【摘 要】
：
ADME-tox study has become an essential part of drug discovery research,aiming to build the necessary druggabilities ("drug-like" properties) into drug candidates with higher successful probabilities i
【机 构】
：
MetabQuest Research and Consulting China
【出 处】
：
中国上海第七届国际新药发明科技年会
论文部分内容阅读
ADME-tox study has become an essential part of drug discovery research,aiming to build the necessary druggabilities ("drug-like" properties) into drug candidates with higher successful probabilities in preclinical and clinical studies.In-depth structure-druggability (drug-like property) relationship (SDR) studies can accelerate lead optimization chemistry programs in many ways:1.Dial out soft spot quickly for lead modification; 2.Detect reactive/toxic metabolite and provide chemical strategy to minimize tox risk of the lead series; 3.Provide me-better approaches for follow-on program; 4.Identify animal species for tox studies of lead series; 5.Identify the correct in vitro system that predicts in vivo behaviors of lead compound; 6.Track druggability behind structural progression of lead series; 7.Address PK-PD discrepancies in animal studies; 8.Design and evaluate prodrug approaches for lead series; etc.This seminar is based on case studies from different lead optimization programs at different stages demonstrating the assisting role of SDR studies and how to do in-depth SDR studies to accelerate lead optimization chemistry programs.
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