pharmacokinetic (PK) properties for a previously disclosed class of cyclopropyl-fused indolobenzazepine HCV NS5B polymerase inhibitors are described. These efforts led to the discovery of BMS-961955 as a viable contingency backup to beclabuvir which was recently approved in Japan for the treatment of HCV as part of a three drug, single pill combination marketed as XimencyTM.
描述了先前公开的一类环丙基融合
吲哚苯并氮杂 HCV NS5B 聚合酶
抑制剂的合成、构效关系 (
SAR) 数据以及代谢稳定性和药代动力学 (PK) 特性的进一步优化。这些努力导致发现 BMS-961955 作为贝克拉布韦的可行应急备用方案,贝克拉布韦最近在日本被批准用于治疗 HCV,作为以 Ximency TM销售的三药单丸组合的一部分。