Bosutinib reduces the efficacy of Dasatinib in triple-negative breast cancer cell lines

Anticancer Res. 2014 Apr;34(4):1629-35.

Abstract

Background: Triple-negative breast cancer (TNBC) is an aggressive sub-type of breast cancer. Dasatinib and bosutinib are FDA-approved Src/Abl kinase inhibitor drugs. Dasatinib potently inhibits the proliferation of many TNBC cell lines.

Materials and methods: The cell viability/proliferation for a panel of 4 TNBC cell lines was measured by detection of cellular ATP levels and cell numbers were directly determined by automated cell counting.

Results: Bosutinib (≤1 μM) had little to no inhibitory activity on cell viability/proliferation, while dasatinib-alone generated potent IC50 values of <100 nM. Combination treatment of cells with both dasatinib and bosutinib resulted in reduced efficacy of dasatinib in all four cell lines, with two of them displaying a dramatic loss of efficacy. Direct cell counting confirmed that bosutinib enhanced cell proliferation in the presence of dasatinib.

Conclusion: Bosutinib potently reduced the in vitro anti-proliferative efficacy of dasatinib in TNBC cell lines. We, hereby, report on a novel drug-induced loss in dasatinib sensitivity.

Keywords: Bosutinib; breast cancer; dasatinib.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aniline Compounds / pharmacology*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Dasatinib
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Female
  • Humans
  • Nitriles / pharmacology*
  • Protein Kinase Inhibitors / pharmacology*
  • Pyrimidines / pharmacology*
  • Quinolines / pharmacology*
  • Thiazoles / pharmacology*
  • Triple Negative Breast Neoplasms* / drug therapy

Substances

  • Aniline Compounds
  • Antineoplastic Agents
  • Nitriles
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Quinolines
  • Thiazoles
  • bosutinib
  • Dasatinib