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Significance of BRAF Kinase Inhibitors for Melanoma Treatment: From Bench to Bedside

1
Department of Dermatology, Tohoku University Graduate School of Medicine, Sendai 980-8574, Japan
2
Department of Dermatology, University of Tsukuba, Tsukuba 305-8576, Japan
*
Author to whom correspondence should be addressed.
Cancers 2019, 11(9), 1342; https://doi.org/10.3390/cancers11091342
Received: 29 August 2019 / Accepted: 9 September 2019 / Published: 11 September 2019
(This article belongs to the Special Issue Oncogenic Forms of BRAF as Cancer Driver Genes)
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. View Full-Text
Keywords: BRAF-mutant metastatic melanoma; BRAF inhibitors; MEK inhibitors; immune checkpoint inhibitors; HDAC inhibitors; BRAF resistance BRAF-mutant metastatic melanoma; BRAF inhibitors; MEK inhibitors; immune checkpoint inhibitors; HDAC inhibitors; BRAF resistance
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Fujimura, T.; Fujisawa, Y.; Kambayashi, Y.; Aiba, S. Significance of BRAF Kinase Inhibitors for Melanoma Treatment: From Bench to Bedside. Cancers 2019, 11, 1342.

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