Tesamorelin

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Tesamorelin
Tesamorelin.svg
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 g·mol−1
3D model (JSmol)

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]

Mechanism of action[edit]

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 release 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 the body fat mass are the lipolysis followed by reduction in triglycerides level.[5]

Contraindication[edit]

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[edit]

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

See also[edit]

References[edit]

  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, Sohita (2011-05-01). "Tesamorelin". Drugs. 71 (8): 1071–1091. doi:10.2165/11202240-000000000-00000. ISSN 1179-1950.
  4. ^ Ferdinandi, Eckhardt S.; Brazeau, Paul; High, Kim; Procter, Bryan; Fennell, Stephen; Dubreuil, Pascal (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. ISSN 1742-7835.
  5. ^ Benedini, Stefano; Terruzzi, Ileana; Lazzarin, Adriano; Luzi, Livio (2008). "Recombinant Human Growth Hormone". BioDrugs. 22 (2): 101–112. doi:10.2165/00063030-200822020-00003. ISSN 1173-8804.
  6. ^ Gandhi, Hardik; Upaganlawar, Aman; Patel, Akash (2011). "Tesamorelin: A hope for ART-induced lipodystrophy". Journal of Pharmacy and Bioallied Sciences. 3 (2): 319. doi:10.4103/0975-7406.80763. ISSN 0975-7406. PMC 3103937.
  7. ^ Alabama, Jack DeRuiter, Ph Professor, Pharmacal Sciences Harrison School of Pharmacy, Auburn University Auburn, Alabama Pamela L. Holston, RPh, BS, BA Health Information Designs, Inc Auburn. "Review of Selected NMEs 2011". www.uspharmacist.com. Retrieved 2019-06-22.
  8. ^ Falutz, Julian; Potvin, Diane; Mamputu, Jean-Claude; Assaad, Hani; Zoltowska, Monika; Michaud, Sophie-Elise; Berger, Daniel; Somero, Michael; Moyle, Graeme (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". JAIDS Journal of Acquired Immune Deficiency Syndromes. 53 (3): 311–322. doi:10.1097/qai.0b013e3181cbdaff. ISSN 1525-4135.