Overcoming Drug Resistance to BRAF Inhibitor

Bull Math Biol. 2020 Jan 14;82(1):8. doi: 10.1007/s11538-019-00691-0.

Abstract

One of the most frequently found mutations in human melanomas is in the B-raf gene, making its protein BRAF a key target for therapy. However, in patients treated with BRAF inhibitor (BRAFi), although the response is very good at first, relapse occurs within 6 months, on the average. In order to overcome this drug resistance to BRAFi, various combinations of BRAFi with other drugs have been explored, and some are being applied clinically, such as a combination of BRAF and MEK inhibitors. Experimental data for melanoma in mice show that under continuous treatment with BRAFi, the pro-cancer MDSCs and chemokine CCL2 initially decrease but eventually increase to above their original level, while the anticancer T cells continuously decrease. In this paper, we develop a mathematical model that explains these experimental results. The model is used to explore the efficacy of combinations of BRAFi with anti-CCL2, anti-PD-1 and anti-CTLA-4, with the aim of eliminating or reducing drug resistance to BRAFi.

Keywords: BRAF inhibitor resistance; Checkpoint inhibitors; Metastatic melanoma cancer.

MeSH terms

  • Animals
  • Chemokine CCL2 / antagonists & inhibitors
  • Computer Simulation
  • Drug Resistance, Neoplasm* / genetics
  • Drug Resistance, Neoplasm* / immunology
  • Humans
  • Immune Checkpoint Inhibitors / administration & dosage
  • Mathematical Concepts
  • Melanoma / drug therapy*
  • Melanoma / immunology
  • Melanoma / pathology
  • Melanoma, Experimental / drug therapy
  • Melanoma, Experimental / immunology
  • Melanoma, Experimental / pathology
  • Mice
  • Models, Biological*
  • Mutation
  • Programmed Cell Death 1 Receptor / antagonists & inhibitors
  • Proto-Oncogene Proteins B-raf / antagonists & inhibitors*
  • Proto-Oncogene Proteins B-raf / genetics

Substances

  • Ccl2 protein, mouse
  • Chemokine CCL2
  • Immune Checkpoint Inhibitors
  • Pdcd1 protein, mouse
  • Programmed Cell Death 1 Receptor
  • BRAF protein, human
  • Braf protein, mouse
  • Proto-Oncogene Proteins B-raf