Trastuzumab emtanzin
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]
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| Klinički podaci | |
|---|---|
| AHFS/Drugs.com | emtansine.html Monografija |
| Identifikatori | |
| CAS broj | 1018448-65- |
| ATC kod | nije dodeljen |
| DrugBank | DB05773 |
| Hemijski podaci | |
| Formula | C6448H9948N1720O2012S44·(C47H62ClN4O13S)n |
| Mol. masa | 148.5 kDa |
| Farmakokinetički podaci | |
| Poluvreme eliminacije | 4 dana |
| Farmakoinformacioni podaci | |
| Trudnoća | ? |
| Pravni status | |
| Način primene | Intravenozno |
Reference uredi
- ↑ Niculescu-Duvaz I (June 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”. American Medical Association. Arhivirano iz originala na datum 2012-09-28. Pristupljeno 22. 2. 2013.
- ↑ LoRusso PM, Weiss D, Guardino E, Girish S, Sliwkowski MX (October 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. DOI:10.1158/1078-0432.CCR-11-0762. PMID 22003071.
- ↑ Poon, Kirsten Achilles (6. 5. 2010.). „Safety Assessment of Antibody Drug Conjugates”. Drug Development: From Small Molecules to Biologics. NorCal Society of Toxicology 2010 Spring Meeting. Arhivirano iz originala na datum 2014-04-13. Pristupljeno 23. 2. 2013.
- ↑ „Trastuzumab emtansine”. NCI Drug Dictionary. Pristupljeno 23. 2. 2013.
- ↑ "FDA denies accelerated approval of Genentech's trastuzumab-DM1 (T-DM1) BLA for metastatic breast cancer" (Press release). Genentech. 2010-08-27. Retrieved 2013-02-23.
- ↑ Teicher BA, Doroshow JH (November 2012). „The promise of antibody-drug conjugates”. N. Engl. J. Med. 367 (19): 1847–8. DOI:10.1056/NEJMe1211736. PMID 23134386.
- ↑ 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. DOI:10.1093/nar/gkq1126. PMC 3013709. PMID 21059682.
- ↑ David S. Wishart, Craig Knox, An Chi Guo, Dean Cheng, Savita Shrivastava, Dan Tzur, Bijaya Gautam, and Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic Acids Res 36 (Database issue): D901-6. DOI:10.1093/nar/gkm958. PMC 2238889. PMID 18048412.
Literatura uredi
- Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.
- Thomas L. Lemke, David A. Williams, ur. (2007). Foye's Principles of Medicinal Chemistry (6 izd.). Baltimore: Lippincott Willams & Wilkins. ISBN 0-7817-6879-9.
