Cambridge Healthtech Institute’s 2nd Annual

Lead Optimization for Drug Metabolism & Safety
( 药物代谢及安全性提升的先导化合物优化 )

Tools and Strategies for Predicting, Evaluating and Building Safety into Drug Design



The more chemists know about how the structure of a compound can possibly impact its drug-like properties, the faster they can optimize it for drug development. Lead compounds in drug discovery need to be optimized for both efficacy and safety. Unfortunately, some of the adverse events related to drug metabolism, clearance, and drug-drug interactions (DDI) do not surface until much later in drug development. This unique one-day symposium on Lead Optimization for Drug Metabolism & Safety will bring together experts from chemistry, ADME, DMPK and pharmacology to talk about some of the factors that must be considered early in lead optimization, particularly for addressing safety concerns. The symposium will cover some important concepts related to drug metabolism, biotransformation, drug transport, drug-drug interactions and more, using relevant case studies and recent research findings.

Coverage will include, but is not limited to:

  • Impact of SAR on ADMET properties: looking beyond the Rule of Five
  • Drug metabolism and role of reactive drug metabolites
  • Drug transporters, drug clearance and drug-drug interactions
  • Insights on biotransformation and tissue concentrations
  • New assays and bioanalytical technologies to optimize leads
  • Early prediction of human dosing and compound safety
  • ADME for new drug modalities: ADCs, bispecifics, macrocyclics and more
  • Computational drug design to improve compound safety
  • Leveraging in silico tools and machine learning for ADMET predictions

* 活动内容有可能不事先告知作更动及调整。