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 off-target 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 triglycerides and total cholesterol are observed, though no significant changes in subcutaneous fat or lean body mass occur. Adverse effects include arthralgias, injection-site reactions, and transient increases in IGF-1; long-term safety data show no increased risk of glucose intolerance or malignancy. PubMed-indexed studies (n=90) confirm its efficacy in VAT reduction, with ongoing research exploring off-label applications in non-HIV metabolic disorders. **Clinical Relevance** Tesamorelin is FDA-approved (Egrifta) for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. It is the only pharmacologic agent specifically indicated for this condition, addressing a significant unmet need in HIV management. Its use requires monitoring of IGF-1, glucose, and pituitary function. Off-label applications (e.g., aging-related sarcopenia, obesity) remain investigational due to limited evidence and potential risks. For research purposes only — not medical advice.
Key data
C221H366N72O67SResearch & studies
Therapeutic peptides are effective for type 2 diabetes and obesity treatment.; Peptides show potential for skin rejuvenation and as hormone analogs.; Novel unapproved peptides are expanding into preventive medicine and performance enhancement.; More research is required to ensure safe human use of most new peptides.
Tesamorelin reduced waist circumference more than standard of care (median difference -2.7 cm, P = .015).; Neurocognitive performance improvement trended in the tesamorelin group (mean change 0.146, P = .060) but between-group difference was not significant (P = .673).; IGF-1 levels increased with tesamorelin but did not correlate with cognitive changes or waist circumference reduction.; The study was limited by insufficient power and lack of placebo arm, suggesting no clear cognitive benefit from short-term abdominal obesity reduction with tesamorelin.
Tesamorelin led to significant declines in visceral fat (median -25 vs. 14 cm², P=0.001).; Hepatic fat fraction decreased significantly with tesamorelin (-4.2% vs. -0.5%, P=0.01).; Trunk-to-appendicular fat ratio improved with tesamorelin (-0.1 vs. 0.0, P=0.03).; Tesamorelin was well tolerated with similar adverse events, including hyperglycemia, 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 for detecting parent peptides and metabolites in urine.; Detection limits for target peptides were generally 1 ng/ml or less, meeting WADA performance limits.
Tesamorelin increased VAT density by +6.2 HU and SAT density by +4.0 HU over 26 weeks, versus +0.3 HU for both in placebo.; Improvements in fat density persisted after controlling for baseline fat density and changes in fat area.; Tesamorelin improves fat quality (density) independently of its effects on fat quantity reduction.
Tesamorelin increased hepatic expression of hallmark gene sets involved in oxidative phosphorylation.; Tesamorelin decreased hepatic expression of gene sets contributing to inflammation, tissue repair, and cell division.; Tesamorelin reciprocally up- and downregulated curated gene sets associated with favorable and poor hepatocellular carcinoma prognosis.; Changes in hepatic expression correlated with improved fibrosis-related gene score among tesamorelin-treated participants.
Tesamorelin significantly decreased waist circumference and visceral adipose tissue after 26 weeks in two Phase 3 trials.; Improvements in visceral adipose tissue were maintained during 26-week extension phases.; No adverse impact on blood glucose or lipid parameters was observed.; Limited data support off-label uses, and limitations include high cost and lack of long-term safety data.
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 93 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).
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