Higher-throughput screening with human cytochromes P450

Recent progress has been made in increasing the throughput of measurements of cytochrome P450-mediated metabolism of drug candidates. This review focuses on two innovations: (i) the reduction of the number of samples for HPLC-based analyses by simultaneous measurement multiple analytes in a single injection (N in one analysis) and (ii) screens for the inhibition of cytochrome P450-mediated metabolism (a mechanism for drug-drug interactions) using fluorometric assays. Both of these innovations substantially increase the throughput and decrease the resources needed for conducting these routine preclinical studies.