Trastuzumab emtanzin
 | |
| Klinički podaci | |
|---|---|
| Drugs.com | emtansine.html Monografija |
| Način primene | Intravenozno |
| Farmakokinetički podaci | |
| Poluvreme eliminacije | 4 dana |
| Identifikatori | |
| CAS broj | 1018448-65-  |
| ATC kod | None |
| DrugBank | DB05773 |
| Hemijski podaci | |
| Formula | C6448H9948N1720O2012S44·(C47H62ClN4O13S)n |
| Molarna masa | 148.5 kDa |
Trastuzumab emtanzin (INN;[1][2], Kadcyla, Ado-trastuzumab emtansin, Trastuzumab-DM1, T-DM1) je konjugat antela i leka koji se sastoji monklonalnog antitela trastuzumaba (Herceptina) vezanog za citotoksični agens mertanzin (DM1).[3][4][5][6] Sam trastuzumab zasutavlja rast ćelija raka vezivanjem za HER2/neu receptor, dok mertanzin ulazi u ćelije i uništva ih vezivanjem za tubulin.[7] Popto je antitelo specifčno za HER2 koji je prekomerno izražen na ćelijama raka, konjugat specifično isporućuje toksin ćelijama tumora.[8][9][10][11]
Reference
[uredi | uredi izvor]- ^ Niculescu-Duvaz I (2010). „Trastuzumab emtansine, an antibody-drug conjugate for the treatment of HER2+ metastatic breast cancer”. Curr. Opin. Mol. Ther. 12 (3): 350—60. PMID 20521224.
- ^ USAN Council (2009). „Statement On A Nonproprietary Name Adopted By The Usan Council: Trastuzumab Emtansine” (PDF). American Medical Association. Архивирано из оригинала (PDF) 28. 09. 2012. г. Приступљено 22. 2. 2013.
- ^ LoRusso PM, Weiss D, Guardino E, Girish S, Sliwkowski MX (2011). „Trastuzumab emtansine: a unique antibody-drug conjugate in development for human epidermal growth factor receptor 2-positive cancer”. Clin. Cancer Res. 17 (20): 6437—47. PMID 22003071. doi:10.1158/1078-0432.CCR-11-0762.
- ^ Poon, Kirsten Achilles (6. 5. 2010). Safety Assessment of Antibody Drug Conjugates (PDF). Drug Development: From Small Molecules to Biologics. NorCal Society of Toxicology 2010 Spring Meeting. Архивирано из оригинала (PDF) 13. 04. 2014. г. Приступљено 23. 2. 2013.
- ^ „Trastuzumab emtansine”. NCI Drug Dictionary. Приступљено 23. 2. 2013.
- ^ „FDA denies accelerated approval of Genentech's trastuzumab-DM1 (T-DM1) BLA for metastatic breast cancer” (Саопштење). Genentech. 27. 8. 2010. Приступљено 23. 2. 2013.
- ^ Teicher BA, Doroshow JH (2012). „The promise of antibody-drug conjugates”. N. Engl. J. Med. 367 (19): 1847—8. PMID 23134386. doi:10.1056/NEJMe1211736.
- ^ Lewis Phillips GD, Li G, Dugger DL, Crocker LM, Parsons KL, Mai E, Blattler WA, Lambert JM, Chari RV, Lutz RJ, Wong WL, Jacobson FS, Koeppen H, Schwall RH, Kenkare-Mitra SR, Spencer SD, Sliwkowski M
- ^ X: Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate. Cancer Res. 2008 Nov 15;68(22):9280-90. doi: 10.1158/0008-5472.CAN-08-1776. PMID 19010901
- ^ Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035—41. PMC 3013709
. PMID 21059682. doi:10.1093/nar/gkq1126.
- ^ David S. Wishart; Craig Knox; An Chi Guo; Dean Cheng; Savita Shrivastava; Dan Tzur; Bijaya Gautam; Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic acids research. 36 (Database issue): D901—6. PMC 2238889 . PMID 18048412. doi:10.1093/nar/gkm958.
Literatura
[uredi | uredi izvor]- Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
- Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.
