Tesamorelin is a synthetic growth hormone releasing hormone analogue used in the treatment of visceral adiposity in human immunodeficiency virus (HIV) infected patients with lipodystrophy. Tesamorelin is given subcutaneously and has major effects on glucose and lipid metabolism, but has not been linked to serum aminotransferase elevations during therapy or to instances of clinically apparent acute liver injury.


Tesamorelin (tes" a moe rel' in) is a synthetic 44 amino acid polypeptide analogue of growth hormone releasing hormone (GHRH). The N terminal portion of the molecule has been modified to improve its stability and pharmacokinetics in comparison to native GHRH. Tesamorelin activates GHRH receptors in the pituitary which leads to synthesis and release of growth hormone that acts on multiple cells of the body including hepatocytes where it stimulates production of insulin like growth factor-1 (IGF-1). IGF-1 mediates many of the effects of growth hormone, which in the liver include growth, inhibition of programmed cell death, glucose update and lipolysis. Serum IGF-1 levels tend to be low in patients with obesity, diabetes and particularly in those with lipodystrophy. Tesamorelin was evaluated and found to be effective in decreasing visceral adiposity in patients with lipodystrophy associated with antiretroviral therapy of human immunodeficiency virus (HIV) infection. Tesamorelin was approved for use in the United States as therapy to reduce excess abdominal fat in HIV-infected patients with antiviral therapy-related lipodystrophy in 2010. Tesamorelin is also being evaluated as therapy of insulin resistance, obesity and nonalcoholic fatty liver. Tesamorelin is available in solution in vials of 1 mg/mL under the brand name Egrifta. The recommended dose is 2 mg daily given by subcutaneous injection. Side effects are not common but can include injection site reactions, itching, arthralgia, myalgia and peripheral edema. Tesamorelin raises IGF-1 levels and monitoring for elevations during therapy is recommended. Potential, rare adverse events include stimulation of malignant tumor growth, glucose intolerance, diabetes and hypersensitivity reactions.


In clinical trials in patients with HIV-associated lipodystrophy, tesamorelin therapy was not associated with de novo elevations in serum enzymes and, in some studies, was associated with decreases in preexisting ALT elevations, possibly mediated by improvements in nonalcoholic fatty liver. Instances of clinically apparent liver injury attributable to tesamorelin use have not been reported.

Likelihood score: E (unlikely cause of clinically apparent liver injury).

Mechanism of Injury

Tesamorelin is a synthetic polypeptide that acts upon growth hormone producing cells in the pituitary and is generally metabolized locally by the receptor bearing cells. As a polypeptide, tesamorelin is unlikely to have direct cytotoxicity. Allergic responses to its administration have not caused hepatic or systemic hypersensitivity responses.

Drug Class: Hormonal Agents



Tesamorelin – Egrifta Depot®


Hormonal Agents


Product labeling at DailyMed, National Library of Medicine, NIH



References updated: 20 October 2018

Abbreviations: VAT, visceral adipose tissue; IGF-1, insulin-like growth factor-1.

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    (Among 61 patients with HIV infection and excess visceral adipose tissue [VAT] treated with tesamorelin [1 or 2 mg sc daily] or placebo for 12 weeks, change in VAT was greatest with the higher dose [-16%] vs lower dose [-4%] and placebo [-5%], while adverse event rates were similar and liver test results “did not differ between the groups”).
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    (Among 412 patients with HIV infection and excess visceral adiposity treated with tesamorelin or placebo by sc injection once daily for 26 weeks, mean VAT decreased with tesamorelin [-15%] more than placebo [+5%], and adverse event rates were similar with no liver related serious adverse events and mean serum ALT levels decreasing in both groups [-4 vs -2 U/L]).
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    (Among 404 HIV infected patients with excess abdominal adiposity treated with tesamorelin or placebo for 6 months and then switched to placebo or given tesamorelin for another 6 months, VAT decreased with tesamorelin compared to placebo, but this effect was lost when tesamorelin was stopped while adverse event rates were similar with either treatment; no mention of ALT elevations or hepatotoxicity).
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    (In retrospective analyses of two large controlled trials of tesamorelin in HIV infected patients with excess VAT, those who responded to treatment with reduction in VAT also had greater reductions in triglyceride levels and measures of glucose homeostasis).
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    (Review of the safety and efficacy of tesamorelin in HIV infected patients with lipodystrophy; mentions that headache and arthralgias were the most frequent adverse events that led to discontinuation; no mention of ALT elevations or hepatotoxicity).
  • Stanley TL, Feldpausch MN, Oh J, Branch KL, Lee H, Torriani M, Grinspoon SK. Effect of tesamorelin on visceral fat and liver fat in HIV-infected patients with abdominal fat accumulation: a randomized clinical trial. JAMA 2014; 312: 380-9. [PMC free article: PMC4363137] [PubMed: 25038357]
    (Among 48 HIV infected patients with excess visceral and hepatic fat treated with tesamorelin vs placebo for 6 months, median changes in hepatic fat were -2% vs +1%, while median ALT levels did not change in either group [20 to 20 U/L vs 19 to 17 U/L]).
  • Chalasani N, Bonkovsky HL, Fontana R, Lee W, Stolz A, Talwalkar J, Reddy KR, et al.; United States Drug Induced Liver Injury Network. Features and outcomes of 899 patients with drug-induced liver injury: The DILIN Prospective Study. Gastroenterology 2015; 148: 1340-52. [PMC free article: PMC4446235] [PubMed: 25754159]
    (Among 899 cases of drug induced liver injury enrolled in a US prospective study between 2004 and 2013, none were attributed to tesamorelin).
  • Fourman LT, Czerwonka N, Feldpausch MN, Weiss J, Mamputu JC, Falutz J, Morin J, et al. Visceral fat reduction with tesamorelin is associated with improved liver enzymes in HIV. AIDS 2017; 31: 2253-9. [PMC free article: PMC5633509] [PubMed: 28832410]
    (Among 176 patients with HIV infection and ALT or AST elevations who were treated with tesamorelin for reduction of visceral adipose tissue [VAT], mean aminotransferase levels decreased more in those with a decrease in VAT [ALT by -9 vs +1 U/L and AST by -4 vs 0 U/L]).
  • Clemmons DR, Miller S, Mamputu JC. Safety and metabolic effects of tesamorelin, a growth hormone-releasing factor analogue, in patients with type 2 diabetes: A randomized, placebo-controlled trial. PLoS One 2017; 12: e0179538. [PMC free article: PMC5472315] [PubMed: 28617838]
    (Among 53 patients with type 2 diabetes treated with tesamorelin or placebo for 12 weeks, there were no changes in measures of insulin response or diabetes control (fasting glucose or HbA1c levels); no mention of ALT levels or liver related adverse events).