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GHRH(1-44) with trans-3-hexenoyl N-terminal modification
Growth Hormone Secretagogue

Tesamorelin

FDA-approved GHRH analog (Egrifta) for visceral fat reduction with Phase III clinical trial data.

Mechanism of Action

Bioregulator compound with targeted biochemical activity.

Evidence Chain

Tesamorelin

COMPOUND

1 Research Goal

• Muscle & Tissue Growth

Evidence Strength

Clinical Trial

2 articles sourced

Knowledge Graph

(3 connections)
CompoundGoalArticleArticle
Compound (Center)
Research Goal
Linked Article

Overview

Tesamorelin is a synthetic growth hormone-releasing hormone (GHRH) analog approved by the FDA under the brand name Egrifta for the treatment of HIV-associated lipodystrophy. It represents one of the few GHRH analogs with FDA approval and Phase III clinical trial data. Tesamorelin's specific indication — reduction of visceral adipose tissue in HIV patients on antiretroviral therapy — demonstrates the potential of GHRH-based therapies for targeted metabolic applications.

Mechanism of Action

Tesamorelin is a modified analog of the first 44 amino acids of naturally occurring GHRH, with the addition of a 3-hexenoyl group at the N-terminus that enhances stability against enzymatic degradation. It acts on GHRH receptors in the anterior pituitary, stimulating the synthesis and pulsatile release of endogenous growth hormone. The resulting increase in GH and IGF-1 promotes lipolysis (fat breakdown) in visceral adipose tissue, reducing the abnormal fat accumulation characteristic of HIV lipodystrophy. The preservation of natural GH pulsatility and feedback regulation distinguishes it from exogenous GH administration.

Research Highlights

The Phase III clinical trials demonstrated Tesamorelin's efficacy in reducing visceral adipose tissue (VAT) by approximately 15-20% in HIV patients with lipodystrophy, with significant improvements in body composition and metabolic markers. Research showed sustained VAT reduction over 26 weeks of treatment, with partial rebound upon discontinuation. Studies explored its potential in non-HIV populations with visceral obesity, cognitive function in mild cognitive impairment, and cardiovascular risk markers. Research has shown improvements in triglycerides, cholesterol, and carotid intima-media thickness.

Dosage & Administration

FDA-approved dosing is 2 mg subcutaneously once daily. The lyophilized powder requires reconstitution with sterile water before administration. For research use only (RUO) — this information is provided for educational purposes only.

Safety Profile

As an FDA-approved drug, Tesamorelin has a well-characterized safety profile. Common side effects include injection site reactions, joint pain, flushing, and peripheral edema. Less common effects include hyperglycemia and carpal tunnel symptoms. Contraindicated in patients with active malignancy, pregnancy, and known hypersensitivity. Does not suppress natural GH production upon discontinuation.

References

Falutz J, et al. Tesamorelin in HIV lipodystrophy. N Engl J Med. 2010. Falutz J, et al. Long-term safety of tesamorelin. AIDS. 2012. FDA Egrifta prescribing information. All content is for educational and research purposes only.

Synergy & Compatibility

(5)

Computational assessment of bio-regulatory compatibility with compounds sharing research goals. Scores reflect half-life alignment, receptor target overlap, and bioavailability data.

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Computational assessment based on available pharmacology data. Does not account for individual variability, dose-dependent effects, or unstudied interactions. For research use only.

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