SGMS Meeting 2000

High throughput analysis, purification and profiling strategies in the area of high throughput drug discovery

D.B. Kassel
DuPont Pharmaceuticals, San Diego, CA 92121, USA

An ever increasing number of pharmaceutical, biotechnology and agrochemical industries are adopting high throughput parallel organic synthesis and high throughput biological screening strategies to accelerate their discovery efforts. Concomitant to these activities have been efforts in the analytical and bioanalytical community to accelerate other key components of the discovery process, including high throughput analysis, purification and ADME profiling.

This presentation will review state-of-the-art analytical tools developed in this laboratory as well as review some of the innovations in combinatorial lipary analysis from other laboratories. In particular, this presentation will focus on high throughput LC/MS and SFC/MS for the analysis of compound liparies, high throughput preparative LC/MS and preparative SFC/MS for the purification of compound liparies, parallel LC/MS analysis and purification and strategies implemented in our laboratory for the rapid ADME profiling of compound liparies, as a means for assessing their "drug-ability" to aid in the selection criteria for lead follow up and lead nomination. In particular, a microsomal stability and cytochrome P450 inhibition assay coupled with parallel LC/MS will be presented.