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grazoprevir
Grazoprevir (MK-5172) is an experimental drug for the treatment of hepatitis C. It is being developed by Merck and is currently in Phase III trials, following promising results in Phase II when used in combination with the NS5A replication complex inhibitor elbasvir, either with or without ribavirin.〔Lawitz E, Gane E, Pearlman B, Tam E, Ghesquiere W, Guyader D, Alric L, Bronowicki JP, Lester L, Sievert W, Ghalib R, Balart L, Sund F, Lagging M, Dutko F, Shaughnessy M, Hwang P, Howe AY, Wahl J, Robertson M, Barr E, Haber B. Efficacy and safety of 12 weeks versus 18 weeks of treatment with grazoprevir (MK-5172) and elbasvir (MK-8742) with or without ribavirin for hepatitis C virus genotype 1 infection in previously untreated patients with cirrhosis and patients with previous null response with or without cirrhosis (C-WORTHY): a randomised, open-label phase 2 trial. ''Lancet''. 2015;385(9973):1075-86. doi: 10.1016/S0140-6736(14)61795-5. PMID 25467591〕
Grazoprevir is a second generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets.〔Harper S, McCauley JA, Rudd MT, Ferrara M, DiFilippo M, Crescenzi B, Koch U, Petrocchi A, Holloway MK, Butcher JW, Romano JJ, Bush KJ, Gilbert KF, McIntyre CJ, Nguyen KT, Nizi E, Carroll SS, Ludmerer SW, Burlein C, DiMuzio JM, Graham DJ, McHale CM, Stahlhut MW, Olsen DB, Monteagudo E, Cianetti S, Giuliano C, Pucci V, Trainor N, Fandozzi CM, Rowley M, Coleman PJ, Vacca JP, Summa V, Liverton NJ. Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor. ''ACS Med Chem Lett''. 2012;3(4):332-6. doi: 10.1021/ml300017p. PMID 24900473〕 It has good activity against a range of HCV genotype variants, including some that are resistant to most currently used antiviral medications.〔Summa V, Ludmerer SW, McCauley JA, Fandozzi C, Burlein C, Claudio G, Coleman PJ, Dimuzio JM, Ferrara M, Di Filippo M, Gates AT, Graham DJ, Harper S, Hazuda DJ, Huang Q, McHale C, Monteagudo E, Pucci V, Rowley M, Rudd MT, Soriano A, Stahlhut MW, Vacca JP, Olsen DB, Liverton NJ, Carroll SS. MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants. ''Antimicrob Agents Chemother''. 2012;56(8):4161-7. doi: 10.1128/AAC.00324-12. PMID 22615282〕〔Gentile I, Buonomo AR, Borgia F, Zappulo E, Castaldo G, Borgia G. MK-5172 : a second-generation protease inhibitor for the treatment of hepatitis C virus infection. ''Expert Opinion on Investigational Drugs''. 2014;23(5):719-28. doi: 10.1517/13543784.2014.902049. PMID 24666106〕
==References==
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