3C样蛋白酶抑制剂博福特韦的研发实践和策略  

Research and Development Practiceand Strategy of 3C-like Protease Inhibitor Bofutrelvir

作　　者：谢东 胡敏 姚成 XIE Dong;HU Min;YAO Cheng(Frontier Biotechnologies Inc,Nanjing 210012,China)

机构地区：[1]前沿生物药业(南京)股份有限公司,江苏南京210012

出　　处：《药学进展》2023年第7期494-498,共5页Progress in Pharmaceutical Sciences

基　　金：国家重点研发计划公共安全风险防控与应急技术装备(No.2021YFC0864900);江苏省工业和信息产业转型升级专项资金、南京市科技计划项目-新型冠状病毒传染应急防治(No.ZX20200007)。

摘　　要：博福特韦是一种靶向新冠病毒3C样蛋白酶的小分子抑制剂,具有注射和雾化吸入两种给药形式,可单药给药,不需要联用肝药酶抑制剂。目前数据显示,博福特韦具有广谱抗冠状病毒活性、高耐药屏障、呼吸道和肺部中的药物浓度比血药浓度更高,在动物模型中可显著抑制肺部和脑部病毒复制等特点。简介了博福特韦的特点及其临床开发经验,旨在为抗COVID-19药物的开发提供思路与参考。Bofutrelvir is a small-molecule inhibitor targeting the SARS-CoV-23C-like protease.It can be administered by injection or atomized inhalation and can be administered as a single drug without the need for a combination of liver drug enzyme inhibitors.Current data show that bofutrelvir has broad-spectrum anti-coronavirus activity,high resistance barrier,higher drug concentration in respiratory tract and lung than in blood,and can significantly inhibit viral replication in lung and brain in animal models.This article briefly introduces the characteristics of bofutrelvir and its clinical development experience,aiming to provide ideas and references for the development of anti-CoVID-19drugs.

关 键 词：博福特韦 3C样蛋白酶抑制剂 新冠病毒感染 耐药屏障 注射制剂 雾化吸入制剂 

分 类 号：R978.7[医药卫生—药品]