CEDAR

Scientific Reference

Tesamorelin

Evidence profile: Human Phase 3 evidence

Tesamorelin is an FDA-approved synthetic growth hormone-releasing hormone (GHRH) analog designed for treating HIV-associated lipodystrophy. This 44-amino acid peptide with a trans-3-hexenoic acid modification at the N-terminus selectively reduces visceral adipose tissue while preserving subcutaneous fat, making it unique among growth hormone therapies. Approved under the brand name Egrifta, tesamorelin stimulates pulsatile GH release through GHRH receptor binding, elevating IGF-1 and driving selective visceral fat reduction. It has additionally been studied off-label for metabolic health, NAFLD treatment, cognitive enhancement, and anti-aging body composition protocols.

Mechanism of Action

Tesamorelin binds to GHRH receptors on pituitary somatotroph cells, stimulating pulsatile release of growth hormone. This leads to increased IGF-1 production, promoting lipolysis and preferential reduction of visceral fat. The modified N-terminal structure enhances stability compared to native GHRH, enabling effective subcutaneous administration.

Molecular Information

  • Type: GHRH analog (growth hormone secretagogue)
  • Length: 44 amino acids
  • Molecular weight: 5136 g/mol
  • Molecular formula: C221H366N72O67S
  • CAS: 218949-48-5

Pharmacokinetics

Mean elimination half-life (T1/2) of tesamorelin was 26 and 38 minutes in healthy subjects and HIV-infected patients, respectively, after subcutaneous administration for 14 consecutive days." (original EGRIFTA label, 2010). By contrast t… The median peak plasma tesamorelin concentration (Tmax) was 0.15 h in both populations." (original EGRIFTA, 2 mg SC, healthy subjects and HIV-infected patients). Current label, EGRIFTA SV: "Following single dose of subcutaneous administr…

Published Research

  • 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. · Obesity research & clinical practice · 2026 · Review

    PMID 41545261 — View on PubMed

  • Effects of Tesamorelin on Neurocognitive Impairment in Persons With HIV and Abdominal Obesity

    Ellis RJ et al. · The Journal of infectious diseases · 2025 · Clinical

    PMID 39813152 — View on PubMed

  • Efficacy and safety of tesamorelin in people with HIV on integrase inhibitors

    Russo SC et al. · AIDS (London, England) · 2024 · Clinical

    PMID 38905488 — View on PubMed

  • Effects of tesamorelin on hepatic transcriptomic signatures in HIV-associated NAFLD

    Fourman LT et al. · JCI insight · 2020 · Clinical

    PMID 32701508 — View on PubMed

  • Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial

    Stanley TL et al. · The lancet. HIV · 2019 · Clinical

    PMID 31611038 — View on PubMed

  • Population pharmacokinetic analysis of tesamorelin in HIV-infected patients and healthy subjects

    González-Sales M et al. · Clinical pharmacokinetics · 2015 · Clinical

    PMID 25358450 — View on PubMed