Overview of Small Molecule Drug Discovery and a Case Study in HBV
Speaker
Wei Zhu
Medicinal Chemistry at Roche Innovation Center Shanghai
Time
Venue
Online
Tencent
Abstract
This talk will give you an overview of small molecule drug discovery, spanning target assessment, hit identification, hit to lead, lead optimization, and clinical candidate selection. To illustrate this process, a case study will be presented on the discovery of core protein assembly modulators (CpAM) for the treatment of hepatitis B virus infection, which features ligand-protein interaction understanding via photoaffinity labelling and co-crystallization, structure and medicinal chemistry knowledge based compound optimization and PKPD (pharmacokinetics and pharmacodynamics) elucidation. This work leads to the discovery of a best in class HBV CpAM with desired liver enrichment, excellent anti-HBV activity and safety profiles, which is currently in phase II clinical trial.
Bio
Dr. Wei Zhu is currently Head of Medicinal Chemistry at Roche Innovation Center Shanghai. He obtained his Ph.D. in 2004 from Shanghai Institute of Organic Chemistry (China) under the supervision of Prof. Dawei Ma. From 2004 to 2009, he pursued postdoc studies at European Institute of Chemistry & Biology (France) with Prof. Léon Ghosez and University of Pittsburg (USA) with Prof. Dennis Curran. He joined Roche in 2009 as a scientist. Since then, he has been working on and leading several programs spanning the disease areas of oncology, virology and immunology, and successfully delivered two molecules into clinic. He is corresponding authors of many papers/book chapters, inventors of >40 patents, frequently invited speakers on multiple domestic/international forums, and invited reviewers for renowned medicinal chemistry journals and PhD theses.
2004年上海有机所马大为院士组博士毕业（硕博连读）。此后5年分别于欧洲化学与生物学研究所 Prof. Léon Ghosez组以及美国匹兹堡大学Prof. Dennis Curran组从事博士后工作。2009年回国加入罗氏研发中国有限公司从事抗病毒，炎症以及肿瘤创新药研发至今。历任药物化学部高级科学家，首席科学家，总监，直到现任药物化学部负责人。在罗氏13年的工作中，曾领导多个项目从靶标验证，苗头化合物发现，先导化合物确定，优化直到临床开发。其中抗乙肝新药RG7907现已在多个国家成功进入临床二期。作为项目负责人，申请了近40篇专利，在JMC发表多篇原创工作，并受邀在多个国际会议上做报告以及撰写药物化学专著。
