Cobalt PeptidesResearch Grade

Scientific Reference

Tesamorelin

Evidence profile: Human Phase 3 evidence

Tesamorelin is a modified form of human growth hormone-releasing hormone (GHRH), keeping all 44 residues but altering the N-terminus. A trans-3-hexenoyl group is attached to the first residue, tyrosine, a change reported to shield the peptide from dipeptidyl peptidase-4, the enzyme that inactivates native GHRH within minutes. That distinguishes it from sermorelin, which keeps only the first 29 residues and carries no protecting group. Human clinical research has concentrated on HIV-associated lipodystrophy, a condition involving abnormal fat distribution, with smaller studies in other areas. Animal and cell work on the growth hormone axis sits alongside this, but outside the lipodystrophy setting, human data are limited.

Mechanism of Action

Tesamorelin binds the GHRH receptor on somatotroph cells of the anterior pituitary, the class B G-protein-coupled receptor also targeted by native GHRH and sermorelin. Receptor activation raises cyclic AMP and has been reported to increase both synthesis and release of growth hormone, which keeps a pulsatile pattern because somatostatin and IGF-1 feedback still operate. Circulating growth hormone in turn drives IGF-1 production, mostly in the liver. Studies of adipose tissue have examined the lipolytic action of growth hormone as one link in this pathway, though the separate roles of growth hormone and IGF-1 are not fully resolved.

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