DRPSHP

Scientific Reference

Tesamorelin

Evidence profile: Human Phase 3 evidence

Native growth hormone-releasing hormone is inactivated by dipeptidyl peptidase-4 within minutes, and Tesamorelin is an attempt to solve that specific problem. It keeps all 44 residues of human GHRH and modifies the N-terminus, attaching a trans-3-hexenoyl group to the first residue, tyrosine, a change reported to shield the peptide from that enzyme. It is a different approach from sermorelin, which truncates the hormone to its first 29 residues and carries no protecting group at all. Human clinical research has concentrated on HIV-associated lipodystrophy, a disorder of fat distribution, with smaller studies elsewhere; animal and cell work on the growth hormone axis sits alongside it. Outside the lipodystrophy setting, human data are limited.

Mechanism of Action

The binding target is the GHRH receptor on anterior pituitary somatotrophs — the same class B G-protein-coupled receptor that native GHRH and sermorelin reach. Activation raises cyclic AMP and has been reported to increase both the synthesis and the release of growth hormone, and the release stays pulsatile because somatostatin and IGF-1 feedback are untouched by any of this. Growth hormone in the circulation then drives IGF-1 production, principally in the liver. Adipose tissue studies have looked at growth hormone's lipolytic action as one step in that chain, although how much belongs to growth hormone and how much to IGF-1 is not fully resolved.

Molecular Information

  • Type: GHRH analogue (growth hormone secretagogue)
  • 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