Tesamorelin 10mg

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-NH₂

Chemical Structure:

Source: PubChem

Mechanism of Action: 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.

Biological Activity: 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.

Storage: −20°C or below. Protect from light and moisture.

Drug Categories: Peptides; Growth Hormone Secretagogues; Endocrine Modulators

Additional Notes:

• FDA-approved for HIV-associated lipodystrophy
• Reduces VAT without worsening glycemic control
• Improves hepatic steatosis in HIV-associated NAFLD

Summary Table:

Disclaimer: For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.

Detailed Product Description

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.

Research Highlights

• 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.

Mechanism of Action

Tesamorelin is a synthetic peptide analogue of human growth hormone-releasing hormone (GHRH) that functions as a potent agonist of the growth hormone-releasing hormone receptor (GHRH-R). By activating this receptor, tesamorelin stimulates the endogenous secretion of growth hormone (GH) from the anterior pituitary, thereby initiating the GH–insulin-like growth factor 1 (IGF-1) axis and driving downstream metabolic effects.

1. GHRH Receptor (GHRH-R) Agonism

• 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 pulsatility^2,3.
• 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.
• Preserves feedback sensitivity: Unlike exogenous GH therapy, tesamorelin maintains the hypothalamic-pituitary feedback loop, allowing for regulation of GH and IGF-1 within physiologic ranges^3,4.
• 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 mass^1,3.
• Receptor Binding Affinity: Tesamorelin binds the GHRH receptor with high affinity, exhibiting similar potency to endogenous GHRH (IC₅₀, Human = ~0.069 nM) and greater resistance to enzymatic degradation by DPP-IV^2,3.

Pharmacokinetic Profile:

• Route of Administration: Subcutaneous injection
• Dosing Frequency: Once daily
• Half-Life: ~38 minutes in HIV+ patients²
• Formulation: Lyophilized acetate salt for reconstitution

Formulation & Handling

• 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

Selected Clinical Trial Activity

References

¹Spooner, L. M., & Olin, J. L. Tesamorelin: A Growth Hormone-Releasing Factor Analogue for HIV-Associated Lipodystrophy. Ann Pharmacother 46, 240–247 (2012).

²Dhillon, S. Tesamorelin: A review of its use in the management of HIV-associated lipodystrophy. Drugs 71, 1071–1091 (2011).

³Fourman, 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).

⁴Wang, Y. & Tomlinson, B. Tesamorelin, a human growth hormone releasing factor analogue. Expert Opin. Investig. Drugs 18, 303–310 (2009).