SC15: METHODOLOGIES FOR OPTIMIZING DRUG CLEARANCE AND DRUG-DRUG INTERACTIONS

WEDNESDAY, APRIL 15 | 6:30 - 9:30 PM (DINNER PROVIDED)

This short course will focus on concepts that will help us understand how drug clearance and drug-drug interactions (DDI) can impact decisions in drug discovery and development. Topics will include drug metabolism, CYP regulation, the role of bioactivation and how they all affect lead optimization. Common assays and methodologies for predicting clearance and drug-drug interactions will be discussed. Those scientists involved in medicinal chemistry, pharmacology and drug metabolism will benefit from this overview.

Topics to be Covered:

  • Drug metabolism enzymes and common reactions
  • Applications of drug metabolism in lead optimization
  • In vitro methods for detecting and characterizing and bioactivation and soft-spot metabolites
  • Common in vitro assays and methodologies for predicting metabolic clearance
  • CYP regulation and induction
  • Methodologies for predicting drug-drug interactions
  • Discovery lead optimization: a case study

Instructors:

Zhengyin_YanZhengyin Yan, PhD, Principal Scientist, Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc.

Zhengyin Yan is currently leading the in vitro DMPK group to support small molecule drug discovery at Genentech. Previously, he had been responsible for in vitro ADME support for nearly 17 years at Johnson & Johnson Pharmaceutical Research & Discovery in Spring House, PA. His main scientific interest includes in vitro assay development, drug metabolism, and ADME-guided lead optimization in drug discovery.

Donglu Zhang, PhD, Principal Scientist, Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc.

Donglu Zhang received a PhD in Organic Chemistry from University of Utah. His current studies focus on soft-spot metabolite identification to support drug designs and to discovery ADCs. He previously worked for Bristol-Myers Squibb and ARIAD Pharmaceuticals. He edited two books ‘Drug metabolism in drug design and development’, and ‘ADME-enabling technologies in drug design and development’. The mass defect filter (MDF) methodologies he co-invented have been widely used in high resolution mass spectrometry for metabolite identification.

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