Applications of high-throughput ADME in drug discovery.
Assessment of physicochemical and pharmacological properties is now conducted at very early stages of drug discovery for the purpose of accelerating the conversion of hits and leads into qualified development candidates. In particular, in vitro absorption, distribution, metabolism and elimination (ADME) assays and in vivo drug metabolism pharmacokinetic (DMPK) studies are being conducted throughout the discovery process, from hit generation through to lead optimization, with the goal of reducing the attrition rate of these potential drug candidates as they progress through development. Because the continuing trend in drug discovery has been to access ADME information earlier and earlier in the discovery process, the need has arisen within the analytical community to introduce faster and better analytical methods to enhance the 'developability' of drug leads. Strategies for streamlined ADME assessment of drug candidates in discovery and pre-clinical development are presented within.
Kassel
Daniel B
DB
Analytical Discovery & Development, Syrrx Inc., 10410 Science Center Drive, San Diego, California 92121, USA. daniel.kassel@syrrx.com
D000042:Absorption; D002626:Chemistry, Pharmaceutical / Q000295:instrumentation / Q000379:methods*; D003627:Data Interpretation, Statistical; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004347:Drug Interactions; D004355:Drug Stability; D007091:Image Processing, Computer-Assisted; D004364:Pharmaceutical Preparations / Q000032:analysis / Q000737:chemistry / Q000378:metabolism; D010599:Pharmacokinetics
D004364:Pharmaceutical Preparations