COMPOUND NAME
Tesamorelin
SYNONYMS
TH9507, Egrifta®
CAS NUMBER
218949-48-5
MOLECULAR FORMULA
C221H366N72O61S
MOLECULAR WEIGHT
~5137.9 Da
STRUCTURE
Synthetic 44-amino acid peptide
PEPTIDE SEQUENCE
H-Tyr-D-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH?
CHEMICAL STRUCTURE
Molecular Formula: C221H366N72O61S
Tesamorelin acts as a GHRH receptor agonist. It binds to pituitary somatotroph cells, stimulating the synthesis and release of endogenous GH. This leads to elevated IGF-1, promoting anabolic and lipolytic activity primarily in adipose tissue, particularly reducing VAT with minimal impact on subcutaneous fat.
1
GHRH Receptor (GHRH-R) Agonism
2
Stimulates pulsatile growth hormone (GH) secretion: Tesamorelin binds to GHRH receptors on a pituitary somatotrophs, increasing cyclic AMP (cAMP) levels and activating PKA and MAPK signaling pathways, resulting in physiologic GH release that mimics natural circadian pulsatility2,3.
3
Increases circulating IGF-1 levels: Endogenous GH released in response to tesamorelin upregulates hepatic IGF-1 production, leading to enhanced lipolytic, anabolic, and metabolic activity throughout peripheral tissues1.
4
Preserves feedback sensitivity: Unlike exogenous GH therapy, tesamorelin maintains the hypothalamic-pituitary feedback loop, allowing for regulation of GH and IGF-1 within physiologic ranges3,4.
5
Depot-selective lipolysis: The GH/IGF-1 signaling axis preferentially targets visceral adipose depots, promoting triglyceride hydrolysis and reduced VAT without significantly affecting subcutaneous fat or lean mass1,3.
6
Receptor Binding Affinity: Tesamorelin binds the GHRH receptor with high affinity, exhibiting similar potency to endogenous GHRH (IC?
?, Human = ~0.069 nM) and greater resistance to enzymatic degradation by DPP-IV2,3.
Tesamorelin increases pulsatile GH and IGF-1 levels, reduces VAT, and improves lipid profiles and body image metrics in HIV patients. It shows minimal effect on glucose homeostasis but may slightly raise HbA1c in some users.
20°C or below. Protect from light and moisture.
Peptides; Growth Hormone Secretagogues; Endocrine Modulators
FDA-approved for HIV-associated lipodystrophy Reduces VAT without worsening glycemic control Improves hepatic steatosis in HIV-associated NAFLD
Property
Description
CAS Number
218949-48-5
Molecular Formula
C221H366N72O61S
Molecular Weight (MW)
~5137.9 Da
Mechanism of Action
Dual agonist at GIP and GLP-1 receptors; biased signaling, GIPR-dominant
Biological Activity
Reduces VAT, increases IGF-1, minimal impact on glucose control
Supplied Form
Lyophilized powder
Purity
?98% (HPLC)
Storage
-20°C, dry, light-protected
Drug Categories
Peptides; Incretin mimetic
Additional Notes
FDA-approved; used in HIV-associated lipodystrophy and NAFLD
For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.
Tesamorelin is a stabilized synthetic analogue of human growth hormone-releasing hormone (GHRH), comprising a 44-amino acid sequence with an N-terminal modification that enhances resistance to enzymatic degradation. Clinically, Tesamorelin is approved for the treatment of excess abdominal fat in HIV-infected individuals with lipodystrophy. This approval is based on consistent reductions in visceral adipose tissue (VAT) observed across controlled studies. The compound has also been evaluated in metabolic conditions related to HIV, including hepatic steatosis, with emerging evidence suggesting benefit in reducing intrahepatic lipid content and modulating fibrotic progression. Tesamorelin is intended for investigational and clinical use in the context of metabolic disorders characterized by altered fat distribution or growth hormone axis dysregulation. It is not indicated for use in the general population outside approved clinical settings.
VAT Reduction:
Tesamorelin significantly reduces visceral adipose tissue (~15–20%) in HIV-associated lipodystrophy, with effects maintained over 52 weeks in continuous users.
Fat Selectivity:
Targets VAT with minimal impact on subcutaneous fat or lean mass.
Body Composition Benefits:
Treatment is associated with reductions in waist circumference and improvements in body image-related outcomes.
Liver Effects:
In HIV-associated NAFLD, tesamorelin reduces liver fat and attenuates fibrosis progression, supported by transcriptomic downregulation of fibrotic and inflammatory gene pathways.
Metabolic Profile:
IGF-1 levels rise predictably with treatment; glycemic effects are minimal, with only modest, clinically insignificant increases in HbA1c observed.
Route of Administration
Subcutaneous
Dosing Frequency
Once daily
Route of Administration: Subcutaneous injection Dosing Frequency: Once daily Half-Life: ~38 minutes in HIV+ patients2 Formulation: Lyophilized acetate salt for reconstitution
Reconstitute lyophilized powder in sterile bacteriostatic water for injection (0.9% benzyl alcohol) Store reconstituted solution at 2–8°C and use within 14 days Unreconstituted vials should be stored at −20°C in a dry, light-protected environment Avoid repeated freeze-thaw cycles; aliquot as needed for stability Stable for up to 12 months when stored properly in lyophilized form
Trial ID
Title
Phase
Study Type
Sponsor
NCT02572323
Phase II Trial of Tesamorelin for Cognition in Aging HIV-Infected Persons
2
Interventional
University of California, San Diego
NCT02012556
Pharmacokinetic and Pharmacodynamic Study of TH9507, a Growth Hormone-Releasing Factor Analog, in HIV Positive Patients
1
Interventional
Theratechnologies
NCT02196831
Tesamorelin Effects on Liver Fat and Histology in HIV
N/A
Interventional
Massachusetts General Hospital
NCT06554717
Tesamorelin as an Adjunct to Exercise for Improving Physical Function in HIV (TRIUMPH)
2
Interventional
Massachusetts General Hospital
1
Spooner, L. M., & Olin, J. L. Tesamorelin: A Growth Hormone-Releasing Factor Analogue for HIV-Associated Lipodystrophy. Ann Pharmacother 46, 240–247 (2012).
2
Dhillon, S. Tesamorelin: A review of its use in the management of HIV-associated lipodystrophy. Drugs 71, 1071–1091 (2011).
3
Fourman, L.T., Stanley, T.L., Bhasin, J.M. et al. Delineating tesamorelin response pathways in HIV-associated NAFLD using a targeted proteomic and transcriptomic approach. Sci. Rep. 11, 20258 (2021).
4
Wang, Y. & Tomlinson, B. Tesamorelin, a human growth hormone releasing factor analogue. Expert Opin. Investig. Drugs 18, 303–310 (2009).
This product is synthesized via solid-phase peptide synthesis (SPPS) and tested to ≥99% purity by HPLC with identity confirmed by mass spectrometry. A Certificate of Analysis (COA) is available for every batch. Learn about our full quality and testing process →