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US 6,830,897 B2Granted
High throughput screen for reducing drug candidate attrition
AssigneePfizer Inc.
InventorsMichael J. Avery, Weichao G. Chen, Hassan G. Fouda
Life of this patent
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Abstract
This invention provides a high throughput method for identifying drug candidates which produce reactive metabolites that contribute to toxicity of the drug product.
Claims8
A high throughput discovery screen for determining the potential toxicity of candidate drugs comprising the steps of:
- (a) incubating the candidate drugs, in a first multi-well plate, with a microsomal enzyme metabolizing system wherein said drugs may form reactive electrophilic metabolites;
- (b) permitting said electrophilic metabolites to react with glutathione in order to form glutathione conjugates;
- (c) processing the samples, containing glutathione-drug cpnjugates, via an automated solid phase extraction system, in order to prepare a further multi-well plate from which the conjugates can be extracted for automated HPLC;
- (d) conducting HPLC column runs on said extracts in order to generate HPLC eluates containing said conjugates;
- (e) introducing said eluates, at source, into a triple quadrapole mass spectrometer, and (f) detecting said conjugates with tandem (MS—MS) mass spectrometry.
2 more elements
Dependencies are inferred from the claim text.