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Dabrafenib mesylate: Serine/threonine-protein kinase B-raf inhibitor oncolytic

机译:达拉非尼甲磺酸盐:丝氨酸/苏氨酸蛋白激酶B-raf抑制剂溶瘤

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摘要

Until recently, treatment options for patients with advanced or metastatic cutaneous melanoma were limited. New targeted agents directed against mutant serine/threonine-protein kinase B-raf, including vemurafenib and dabrafenib (GSK-2118436), have shown promising activity in several clinical trials. Rationally designed clinical studies, especially for patients with BRAF-mutant melanoma, have illuminated the complexity of the mitogen-activated protein (MAP) kinase and PI3K/Akt/mTOR signaling pathways. This review focuses on the preclinical and clinical development process of dabrafenib, a selective B-raf inhibitor.
机译:直到最近,晚期或转移性皮肤黑色素瘤患者的治疗选择仍然有限。针对突变型丝氨酸/苏氨酸蛋白激酶B-raf的新型靶向药物,包括vemurafenib和dabrafenib(GSK-2118436),已在多项临床试验中显示出令人鼓舞的活性。合理设计的临床研究,尤其是针对BRAF突变型黑色素瘤的患者,阐明了促分裂原活化蛋白(MAP)激酶和PI3K / Akt / mTOR信号通路的复杂性。这篇综述的重点是选择性B-raf抑制剂dabrafenib的临床前和临床开发过程。

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