Session Chairs:
Kirk McMillan, Exelixis, Inc., USA
David M. Stresser, BD Biosciences, USA
Early application of ADME/toxicology assays in support of lead validation/optimization has become a critical component of small molecule drug discovery in both pharma and biotech organizations. Implementation of in vitro assays for profiling metabolic stability, cytochrome P450 inhibition, cell (or membrane) permeability and physicochemical properties (solubility, lipophilicity, pKa, etc.), as well as assays for identifying hepatoxicity, reactive metabolites, HERG channel interaction and genotoxicity have become routine determinants of a candidate's "drugability". These profiling assays in conjunction with extensive in vivo DMPK/toxicology studies have resulted in the selection of better clinical candidates and reduced compound attrition. This session will address new technologies, current practices and future directions for this important aspect of preclinical drug discovery and development