达布拉芬尼
曲美替尼
威罗菲尼
医学
黑色素瘤
转移性黑色素瘤
MEK抑制剂
癌症研究
肿瘤科
化疗
内科学
MAPK/ERK通路
激酶
生物
细胞生物学
作者
Mark M. Awad,Ryan J. Sullivan
标识
DOI:10.1586/17512433.2015.974556
摘要
Oncogenic BRAF mutations are present in approximately 40–50% of patients with metastatic melanoma. Targeting BRAF mutations with either small molecule inhibitors of BRAF or one of the downstream mediators of oncogenic BRAF – MEK – is associated with improved outcomes compared with chemotherapy and has led to the US FDA approval of two BRAF inhibitors – vemurafenib and dabrafenib – and the MEK inhibitor trametinib. Further, the combination of dabrafenib and trametinib is well tolerated and associated with higher responses and improved survival compared with single-agent BRAF inhibitors.
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