title: BRAF inhibitors: the current and the future.
abstract: The introduction of BRAF inhibitors (BRAFi), vemurafenib and dabrafenib, revolutionized BRAFV600-mutated metastatic melanoma treatment with improved response rate and overall survival compared to standard chemotherapy. However, the mechanism related cutaneous toxicity remains a concern. In addition, intrinsic and acquired resistance remain the key challenges in BRAFi therapy. Extensive efforts to elucidate the mechanisms have led to an improved understanding of disease biology and resulted in exploration of multiple new therapeutic options. While the future looks bright with multiple new therapeutic strategies in exploration and possible new generations of BRAFi, there are questions remaining to be answered to enable more efficient use of BRAFi in cancer therapy.
authors.affiliation: Roche Innovation Center New York, 430 E. 29th Street, New York, NY 10016, United States. Electronic address: Weijiang.zhang@roche.com.
authors.forename: Weijiang
authors.initials: W
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D005544:Forecasting; D006801:Humans; D007093:Imidazoles / Q000008:administration & dosage; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology; D010091:Oximes / Q000008:administration & dosage; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage*; D048493:Proto-Oncogene Proteins B-raf / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D007093:Imidazoles; D010091:Oximes; D047428:Protein Kinase Inhibitors; C482119:BRAF protein, human; D048493:Proto-Oncogene Proteins B-raf; C561627:dabrafenib