Grazoprevir
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Surname | Grazoprevir | |||||||||||||||
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Molecular formula | C 38 H 50 N 6 O 9 S | |||||||||||||||
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Molar mass | 766.90 g mol −1 | |||||||||||||||
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As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . |
Grazoprevir (synonym MK-5172 ) is an antiviral drug from the quinoxaline group that is used to treat infections with the hepatitis C virus .
properties
Grazoprevir is a second generation inhibitor and inhibits the viral protease consisting of the heterodimer NS3 / NS4A . It is effective against most HCV subtypes that are resistant to first generation HCV protease inhibitors .
Interactions
Grazoprevir is removed from the bloodstream by the proteins SLCO1B1 and SLCO1B3 . Drugs that inhibit these proteins increase the concentration of grazeprovir in the blood plasma , such as rifampicin , ciclosporin , the HIV drugs atazanavir , darunavir , lopinavir , saquinavir , tipranavir , cobicistat . It is broken down in the liver by cytochrome P450 3A4 . Drugs that induce CYP3A4 lower the concentration of grazoprevir, such as efavirenz , carbamazepine or St. John's wort , whereas CYP3A4 inhibitors increase the concentration.
Trade names
Grazoprevir is sold in combination with Elbasvir under the trade name Zepatier by MSD Sharp & Dohme .
Individual evidence
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ↑ S. Harper, JA McCauley, MT Rudd, M. Ferrara, M. DiFilippo, B. Crescenzi, U. Koch, A. Petrocchi, MK Holloway, JW Butcher, JJ Romano, KJ Bush, KF Gilbert, CJ McIntyre, KT Nguyen, E. Nizi, SS Carroll, SW Ludmerer, C. Burlein, JM DiMuzio, DJ Graham, CM McHale, MW Stahlhut, DB Olsen, E. Monteagudo, S. Cianetti, C. Giuliano, V. Pucci, N. Trainor , CM Fandozzi, M. Rowley, PJ Coleman, JP Vacca, V. Summa, NJ Liverton: Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3 / 4a Protease Inhibitor. In: ACS medicinal chemistry letters. Volume 3, number 4, April 2012, pp. 332-336, doi: 10.1021 / ml300017p , PMID 24900473 , PMC 4025840 (free full text).
- ↑ I. Gentile, AR Buonomo, F. Borgia, E. Zappulo, G. Castaldo, G. Borgia: MK-5172: a second-generation protease inhibitor for the treatment of hepatitis C virus infection. In: Expert opinion on investigational drugs. Volume 23, number 5, May 2014, pp. 719-728, doi: 10.1517 / 13543784.2014.902049 , PMID 24666106 .