The broad-spectrum receptor tyrosine kinase inhibitor dovitinib suppresses growth of BRAF-mutant melanoma cells in combination with other signaling pathway inhibitors

Pigment Cell Melanoma Res. 2015 Jul;28(4):417-30. doi: 10.1111/pcmr.12376. Epub 2015 May 6.

Abstract

BRAF inhibitors have revolutionized treatment of mutant BRAF metastatic melanomas. However, resistance develops rapidly following BRAF inhibitor treatment. We have found that BRAF-mutant melanoma cell lines are more sensitive than wild-type BRAF cells to the small molecule tyrosine kinase inhibitor dovitinib. Sensitivity is associated with inhibition of a series of known dovitinib targets. Dovitinib in combination with several agents inhibits growth more effectively than either agent alone. These combinations inhibit BRAF-mutant melanoma and colorectal carcinoma cell lines, including cell lines with intrinsic or selected BRAF inhibitor resistance. Hence, combinations of dovitinib with second agents are potentially effective therapies for BRAF-mutant melanomas, regardless of their sensitivity to BRAF inhibitors.

Keywords: MEK inhibitor; combination therapy; dovitinib; mutant BRAF; vemurafenib resistance.

Publication types

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

MeSH terms

  • Animals
  • Benzimidazoles / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Resistance, Neoplasm / drug effects
  • Drug Synergism
  • Humans
  • Indoles / pharmacology
  • Male
  • Melanoma / enzymology
  • Melanoma / genetics*
  • Melanoma / pathology*
  • Melanoma, Cutaneous Malignant
  • Mice, Nude
  • Mutation / genetics*
  • Neoplasm Proteins / metabolism
  • Protein Kinase Inhibitors / pharmacology*
  • Quinolones / pharmacology*
  • Signal Transduction / drug effects*
  • Skin Neoplasms
  • Small Molecule Libraries / pharmacology
  • Sulfonamides / pharmacology
  • Vemurafenib

Substances

  • 4-amino-5-fluoro-3-(5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl)quinolin-2(1H)-one
  • AZD 6244
  • Benzimidazoles
  • Indoles
  • Neoplasm Proteins
  • Protein Kinase Inhibitors
  • Quinolones
  • Small Molecule Libraries
  • Sulfonamides
  • Vemurafenib