Challenges in Modern Drug Discovery: A Case Study of Boceprevir, an HCV Protease Inhibitor for the Treatment of Hepatitis C Virus Infection

2008 ◽  
Vol 41 (1) ◽  
pp. 50-59 ◽  
Author(s):  
F. George Njoroge ◽  
Kevin X. Chen ◽  
Neng-Yang Shih ◽  
John J. Piwinski
2007 ◽  
Vol 1 ◽  
pp. 1177391X0700100 ◽  
Author(s):  
K.-C. Cheng ◽  
Walter A. Korfmacher ◽  
Ronald E. White ◽  
F. George Njoroge

Lead optimization using drug metabolism and pharmacokinetics (DMPK) parameters has become one of the primary focuses of research organizations involved in drug discovery in the last decade. Using a combination of rapid in vivo and in vitro DMPK screening procedures on a large array of compounds during the lead optimization process has resulted in development of compounds that have acceptable DMPK properties. In this review, we present a general screening paradigm that is currently being used as part of drug discovery at Schering-Plough and we describe a case study using the Hepatitis C Virus (HCV) protease inhibitor program as an example. By using the DMPK optimization tools, a potent HCV protease inhibitor, SCH 503034, was selected for development as a candidate drug.


2020 ◽  
Vol 63 (23) ◽  
pp. 14740-14760
Author(s):  
Li-Qiang Sun ◽  
Eric Mull ◽  
Stanley D’Andrea ◽  
Barbara Zheng ◽  
Sheldon Hiebert ◽  
...  

2014 ◽  
Vol 23 (5) ◽  
pp. 719-728 ◽  
Author(s):  
Ivan Gentile ◽  
Antonio Riccardo Buonomo ◽  
Federico Borgia ◽  
Emanuela Zappulo ◽  
Giuseppe Castaldo ◽  
...  

2019 ◽  
Vol 70 (1) ◽  
pp. e747-e748 ◽  
Author(s):  
Victor De Ledinghen ◽  
Bureau christophe ◽  
Yuri Sanchez ◽  
Fabrice Ruggeri ◽  
Pierre-Henri Delaage ◽  
...  

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