February 11 - 13, 2004, ADMET-1 Conference, San Diego, CA, USA

Strategies and tactics for achieving potency and exposure

Rob DeWitte

Abstract

Finding a new drug is even more complicated than validating a target and optimizing the potency of the lead compound. Until the availability of larger samples (>~100mg) and animal data, the medicinal chemist has little input about the aspects of his/her molecules that influence exposure at the site of action. This talk explores the physical basis of many of the in vivo barriers between dose and exposure and provides a set of rational working hypotheses that may assist drug discovery projects to bring forward promising candidates more quickly.