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P1003
Identification of Cytochrome P450 Mechanism-Based Inhibitors Using In vitro High-Throughput Assay
Presenter Weimin Tang, Johnson & Johnson Pharmaceutical, USA
Additional Authors: Zhengyin Yan & Norman Huebert
Mechanism-based CYP inhibition (MBI) has been proposed to be associated with serious adverse drug effects such as drug-drug interactions and idiosyncratic toxicity. The potential of new chemical entities (NCEs) to inhibit human CYPs is usually assessed during the pre-clinical stage, since MBI could potentially contribute to the high cost resulting from development failures. This presentation will discuss a high-throughput assay that can be routinely utilized to rapidly identify potential MBI at the early stage of discovery. Application of this approach in the early discovery stage has successfully helped several projects in selecting lead compounds with more favorable ADMET profiles.