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Ultra-high throughput determination of CYP450 enzyme inhibition through mass spectrometry

Abstract: This Application Note describes how the BioTrove RapidFire highthroughout mass spectrometry (RF-MS) system interfaced to an Agilent 6410 triple quadrupole mass spectrometer was used for the characterization of the enzymatic reaction of CYP450 3A4/5 enzyme in a preparation of human liver microsomes and for the determination of IC50 curves of potentially inhibiting drug compounds. The major features of this solution are: • Ultra high throughput – mass spectrometry data is obtained at speeds approaching those of fluorescent assays.• Fully compatible with liver microsomes – biologically relevant data is generated, as recommended by the September 2006 FDA DraftGuidance to Industry.• Drug probes screened – the need for fluorogenic substrates is eliminated.• Improved data quality – time-course data is obtained in the time required for end-point analysis by LC-MS.

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