High throughput physicochemical profiling for drug discovery.
The drug development bottlenecks of attrition and development time are being addressed by acquiring a profile of the candidate's physicochemical and physiological properties during early discovery phases. This information assists selection and optimization of pharmaceutical properties in parallel with activity. High throughput methods to measure the properties: solubility, permeability, lipophilicity, pKa, stability and integrity are described and compared in this article. The underlying discovery requirements, needs and application strategies are discussed.
Kerns
E H
EH
Wyeth-Ayerst Research, Princeton, New Jersey 08543-8000, USA. kernse@war.wyeth.com
D000818:Animals; D001702:Biopharmaceutics; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006801:Humans; D013678:Technology, Pharmaceutical / Q000295:instrumentation / Q000379:methods*