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Tepotinib reverses ABCB1-mediated multidrug resistance in cancer cells

Zhuo-Xun Wu1, Qiu-Xu Teng1, Chao-Yun Cai1

  • 1Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, USA.

Biochemical Pharmacology
|May 13, 2019
PubMed

Insights

Tepotinib effectively reverses multidrug resistance (MDR) mediated by ABCB1 transporters by inhibiting their efflux activity. This suggests tepotinib as a potential co-treatment to enhance chemotherapy effectiveness.

Area of Science:

  • Pharmacology
  • Oncology
  • Molecular Biology

Background:

  • Multidrug resistance (MDR) mediated by ABCB1 transporters limits chemotherapy efficacy.
  • Inhibiting ABCB1 is crucial for maintaining effective intracellular drug concentrations.

Purpose of the Study:

  • To investigate tepotinib's potential to antagonize ABC transporter-mediated MDR.
  • To elucidate the mechanisms by which tepotinib affects ABCB1 activity.

Main Methods:

  • Cell-based assays to assess MDR reversal.
  • ATPase assays to measure transporter activity.
  • Western blotting and subcellular localization studies.
  • Molecular docking analysis.

Main Results:

  • Tepotinib significantly reversed ABCB1-mediated MDR, but not MDR mediated by ABCG2 or ABCC1.
  • Tepotinib inhibited ABCB1 efflux activity and ATPase activity in a concentration-dependent manner.
  • Protein expression and subcellular localization of ABCB1 remained unchanged.
  • Docking analysis suggested tepotinib binds to the ABCB1 drug-binding site.

Conclusions:

  • Tepotinib antagonizes ABCB1 transporter activity, offering a strategy to overcome MDR.
  • Co-administration of tepotinib with chemotherapeutics may improve treatment outcomes in cancer patients.
Keywords:
ABCB1ATP-binding cassette (ABC) transporterMultidrug resistance (MDR)TepotinibTyrosine kinase inhibitor

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