Chemistry:Tesamorelin
Tesamorelin (INN; trade name Egrifta SV) 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]
Mechanism of action
Tesamorelin is the N-terminally modified compound based on 44 amino acids sequence of human GHRH.[2] 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.[3] 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.[4]
Contraindication
Tesamorelin therapy may cause glucose intolerance and increase the risk of type 2-diabetes, so it is contraindicated in pregnancy.[5] Another reason for contraindication in category X is the fact it may harm the fetus before birth, and in earlier trimesters. It is also contraindicated in patients affected by hypothalamic-pituitary axis disruption due to pituitary gland tumor, head irradiation and hypopituitarism.[6]
Adverse effects
Injection site erythema, peripheral edema, injection site pruritus and diarrhea.[7]With frequent usage, may cause joint, arm, and leg pains, as a result of the depletion of body fat mass upon use. [8]Tesamorelin can also cause a greater risk for lipoatrophy, due to its allowance of prolonged exposure to thymadine NTRI.[9]
See also
- List of growth hormone secretagogues
References
- ↑ "FDA Application Chemistry Review". http://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022505Orig1s000ChemR.pdf.
- ↑ "Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy". Drugs 71 (8): 1071–1091. May 2011. doi:10.2165/11202240-000000000-00000. PMID 21668043.
- ↑ "Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue". Basic & Clinical Pharmacology & Toxicology 100 (1): 49–58. January 2007. doi:10.1111/j.1742-7843.2007.00008.x. PMID 17214611.
- ↑ "Recombinant human growth hormone: rationale for use in the treatment of HIV-associated lipodystrophy". BioDrugs 22 (2): 101–112. 2008. doi:10.2165/00063030-200822020-00003. PMID 18345707.
- ↑ "Tesamorelin: A hope for ART-induced lipodystrophy". Journal of Pharmacy & Bioallied Sciences 3 (2): 319–320. April 2011. doi:10.4103/0975-7406.80763. PMID 21687371.
- ↑ "Review of Selected NMEs 2011" (in en). Auburn: Health Information Designs, Inc. https://www.uspharmacist.com/article/review-of-selected-nmes-2011.
- ↑ "Effects of tesamorelin, a growth hormone-releasing factor, in HIV-infected patients with abdominal fat accumulation: a randomized placebo-controlled trial with a safety extension". Journal of Acquired Immune Deficiency Syndromes 53 (3): 311–322. March 2010. doi:10.1097/qai.0b013e3181cbdaff. PMID 20101189.
- ↑ "Tesamorelin - an overview | ScienceDirect Topics". https://www.sciencedirect.com/topics/medicine-and-dentistry/tesamorelin.
- ↑ Martínez, Esteban (2011-06-01). "Disorders of fat partitioning in treated HIV–infection". Best Practice & Research Clinical Endocrinology & Metabolism. Endocrine Disease in HIV Infection 25 (3): 415–427. doi:10.1016/j.beem.2010.10.019. ISSN 1521-690X. https://www.sciencedirect.com/science/article/pii/S1521690X10001466.
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