Significance of BRAF kinase inhibitors for melanoma treatment: From bench to bedside

Taku Fujimura, Yasuhiro Fujisawa, Yumi Kambayashi, Setsuya Aiba

Research output: Contribution to journalReview articlepeer-review

18 Citations (Scopus)


According to clinical trials, BRAF kinase inhibitors in combination with MEK kinase inhibitors are among the most promising chemotherapy regimens for the treatment of advanced BRAF-mutant melanoma, though the rate of BRAF mutation gene-bearing cutaneous melanoma is limited, especially in the Asian population. In addition, drug resistance sometimes abrogates the persistent efficacy of combined therapy with BRAF and MEK inhibitors. Therefore, recent pre-clinical study-based clinical trials have attempted to identify optimal drugs (e.g., immune checkpoint inhibitors or histone deacetylase (HDAC) inhibitors) that improve the anti-melanoma effects of BRAF and MEK inhibitors. In addition, the development of novel protocols to avoid resistance of BRAF inhibitors is another purpose of recent pre-clinical and early clinical trials. This review focuses on pre-clinical studies and early to phase III clinical trials to discuss the development of combined therapy based on BRAF inhibitors for BRAF-mutant advanced melanoma, as well as mechanisms of resistance to BRAF inhibitors.

Original languageEnglish
Article number1342
Issue number9
Publication statusPublished - 2019 Sept


  • BRAF inhibitors
  • BRAF resistance
  • BRAF-mutant metastatic melanoma
  • HDAC inhibitors
  • Immune checkpoint inhibitors
  • MEK inhibitors

ASJC Scopus subject areas

  • Oncology
  • Cancer Research


Dive into the research topics of 'Significance of BRAF kinase inhibitors for melanoma treatment: From bench to bedside'. Together they form a unique fingerprint.

Cite this