High throughput P450 inhibition screens in early drug discovery

Drug Discov Today. 2005 Nov 1;10(21):1443-50. doi: 10.1016/S1359-6446(05)03580-4.

Abstract

This review of high throughput (HT) P450 inhibition technologies and their impact on early drug discovery finds the field at a mature stage. The relationship between P450 inhibition and drug-drug interactions is well understood. A wide variety of P450 inhibition detection technologies are readily available off-the-shelf, but what seems still to be missing is a general agreement on how much weight one should give to the various types of early discovery HT P450 inhibition data. Method-dependent potency differences are a cause of concern, and to resolve this issue the authors advocate calibration of the HT methods with a large set of marketed drugs.

Publication types

  • Review

MeSH terms

  • Calibration
  • Cytochrome P-450 Enzyme Inhibitors*
  • Drug Design*
  • Drug Evaluation, Preclinical / instrumentation*
  • Drug Evaluation, Preclinical / methods*
  • Drug Interactions

Substances

  • Cytochrome P-450 Enzyme Inhibitors