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Stabilized GHRH analog with demonstrated reductions in visceral adipose tissue in HIV‑associated lipodystrophy. Potential benefits include improved body composition and certain metabolic markers via increased GH/IGF‑1. Indication is specific; benefits outside labeled use are not established and require monitoring for glucose and IGF‑1.
Description
Tesamorelin is a synthetic 44–amino‑acid peptide analogue of human growth hormone‑releasing hormone (GHRH). It is N‑terminally modified with a trans‑3‑hexenoyl group at Tyr¹ to improve stability against dipeptidyl peptidase‑IV and prolong activity. Tesamorelin binds the pituitary GHRH receptor to stimulate pulsatile growth hormone (GH) secretion and secondarily raises insulin‑like growth factor‑1 (IGF‑1). It is approved in certain regions for the reduction of excess abdominal fat in adults with HIV‑associated lipodystrophy.
Chemical Structure / Identifiers
| Property | Detail |
| Class/Target | GHRH analogue; agonist at the GHRH receptor (GHRHR) |
| Length / Modification | 44 amino acids; N‑terminal trans‑3‑hexenoyl group at Tyr¹ |
| Molecular Formula (free base) | C221H366N72O67S |
| Approx. Molecular Weight | ≈ 5131 g/mol (sequence‑based; database entries ~4.7–5.1 kDa vary by salt/hydration) |
| CAS Number | 218949‑48‑5 (tesamorelin); 901758‑09‑6 (tesamorelin acetate) |
| PubChem CID | 16137828 (free base) |
| Synonyms | TH9507; tesamorelin acetate (salt); INN tesamorelin |
Primary Research Focus / Clinical Effects
• HIV‑associated lipodystrophy: randomized trials demonstrate reductions in visceral adipose tissue and waist circumference vs placebo.
• Endocrine physiology: increases GH pulse amplitude and IGF‑1 concentrations; effects on lipid profiles and hepatic fat have been reported.
• Metabolic endpoints: exploratory data on glucose tolerance and triglycerides; ongoing interest in broader cardiometabolic risk modification.
• Mechanistic rationale: restoration of GHRH‑GH signaling to reshape adipose distribution and metabolism.
Safety / Limitations
• Common adverse reactions: injection‑site reactions, arthralgia, myalgia, peripheral edema, nausea, and erythema.
• Glucose metabolism: may worsen glucose intolerance; monitor fasting glucose/HbA1c in at‑risk individuals.
• Neoplasia and IGF‑1: avoid in active malignancy; evaluate prior malignancy for stability; monitor IGF‑1 for sustained elevations.
• Hypersensitivity: contraindicated in known hypersensitivity to tesamorelin or formulation excipients (e.g., mannitol in some products).
• Pregnancy: not recommended; use is contraindicated in pregnancy in labeling for some regions.
• Indication‑specific: approvals are limited to HIV‑associated lipodystrophy; safety/efficacy for other uses not established.
Key Publications / References
PubChem Compound Summary: Tesamorelin (CID 16137828). https://pubchem.ncbi.nlm.nih.gov/compound/16137828
FDA Labeling (2025 update): Tesamorelin prescribing information. https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/022505s020lbl.pdf
EGRIFTA SV (tesamorelin) Full Prescribing Information (2024). https://www.egriftasv.com/documents/Prescribing-Information.pdf
Ferdinandi ES et al. Non‑clinical pharmacology and safety evaluation of TH9507 (tesamorelin), a stabilized GHRH analogue. Regul Toxicol Pharmacol. 2007. PubMed: https://pubmed.ncbi.nlm.nih.gov/17214611/
NEJM/clinical literature summary of tesamorelin in HIV‑associated lipodystrophy (reviewed in DrugBank article). https://go.drugbank.com/articles/A7430
Wikipedia overview (identifiers, modification at Tyr¹). https://en.wikipedia.org/wiki/Tesamorelin
Disclaimer: For research background only. Consult current prescribing information for indication‑specific dosing and safety.
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