Tesamorelin

Tesamorelin (INN) (trade name Egrifta) 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.[2]

Tesamorelin
Clinical data
Trade namesEgrifta
AHFS/Drugs.comMultum Consumer Information
MedlinePlusa611035
Pregnancy
category
  • US: X (Contraindicated)
    Routes of
    administration    		Subcutaneous injection
    ATC code
    Legal status
    Legal status
    • US: ℞-only
    • In general: ℞ (Prescription only)
    Pharmacokinetic data
    Bioavailability≤4%[1]
    MetabolismProteolysis
    Elimination half-life26–38 min
    ExcretionRenal/proteolysis
    Identifiers
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    KEGG
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC221H366N72O67S
    Molar mass5135.86 g·mol−1
    3D model (JSmol)

    Mechanism of action

    Tesamorelin is the N-terminally modified compound based on 44 amino acids sequence of human GHRH.[3] 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.[4] 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 mainly because of the combination 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]

    Contraindication

    Tesamorelin therapy may cause glucose intolerance and increase the risk of type 2-diabetes, so it is contraindicated in pregnancy.[6] It is also contraindicated in pregnancy (category X) because it may cause harm to fetus. It also causes disruption of hypothalamic-pituitary axis due to pituitary gland tumor, head irradiation and hypopituitarism.[7]

    Adverse effects

    Injection site erythema, peripheral edema, injection site pruritis and diarrhea.[8]

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    See also

    References
    1. "Egrifta (tesamorelin for injection) for Subcutaneous Use. U.S. Full Prescribing Information" (PDF). EMD Serono, Inc. Retrieved 9 April 2016.
    2. "FDA Application Chemistry Review" (PDF).
    3. Dhillon S (May 2011). "Tesamorelin: a review of its use in the management of HIV-associated lipodystrophy". Drugs. 71 (8): 1071–91. doi:10.2165/11202240-000000000-00000. PMID 21668043.
    4. Ferdinandi ES, Brazeau P, High K, Procter B, Fennell S, Dubreuil P (January 2007). "Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue". Basic & Clinical Pharmacology & Toxicology. 100 (1): 49–58. doi:10.1111/j.1742-7843.2007.00008.x. PMID 17214611.
    5. Benedini S, Terruzzi I, Lazzarin A, Luzi L (2008). "Recombinant human growth hormone: rationale for use in the treatment of HIV-associated lipodystrophy". BioDrugs. 22 (2): 101–12. doi:10.2165/00063030-200822020-00003. PMID 18345707. S2CID 34340539.
    6. Patel A, Gandhi H, Upaganlawar A (April 2011). "Tesamorelin: A hope for ART-induced lipodystrophy". Journal of Pharmacy & Bioallied Sciences. 3 (2): 319–20. doi:10.4103/0975-7406.80763. PMC 3103937. PMID 21687371.
    7. DeRuiter J, Holston PL. "Review of Selected NMEs 2011". www.uspharmacist.com. Auburn: Health Information Designs, Inc. Retrieved 2019-06-22.
    8. Falutz J, Potvin D, Mamputu JC, Assaad H, Zoltowska M, Michaud SE, et al. (March 2010). "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): 311–22. doi:10.1097/qai.0b013e3181cbdaff. PMID 20101189.
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