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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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Related Experiment Video

Updated: Dec 20, 2025

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
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Does Crizotinib Auto-Inhibit CYP3A in vivo?

Abigail R Bland1, Nensi Shrestha1, Rhonda J Rosengren1

  • 1Department of Pharmacology & Toxicology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.

Pharmacology
|May 28, 2020
PubMed
Summary

Crizotinib, a lung cancer drug, does not inhibit cytochrome P450 3A (CYP3A) activity in vivo, contrary to in vitro findings. This study found no alteration in CYP3A activity or expression in mice treated with crizotinib.

Area of Science:

  • Pharmacology
  • Oncology
  • Drug Metabolism

Background:

Keywords:
Anaplastic lymphoma kinaseCancerCrizotinibCytochrome P450 3APharmacokinetics

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  • Crizotinib is a targeted therapy for anaplastic lymphoma kinase-positive non-small cell lung cancer.
  • In vitro studies suggest crizotinib may inhibit cytochrome P450 3A (CYP3A) activity, potentially affecting its pharmacokinetics.
  • Understanding crizotinib's in vivo drug metabolism interactions is crucial for patient safety and treatment efficacy.