your speakers for our 2 events

Biography

Edward Kerns is currently consultant on the ADME optimization of clinical candidates in drug discovery at www.discoveryadme.com. He provides guidance on project review, methodology, diagnosis, structure design, due diligence, and training. He was previously Associate Director of Chemical Sciences at Pfizer (formerly Wyeth), where he developed and led the Pharmaceutical Profiling department for compound selection and optimization and collaboration with discovery teams for diagnosis and structure modification for over 10 years. Previously, Ed was Associate Director of Analytical Research at Bristol-Myers Squibb, where he introduced mass spectrometry and LC/MS/MS for bioanalysis and structure elucidation. During 17 years at BMS he led structure elucidation groups and analytical departments and introduced new methodologies for study of drug metabolites, impurities, degradants, licensing candidate due diligence and technology transfer. He provided key support for NDAs of TAXOL™, buspirone, trazodone and nefazodone. He is known for innovating novel assays and strategies. He is co-author of Drug-like Properties: Concepts, Structure Design and Methods a leading book in medicinal chemistry, co-instructor of the ACS Short Course Drug-Like Properties in Drug Discovery, co-author of 85 scientific articles and 3 patents, co-chair of 20 scientific conferences or symposia, and presenter of over 45 invited lectures.

Abstract

Integrating in vitro and in vivo DMPK studies to guide structure optimization in drug discovery

Selection and optimization of lead compounds in drug discovery for quality pharmacokinetics (PK) and safety have become necessary functions in the advancement of excellent clinical candidates.  Consistent strategies for implementing the ADME function are beneficial to the drug discovery project team collaboration and timetable, including the following.  Rapid ADME Profiling of selected physicochemical, metabolic and transporter properties provides due diligence of leads entering lead optimization (LO)  and an overview of key components contributing to PK for analog synthesis during LO.  IVIVC Diagnosis - correlation of in vivo PK results with the in vitro ADME Profile - assists determination of the underlying properties that can be improved to enhance the inadequate PK performance.  Structure Modification Strategies guide enhancement of the PK performance of the chemical series.  Diagnostic ADME Assays in vitro assist determination of less common properties that limit PK performance and biological activity assays.