IC50-based approaches as an alternative method for assessment of time-dependent inhibition of CYP3A4. (Q43129481)

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19 January 2020

title

IC50-based approaches as an alternative method for assessment of time-dependent inhibition of CYP3A4 (English)

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19 January 2020

2

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19 January 2020

author name string

Howard J Burt

series ordinal

1

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19 January 2020

J Brian Houston

series ordinal

3

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19 January 2020

language of work or name

English

0 references

publication date

1 May 2010

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19 January 2020

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19 January 2020

volume

40

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19 January 2020

issue

5

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19 January 2020

page(s)

331-343

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Automated assessment of time-dependent inhibition of human cytochrome P450 enzymes using liquid chromatography-tandem mass spectrometry analysis

19 January 2020

cites work

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An examination of IC50 and IC50-shift experiments in assessing time-dependent inhibition of CYP3A4, CYP2D6 and CYP2C9 in human liver microsomes.

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In vivo CYP3A4 heteroactivation is a possible mechanism for the drug interaction between felbamate and carbamazepine

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Mechanism-based inactivation of CYP3A by HIV protease inhibitors

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Maximal inhibition of intestinal first-pass metabolism as a pragmatic indicator of intestinal contribution to the drug-drug interactions for CYP3A4 cleared drugs.

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Grapefruit juice-drug interaction studies as a method to assess the extent of intestinal availability: utility and limitations.

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A critical evaluation of the experimental design of studies of mechanism based enzyme inhibition, with implications for in vitro-in vivo extrapolation

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Mechanism-based inhibition of cytochrome P450 enzymes: an evaluation of early decision making in vitro approaches and drug-drug interaction prediction methods

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Drug interaction studies: study design, data analysis, and implications for dosing and labeling

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Database analyses for the prediction of in vivo drug-drug interactions from in vitro data

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Prediction of the in vivo interaction between midazolam and macrolides based on in vitro studies using human liver microsomes

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Impact of mechanism-based enzyme inactivation on inhibitor potency: implications for rational drug discovery

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The utility of in vitro cytochrome P450 inhibition data in the prediction of drug-drug interactions

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Some suggestions for measuring predictive performance

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Evaluation of recombinant cytochrome P450 enzymes as an in vitro system for metabolic clearance predictions

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Mechanism-based inactivation of human cytochrome P450 enzymes: strategies for diagnosis and drug-drug interaction risk assessment

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