Tesamorelin
Human RCTTH9507 · TH-9507 · Egrifta · Tesamorelin acetate
Highest available evidence among curated papers: Human RCT (as of 2026-06-04).
Chemical & identity
- Sequence
- YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL
- Length
- 44 residues
- Molecular formula
- C221H366N72O67S
- Molecular weight
- 5136 g/mol · PubChem
- PubChem CID
- 16137828 · PubChem
- SMILES
- CC/C=C/CC(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N
- InChIKey
- QBEPNUQJQWDYKU-BMGKTWPMSA-N
- ChEMBL ID
- CHEMBL1237026 · ChEMBL
- UniProt
- P01286 · UniProt
- Category
- GH secretagogue/GHRH
Chemical/structural fields are auto-pulled and source-linked. ChEMBL data: ChEMBL_36, CC BY-SA 3.0.
Mechanism (curated)
Stabilized analog of growth-hormone-releasing hormone (GHRH, residues 1-44 with an N-terminal hexenoyl group); binds pituitary GHRH receptors to stimulate endogenous GH secretion and raise IGF-1.
Pharmacology & handling
- Half-life
- Approximately 25-40 minutes; administered once daily subcutaneously.
Research
Badran AS et al. · Obesity research & clinical practice · 2026 · Meta-analysis
A meta-analysis of five randomized controlled trials in HIV-positive adults examined tesamorelin, a synthetic growth hormone-releasing hormone analogue, versus placebo for HIV-associated lipodystrophy. Tesamorelin significantly reduced visceral adipose tissue (−27.71 cm²), trunk fat (−1.18 kg), limb fat (−0.22 kg), hepatic fat percentage (−4.28%), and waist circumference (−1.61 cm), while increasing lean body mass (1.42 kg). No significant changes in subcutaneous adipose tissue, BMI, or CD4+ T-cell counts were observed. Adverse events included arthralgia, myalgia, paresthesia, and injection-site reactions like erythema, but no serious adverse effects or glucose perturbation were reported.
2016 · Systematic review
This is a systematic review evaluating tesamorelin, a synthetic growth hormone–releasing factor analogue, for treatment of excess visceral adipose tissue (VAT) in HIV-infected patients with lipodystrophy. The review assessed both beneficial and harmful effects of tesamorelin in treatment-experienced adult HIV patients, using waist circumference and CT-confirmed VAT measurements as outcome criteria. Lipodystrophy in HIV patients is characterized by body composition changes including lipohypertrophy, which negatively affects quality of life; the condition is hypothesized to relate to the virus or specific antiretroviral regimens, particularly protease inhibitors. Tesamorelin is a synthetic analogue that triggers metabolic effects including lipolysis.
Stanley TL et al. · The lancet. HIV · 2019 · RCT
This randomized, double-blind, multicentre trial enrolled 61 HIV-positive patients with non-alcoholic fatty liver disease (NAFLD) and compared tesamorelin 2 mg daily versus placebo for 12 months. Tesamorelin produced a greater reduction in hepatic fat fraction (HFF) than placebo (absolute effect size −4.1%, p=0.018), with 35% of tesamorelin recipients achieving HFF <5% versus 4% of placebo recipients (p=0.0069). Changes in fasting glucose and glycated haemoglobin were not significantly different between groups; localised injection site complaints were more common in the tesamorelin group. The authors conclude tesamorelin might be beneficial in HIV-positive patients with NAFLD, but note that further studies are needed to assess long-term effects on liver histology.
Fourman LT et al. · JCI insight · 2020 · RCT
This study analyzed liver tissue specimens from a randomized placebo-controlled trial of tesamorelin, a growth hormone-releasing hormone analog, in people with HIV-associated nonalcoholic fatty liver disease (NAFLD). Using gene set enrichment analysis on paired liver biopsies, tesamorelin increased hepatic expression of genes involved in oxidative phosphorylation and decreased expression of genes related to inflammation, tissue repair, and cell division compared to placebo. Tesamorelin also upregulated gene sets associated with favorable hepatocellular carcinoma prognosis and downregulated those associated with poor prognosis, with these changes correlating with improved fibrosis-related gene scores in treated participants. The findings provide a mechanistic basis for tesamorelin's observed clinical effects in reducing liver fat and preventing fibrosis progression in this population.
Stanley TL et al. · JAMA · 2014 · RCT
This double-blind, randomized, placebo-controlled trial enrolled 50 antiretroviral-treated HIV-infected patients with abdominal fat accumulation to evaluate tesamorelin (2 mg daily) versus placebo over 6 months. Tesamorelin significantly reduced visceral adipose tissue (mean change -34 cm² vs +8 cm² with placebo) and liver fat (median change -2.0% vs +0.9% in lipid-to-water percentage) at 6 months. Fasting glucose increased transiently at 2 weeks with tesamorelin but differences were not significant at 6 months or for 2-hour glucose. The authors concluded that tesamorelin was associated with reductions in visceral and liver fat in this preliminary study, though further research is needed to determine clinical significance.
Fourman LT et al. · Scientific reports · 2021 · RCT
This analysis examined plasma proteins and transcriptomic pathways in HIV-associated NAFLD treated with tesamorelin, leveraging data from a prior randomized-controlled trial. Tesamorelin significantly reduced plasma levels of three proteins—VEGFA, TGFB1, and CSF1—compared to placebo. Among tesamorelin-treated participants, reductions in VEGFA and CSF1 correlated with improvement in NAFLD activity score, while decreases in TGFB1 and CSF1 correlated with reduced fibrosis score. The authors conclude that tesamorelin suppresses angiogenic, fibrogenic, and pro-inflammatory mediators, with CSF1 identified as a potential therapeutic target in NAFLD associated with HIV.
Russo SC et al. · AIDS (London, England) · 2024 · RCT
This randomized double-blind trial evaluated tesamorelin 2 mg daily versus placebo in 38 people with HIV on integrase inhibitor-based regimens, with 31 completing the 12-month study. Tesamorelin produced significant reductions in visceral fat, hepatic fat, and trunk-to-appendicular fat ratio compared to placebo, with no difference in adverse events between groups. The findings represent the first dedicated data on tesamorelin efficacy and safety in PWH on integrase inhibitors, showing beneficial effects on body composition without exacerbation of glycemic control.
Effects of Tesamorelin on Neurocognitive Impairment in Persons With HIV and Abdominal Obesity.
Human RCTEllis RJ et al. · The Journal of infectious diseases · 2025 · RCT
A 6-month phase 2 randomized open-label trial compared tesamorelin (2 mg subcutaneously daily) versus standard of care in 73 virally suppressed people with HIV and abdominal obesity to assess effects on neurocognitive impairment. Tesamorelin showed a trend toward improved neurocognitive performance (P = 0.060) and reduced waist circumference more than standard of care (median difference −2.7 cm; P = 0.015), but the between-group difference in cognitive outcomes was not significant (P = 0.673). IGF-1 levels increased with tesamorelin but did not correlate with neurocognitive change or waist circumference reduction. The authors concluded that while tesamorelin reduced abdominal obesity, short-term reduction in abdominal obesity did not produce clear cognitive benefits.
Lake JE et al. · AIDS (London, England) · 2021 · RCT
This analysis of data from two placebo-controlled randomized trials examined whether tesamorelin, a growth hormone-releasing hormone analogue, affects fat quality (measured by CT density in Hounsfield Units) independent of fat quantity in people living with HIV. Among 193 tesamorelin responders and 148 placebo-treated participants, tesamorelin-treated individuals showed significant increases in both visceral adipose tissue (VAT) and subcutaneous adipose tissue (SAT) density over 26 weeks compared to placebo, even after controlling for changes in fat area. The authors conclude that tesamorelin improves fat quality in addition to reducing VAT quantity in people living with HIV who respond to treatment.
Falutz J et al. · The Journal of clinical endocrinology and metabolism · 2010 · RCT
This pooled analysis of two phase-3 multicenter, randomized, placebo-controlled trials evaluated tesamorelin 2 mg daily (a GHRH analog) in 806 HIV-infected patients on antiretroviral therapy with excess abdominal fat. At 26 weeks, tesamorelin significantly reduced visceral adipose tissue (VAT) by 24 cm² compared to a 2 cm² increase with placebo, and improved triglycerides, cholesterol-to-HDL ratio, and patient-reported body image without meaningful changes in glucose parameters. VAT reductions and lipid improvements were sustained through 52 weeks in patients who continued tesamorelin. The treatment was generally well tolerated.
Rahman F et al. · Journal of clinical and translational science · 2023 · RCT
This is a post hoc analysis of a phase III double-blind placebo-controlled trial examining tesamorelin, a synthetic growth hormone-releasing hormone indicated for reducing visceral adipose tissue (VAT) in people with HIV. Participants received tesamorelin for 26 weeks, and efficacy was compared between those with and without dorsocervical fat. Among tesamorelin responders, VAT and waist circumference decreased in both groups without statistically significant differences, suggesting tesamorelin's effectiveness is similar regardless of dorsocervical fat presence.
Falutz J et al. · Journal of acquired immune deficiency syndromes (1999) · 2010 · RCT
A 12-month randomized controlled trial of 404 HIV-infected patients with excess abdominal fat compared tesamorelin (2 mg subcutaneous daily) to placebo in a 2:1 ratio for 6 months, followed by an extension phase. Tesamorelin reduced visceral adipose tissue by 10.9% versus 0.6% in placebo at 6 months (P < 0.0001), with improvements in trunk fat, waist circumference, waist-hip ratio, and patient/physician ratings of belly appearance. Insulin-like growth factor-1 increased, but glucose parameters remained unchanged. Continued tesamorelin treatment for 12 months achieved approximately 18% reduction in visceral fat, and improvements were rapidly lost upon switching to placebo.
Falutz J et al. · AIDS (London, England) · 2008 · RCT
This randomized controlled trial of 410 HIV patients with central fat accumulation compared tesamorelin 2 mg daily to placebo for 26 weeks, followed by a 26-week extension phase with reallocation of treatment groups. Tesamorelin was generally well tolerated with adverse event rates comparable between initial and extension phases, and glucose parameter changes were not clinically significant. Treatment with tesamorelin sustained a 18% decrease in visceral adipose tissue and 51 mg/dl decrease in triglycerides over 52 weeks total, with improvements also seen in total cholesterol; however, these effects reversed upon discontinuation of the drug.
Baker LD et al. · Archives of neurology · 2012 · RCT
This randomized, double-blind, placebo-controlled trial examined the effects of tesamorelin, a stabilized analog of growth hormone-releasing hormone (GHRH), on cognitive function in 152 adults (66 with mild cognitive impairment, 86 healthy older adults; aged 55–87 years). Participants self-administered daily subcutaneous injections of tesamorelin 1 mg/day or placebo for 20 weeks, with cognitive testing at baseline, weeks 10 and 20, and after a 10-week washout. Intent-to-treat analysis showed a favorable effect of GHRH on overall cognition (P=0.03), with significant improvement in executive function (P=0.005) and a trend in verbal memory (P=0.08); benefits were comparable in adults with MCI and healthy older adults. Tesamorelin increased insulin-like growth factor 1 levels by 117%, reduced body fat by 7.4%, and increased fasting insulin levels by 35% in adults with MCI. Adverse events were mild and more frequent in the tesamorelin group (68%) than placebo (36%).
Friedman SD et al. · JAMA neurology · 2013 · RCT
This randomized, double-blind, placebo-controlled substudy examined neurochemical effects of tesamorelin (1 mg/day subcutaneously), a GHRH analogue, in 30 adults aged 55–87 years (17 with mild cognitive impairment, 13 healthy older adults) over 20 weeks. Brain proton magnetic resonance spectroscopy showed that tesamorelin increased GABA levels in all three measured brain regions (dorsolateral frontal, posterior cingulate, posterior parietal; P < 0.04), increased NAAG in the dorsolateral frontal cortex (P = 0.03), and decreased myo-inositol in the posterior cingulate (P = 0.002), with no changes in glutamate. Cognitive testing showed a favorable treatment effect (P = 0.03), though no significant associations were found between neurochemical and cognitive changes. The authors propose that modulation of inhibitory neurotransmitters and brain metabolites may explain GHRH effects on cognition in both MCI and healthy aging.
Summaries are our own; we link to originals (PubMed / DOI) and never rehost full text.
Regulatory status
- FDA approved
- Yes
- WADA prohibited
- Yes
- Compounding status
- FDA-approved (Egrifta) to reduce excess visceral abdominal fat in HIV-associated lipodystrophy.
- Notes
- FDA-approved tesamorelin (Egrifta) for excess visceral abdominal fat in HIV-associated lipodystrophy as of 2026-06-04. Prohibited in sport under WADA (GHRH analog).
Legal/regulatory status varies by jurisdiction and changes over time — accurate as of last review (2026-06-04).
Data sources: Curated IDs (PubChem/UniProt/ChEMBL) + Europe PMC + ClinicalTrials.gov (2026-06-04).
Last reviewed 2026-06-04