Paragon Sports Medicine

Tesamorelin

Tesamorelin is a synthetic 44-amino acid polypeptide analogue of human Growth Hormone-Releasing Hormone (GHRH) developed by Theratechnologies, Inc. and approved by the FDA in 2010 as the first and only medication specifically indicated for reducing excess abdominal fat in HIV-infected patients with lipodystrophy.

The peptide features enhanced stability and potency through N-terminal modification with a trans-3-hexenoic acid group, providing greater resistance to enzymatic degradation than endogenous GHRH. This structural enhancement results in superior therapeutic efficacy and improved pharmacological properties.

Beyond its FDA-approved indication, tesamorelin demonstrates significant research potential for metabolic disorders, nonalcoholic fatty liver disease (NAFLD), insulin resistance, and visceral adiposity reduction. Its mechanism through growth hormone stimulation offers unique therapeutic benefits while preserving natural hormonal feedback mechanisms.

Structural chemical formula of Tesamorelin molecule with labeled atoms and bonds.

Overview

Tesamorelin demonstrates enhanced pharmacokinetic properties compared to endogenous GHRH, contributing to its unique therapeutic profile. The peptide is metabolized primarily through local receptor-mediated pathways and excreted through urine, with detectability up to several days post-administration using specialized assay methods.

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Chemical structure & Properties

  • Molecular Formula: C₂₂₁H₃₆₆N₇₂O₆₇S
  • Molecular Weight: 5135.9 Daltons (free base)
  • Sequence: 44-amino acid synthetic analogue of human GHRH with trans-3-hexenoic acid modification
  • Half-life: 26-38 minutes (subcutaneous administration)
  • Stability:  Enhanced resistance to dipeptidyl aminopeptidase degradation, superior to native GHRH

Regulatory Status and Legal Considerations

Regulatory information current as of 28 August 2026. This is a summary, not legal or medical advice, and status can change.

FDA Status

  • Classification: Prescription medication for HIV-associated lipodystrophy
  • Approval Status: FDA-approved for specific indication (2010). Egrifta SV was approved in 2019 and Egrifta WR in March 2025.
  • Compounding: Available through specialty pharmacies only
  • Regulatory Position: Approved with established safety and efficacy profile

International Status

  • Classification: Prohibited under S2 at all times; tesamorelin is named as a GHRH analogue.
  • Athletic Use: Banned in competitive sports
  • Testing: Detectable in anti-doping screenings

Legal Availability

  • Commercial Status: FDA approved for one specific indication. Not approved for any other use.
  • Market Presence: Distributed through specialty pharmacy networks
  • Quality Control: FDA-regulated manufacturing and distribution standards
  • Clinical Use: Approved for medical use with physician supervision
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Conclusion

What the evidence supports

Tesamorelin is a growth-hormone-releasing hormone analog supported by controlled trials in HIV-associated lipodystrophy, for which it is FDA approved (Egrifta, with Egrifta SV in 2019 and Egrifta WR in 2025). Uses outside that indication are off-label and are not established by the same evidence, and it is prohibited under WADA. This page summarizes the published research and nothing further.

TESAMORELIN SCIENTIFIC

DATA SUMMARY

Parameter
Molecular Weight
Amino Acid Length
Half-Life
Bioavailability
Detection Window
Value
5135.9 Da (free base)
44 residues
26-38 minutes (subcutaneous)
Less than 4% (subcutaneous)
Up to 4 days (urine)
Application
Growth Hormone Release
Lipolysis Enhancement
IGF-1 Stimulation
Metabolic Function
Reported outcome (model)
8-hour sustained GH elevation, superior to native GHRH
Hormone-sensitive lipase activation, increased fat breakdown
Dose-dependent IGF-1 production increase
Improved glucose homeostasis, enhanced fat oxidation
Study Type
Phase III Trials
Cardiovascular Risk Study
Diabetes Safety Trial
Fat Quality Analysis
Population
806 HIV patients
Phase III subanalysis
53 type 2 diabetics
341 HIV patients
Results
approx. 15-18% VAT reduction vs placebo
0.40% reduction in 10-year ASCVD risk
No significant glucose intolerance
Improved adipose tissue density and quality
Limitations
HIV-specific population
Post-hoc analysis
Short-term study (12 weeks)
Surrogate endpoints
Parameter
Acute Toxicity
Organ Toxicity
Adverse Events
Long-term Safety
Finding
No LD50 established (up to 0.6 mg/kg tested)
No significant histologic changes in major organs
Injection site reactions (approximately one third of patients), arthralgia, myalgia
Long-term data limited to the HIV lipodystrophy population; no long-term cardiovascular outcome data
Authority
FDA
WADA Status
DEA
Classification
Prescription Drug
S2 - prohibited at all times
Unscheduled
Status
Approved for HIV lipodystrophy
Prohibited in sports
Not controlled substance

About this library

This library is published for education. It summarizes published research on compounds studied in this field. Many have no approved medical use, and several cannot lawfully be compounded in the United States. The presence of a page here does not mean Paragon offers that compound. Nothing on these pages is an offer to treat.

This page is general education about a compound studied in this field. Nothing here is medical advice, a recommendation, or an offer to prescribe or supply. A page appearing in this library does not mean Paragon Sports Medicine offers that compound.

Disclaimer: This information is provided for educational purposes only and does not constitute medical advice. Tesamorelin is FDA-approved only for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. Patients should consult with qualified healthcare providers before considering any peptide therapy.

Statements on this page have not been evaluated by the FDA and are not intended to diagnose, treat, cure, or prevent any disease. Many peptides described here are not FDA approved for the uses discussed, and some cannot lawfully be compounded in the United States. Nothing on this page is medical advice or a recommendation for any individual. Whether any therapy is appropriate depends on your history, your laboratory results, and a clinical evaluation. Individual results vary. This page is published for education. Use of this site does not create a physician-patient relationship.