Tesamorelin
Also called Egrifta
Part of the metabolic pathway of Tesamorelin. See the timeline on the metabolic highway.
Overview
Tesamorelin (INN; trade names Egrifta, Egrifta SV and Egrifta WR) is a synthetic form of growth-hormone-releasing hormone (GHRH) which is used in the treatment of HIV-associated lipodystrophy, approved initially in 2010. It is produced and developed by Theratechnologies, Inc. of Canada. The drug is a synthetic peptide consisting of all 44 amino acids of human GHRH with the addition of a trans-3-hexenoic acid group.[1] WP
Risks and side effects
Adverse effects
Injection site erythema, peripheral edema, injection site pruritus and diarrhea. With frequent usage, may cause joint, arm, and leg pains, as a result of the depletion of body fat mass upon use. Tesamorelin can also cause a greater risk for lipoatrophy, due to its allowance of prolonged exposure to thymadine NTRI.[2]
Pharmacology
Mechanism of action
Tesamorelin is the N-terminally modified compound based on 44 amino acids sequence of human GHRH. This modified synthetic form is more potent and stable than the natural peptide. It is also more resistant to cleavage by the dipeptidyl aminopeptidase than human GHRH. It stimulates the synthesis and release of endogenous GH, with an increase in level of insulin-like growth factor (IGF-1). The released GH then binds with the receptors present on various body organs and regulates the body composition. This regulation is due to the mixing of anabolic and lipolytic mechanisms. However, it has been found that the main mechanisms by which Tesamorelin reduces body fat mass are lipolysis followed by reduction in triglycerides level.[5]
Chemistry
- Formula
- C221H366N72O67S PC
- CAS number
- 218949-48-5 PC
- Molar mass (g/mol)
- 5136 PC
- IUPAC name (computed by PubChem)
- (4S)
- 4- [[2- [[(2S) - 5- amino- 2- [[(2S) - 5- amino- 2- [[(2S) - 2- [[(2S) - 2- [[(2S) - 2- [[(2S, 3S) - 2- [[(2S) - 2- [[(2S) - 5- amino- 2- [[(2S) - 2- [[(2S) - 2- [[(2S) - 6- amino- 2- [[(2S) - 2- [[(2S) - 2- [[(2S) - 2- [[(2S) - 2- [[(2S) - 5- amino- 2- [[2- [[(2S) - 2- [[(2S) - 2- [[(2S) - 6- amino- 2- [[(2S) - 2- [[(2S) - 2- [[(2S) - 2- [[(2S) - 4- amino- 2- [[(2S, 3R) - 2- [[(2S) - 2- [[(2S, 3S) - 2- [[(2S) - 2- [[(2S) - 3- carboxy- 2- [[(2S) - 2- [[(2S) - 2- [[(E) - hex- 3- enoyl] amino] - 3- (4- hydroxyphenyl) propanoyl] amino] propanoyl] amino] propanoyl] amino] propanoyl] amino] - 3- methylpentanoyl] amino] - 3- phenylpropanoyl] amino] - 3- hydroxybutanoyl] amino] - 4- oxobutanoyl] amino] - 3- hydroxypropanoyl] amino] - 3- (4- hydroxyphenyl) propanoyl] amino] - 5- carbamimidamidopentanoyl] amino] hexanoyl] amino] - 3- methylbutanoyl] amino] - 4- methylpentanoyl] amino] acetyl] amino] - 5- oxopentanoyl] amino] - 4- methylpentanoyl] amino] - 3- hydroxypropanoyl] amino] propanoyl] amino] - 5- carbamimidamidopentanoyl] amino] hexanoyl] amino] - 4- methylpentanoyl] amino] - 4- methylpentanoyl] amino] - 5- oxopentanoyl] amino] - 3- carboxypropanoyl] amino] - 3- methylpentanoyl] amino] - 4- methylsulfanylbutanoyl] amino] - 3- hydroxypropanoyl] amino] - 5- carbamimidamidopentanoyl] amino] - 5- oxopentanoyl] amino] - 5- oxopentanoyl] amino] acetyl] amino] - 5- [[(2S) - 1- [[(2S) - 4- amino- 1- [[(2S) - 5-