核苷单磷酸前药作为抗丙型肝炎病毒药物的研究进展。
Advances in nucleoside monophosphate prodrugs as anti-HCV agents.
作者信息
Bobeck Drew R, Schinazi Raymond F, Coats Steven J
机构信息
RFS Pharma LLC, Tucker, GA, USA.
出版信息
Antivir Ther. 2010;15(7):935-50. doi: 10.3851/IMP1667.
Abstract
Nucleoside monophosphate prodrugs that are eventually bioconverted to the active nucleoside triphosphate (NTP) offer the potential to deliver increased intracellular NTP levels and/or organ-specific NTP enhancement. There are several classes of monophosphate prodrugs that have been applied to HCV drug discovery, and some of these approaches are currently being evaluated in humans. This review discusses recent advances in monophosphate prodrug approaches to improve oral absorption, stability and pharmacokinetic profile, including their advantages and potential pitfalls.
摘要
最终生物转化为活性核苷三磷酸（NTP）的核苷单磷酸前药，具有提高细胞内NTP水平和/或器官特异性NTP增强的潜力。有几类单磷酸前药已应用于丙型肝炎病毒（HCV）药物研发，其中一些方法目前正在人体中进行评估。本综述讨论了单磷酸前药方法在改善口服吸收、稳定性和药代动力学方面的最新进展，包括其优点和潜在问题。
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