Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety-Reference-Cited by-同舟云学术

Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety

Published:2018-11-02 Issue:23 Volume:61 Page:10700-10708
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Mandal Mihirbaran^ORCID,Mitra Kaushik,Grotz Diane,Lin Xinjie,Palamanda Jairam,Kumari Pramila,Buevich Alexei^ORCID,Caldwell John P.,Chen Xia,Cox Kathleen,Favreau Leonard,Hyde Lynn,Kennedy Matthew E.,Kuvelkar Reshma,Liu Xiaoxiang,Mazzola Robert D.,Parker Eric,Rindgen Diane,Sherer Edward^ORCID,Wang Hongwu,Zhu Zhaoning,Stamford Andrew W.,Cumming Jared N.

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.8b01326

Reference28 articles.

1. Cytochrome P450 enzymes in drug metabolism: Regulation of gene expression, enzyme activities, and impact of genetic variation

2. Drugs as CYP3A Probes, Inducers, and Inhibitors

3. Structural Alert/Reactive Metabolite Concept as Applied in Medicinal Chemistry to Mitigate the Risk of Idiosyncratic Drug Toxicity: A Perspective Based on the Critical Examination of Trends in the Top 200 Drugs Marketed in the United States

4. Mechanism-Based Inactivation (MBI) of Cytochrome P450 Enzymes: Structure–Activity Relationships and Discovery Strategies To Mitigate Drug–Drug Interaction Risks

5. CYP3A Time-Dependent Inhibition Risk Assessment Validated with 400 Reference Drugs

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