A phase I/IIa study assessing single and multiple doses of hepatitis C virus (HCV) non-nucleoside polymerase inhibitor IDX375 in healthy and genotype 1 HCV-infected subjects

开始日期2010-06-09

申办/合作机构

Idenix Pharmaceuticals LLC

100 项与 IDX-375 相关的临床结果

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100 项与 IDX-375 相关的转化医学

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100 项与 IDX-375 相关的专利（医药）

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项与 IDX-375 相关的文献（医药）

2017-06-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Discovery of benzophosphadiazine drug candidate IDX375: A novel hepatitis C allosteric NS5B RdRp inhibitor

4区 · 医学

Article

作者: Badaroux, Eric ; Pierra, Claire ; Paparin, Jean-Laurent ; Griffe, Ludovic ; Dukhan, David ; Onidi, Loredana ; Griffon, Jean-François ; Bot, Stéphanie ; Leroy, Frédéric ; Milhau, Julien ; Dousson, Cyril B ; Surleraux, Dominique ; Da Costa, Daniel ; Rosinosky, Elodie ; Convard, Thierry ; Giulia Loi, Anna ; Mascia, Valeria ; Rahali, Rachid ; Sais, Efisio ; Amador, Agnès ; LaColla, Massimiliano ; Seifer, Maria ; Liuzzi, Michel ; Caillet, Catherine ; McCarville, Joe ; Standring, David

Hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent in mammalian cells, and as a consequence is an attractive target for selective inhibition. This paper describes the discovery of a novel family of HCV NS5B non-nucleoside inhibitors inspired by the bioisosterism between sulfonamide and phosphonamide. Systematic structural optimization in this new series led to the identification of IDX375, a potent non-nucleoside inhibitor that is selective for genotypes 1a and 1b. The structure and binding domain of IDX375 were confirmed by X-ray co-crystalisation study.

2012-08-01·Antimicrobial Agents and Chemotherapy2区 · 医学

First-in-Human Study of the Pharmacokinetics and Antiviral Activity of IDX375, a Novel Nonnucleoside Hepatitis C Virus Polymerase Inhibitor

2区 · 医学

Article

作者: van Vliet, A. A. ; Molles, J. ; Pietropaolo, K. ; Temam, M. F. ; van de Wetering de Rooij, J. ; Zhou, X. J. ; de Bruijne, J. ; Mayers, D. ; Sullivan-Bólyai, J. Z. ; Chen, J. ; Reesink, H. W.

ABSTRACT IDX375 is a potent and selective palm-binding nonnucleoside inhibitor of the hepatitis C virus (HCV) genotype 1 polymerase. This first-in-human study evaluated the safety, tolerability, and pharmacokinetics of IDX375 in healthy volunteers, as well as its antiviral activity in HCV-infected patients. IDX375, as a choline salt, was administered for 1 day to 40 healthy male volunteers (25- to 200-mg IDX375-equivalent single ascending doses and a 200-mg twice-daily [BID] dose) and three patients chronically infected with HCV genotype 1 (200 mg BID only). IDX375 was well absorbed and well tolerated by all of the study participants. A single-day 200-mg BID dose resulted in exposure-related anti-HCV activity with maximal 0.5 to 1.1 log 10 reductions in plasma HCV RNA. These observations support further clinical investigations of IDX375.

100 项与 IDX-375 相关的药物交易

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