Tesamorelin
approvedAlso known as: Egrifta, TH9507
**Mechanism of Action** Tesamorelin is a synthetic stabilized analog of growth hormone-releasing hormone (GHRH), designed to restore endogenous growth hormone (GH) secretion. By binding to GHRH receptors on pituitary somatotrophs, it stimulates pulsatile GH release, subsequently elevating insulin-like growth factor 1 (IGF-1) levels. This activation of the GH/IGF-1 axis promotes lipolysis and reduces visceral adipose tissue (VAT) accumulation, particularly in patients with HIV-associated lipodystrophy, where GH deficiency is common. Unlike recombinant GH, tesamorelin preserves the physiological pulsatility of GH secretion, potentially reducing adverse metabolic effects. **Key Research Findings** Clinical trials (e.g., Phase III studies) demonstrate that tesamorelin (2 mg/day subcutaneous) significantly reduces VAT by 15–20% over 26 weeks in HIV patients with lipodystrophy, with sustained effects during long-term use. Improvements in triglyceride levels and body composition are observed, though no significant changes in subcutaneous fat or glycemic control are noted. Adverse effects include arthralgias, injection-site reactions, and transient increases in IGF-1 levels. Long-term safety data (up to 2 years) show no increased risk of neoplasia or glucose intolerance, though monitoring of IGF-1 and HbA1c is recommended. **Clinical Relevance** Tesamorelin is FDA-approved for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. It is the only GHRH analog specifically indicated for this condition, offering a targeted approach to VAT reduction without the systemic risks of exogenous GH. Its use is contraindicated in patients with active malignancies, pituitary disorders, or hypersensitivity. Ongoing research explores its potential in non-HIV metabolic disorders, including obesity and nonalcoholic fatty liver disease (NAFLD), though these remain investigational. For research purposes only — not medical advice.
Key data
C221H366N72O67SResearch & studies
Tesamorelin reduced visceral fat area by median -25 cm² vs. +14 cm² with placebo (P=0.001).; Hepatic fat fraction decreased by -4.2% with tesamorelin vs. -0.5% with placebo (P=0.01).; Trunk-to-appendicular fat ratio improved significantly with tesamorelin (P=0.03).; Adverse events including hyperglycemia were similar between groups.
Nineteen major in vitro metabolites of four GHRH analogs were identified and synthesized as reference materials.; A sensitive LC-MS/MS method was developed using parent peptides and metabolites spiked into urine.; Detection limits for target peptides were generally 1 ng/ml or less, meeting WADA's required performance limit.
Frequently asked questions
What is Tesamorelin?
**Mechanism of Action** Tesamorelin is a synthetic stabilized analog of growth hormone-releasing hormone (GHRH), designed to restore endogenous growth hormone (GH) secretion. By binding to GHRH receptors on pituitary somatotrophs, it stimulates pulsatile GH release, subsequently elevating insulin-like growth factor 1 (
How does Tesamorelin work?
Stabilized GHRH analog approved for HIV-associated lipodystrophy; reduces visceral adipose tissue via GH/IGF-1 axis stimulation.
What is the research status of Tesamorelin?
Tesamorelin is currently classified as approved, with 90 research references on record. This is for research purposes only and is not medical advice.
What is the half-life of Tesamorelin?
The reported half-life of Tesamorelin is 26-38 minutes.
What is the molecular weight of Tesamorelin?
Tesamorelin has a molecular weight of approximately 5136 g/mol (formula C221H366N72O67S).
Related peptides
Endogenous cyclic peptide that inhibits GH, insulin, glucagon, and gastric secretion via SSTR1-5 receptors.
Endogenous 28-aa 'hunger hormone' from the stomach; activates GHS-R1a to stimulate GH release and appetite.
First-generation ghrelin receptor agonist hexapeptide that stimulates GH release and strongly increases appetite.
Potent GHRP-family ghrelin receptor agonist with studied cardioprotective effects independent of GH release.
Synthetic hexapeptide ghrelin receptor agonist that potently stimulates GH secretion; also raises appetite, cortisol, and prolactin.
Selective ghrelin receptor (GHS-R1a) agonist that stimulates GH release with minimal effect on cortisol or prolactin.
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