth Hormone-Releasing Hormone on Cognitive Function in Adults With Mild Cognitive Impairment and Healthy Older Adults. Arch Neurol, 69(11), 1420-9, 2012.
- Lopez J, Quan A, Budihardjo J, et al. Growth Hormone Improves Nerve Regeneration, Muscle Re-innervation, and Functional Outcomes After Chronic Denervation Injury. Sci Rep, 9(1), 3117, 2019.
- Grinspoon SK, Fourman L, Stanley T, et al. Impact of Tesamorelin on Cardiovascular Disease Risk Prediction Scores: Subanalysis. Open Forum Infect Dis, 12(Suppl 1), 2025.
- Clemmons DR, Miller S, Mamputu JC. tolerability and metabolic effects of tesamorelin in study subjects with type 2 diabetes: A randomized, placebo-controlled trial. PLoS One, 12(6), e0179538, 2017.
- Makimura H, Feldpausch MN, Rope AM, et al. Metabolic effects of a growth hormone-releasing factor in obese subjects with reduced growth hormone secretion. J Clin Endocrinol Metab, 97(12), 4769-79, 2012.
- Fourman LT, Czerwonka N, Feldpausch MN, et al. Visceral fat reduction with tesamorelin is associated with improved liver enzymes in HIV. AIDS, 31(16), 2253-9, 2017.
- Mangili A, Falutz J, Mamputu JC, et al. Predictors of research application response to tesamorelin in HIV-infected study subjects with excess abdominal fat. PLoS One, 10(10), e0140358, 2015.
- Lake JE, La K, Erlandson KM, et al. Tesamorelin Improves Fat Quality Independent of Changes in Fat Quantity. AIDS, 35(9), 1395-1402, 2021.
- Makimura H, Murphy CA, Feldpausch MN, Grinspoon SK. The Effects of Tesamorelin on Phosphocreatine Recovery in Obese Subjects With Reduced GH. J Clin Endocrinol Metab, 99(1), 338-343, 2014.
- Stanley TL, Feldpausch MN, Oh J, et al. Effect of tesamorelin on visceral fat and liver fat in HIV-infected study subjects: a randomized clinical trial. JAMA, 312(4), 380-9, 2014.
- Ellis RJ, Vaida F, Hu K, et al. Effects of Tesamorelin on Neurocognitive Impairment in Persons With HIV and Abdominal Obesity. J Infect Dis, 231(5), 1230-1238, 2025.
- Falutz J, Potvin D, Mamputu JC, et al. Effects of tesamorelin in HIV-infected study subjects with abdominal fat accumulation: a randomized placebo-controlled trial with safety extension. J Acquir Immune Defic Syndr, 53(3), 311-22, 2010.
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