抗黑色素瘤新药cobimetinib

A new anti-melanoma drug:cobimetinib

黑色素瘤是由黑色素细胞引发的恶性肿瘤。2015年11月10日,美国FDA批准cobimetinib（商品名：Cotellic ）联合vemurafenib（商品名：Zelboraf ）治疗伴有B-RAF^V600E或B-RAF^V600K突变的不可切除或转移性黑色素瘤。vemurafenib和cobimetinib分别作为B-RAF抑制剂和MEK抑制剂,多靶点阻断细胞通路,降低了不良发应发生率,但该方案对于B-RAF（RAF亚型B）野生型黑色素瘤的治疗无明显效果。本文对cobimetinib作用机制、药效学、药动学、临床试验及不良反应进行综述,为临床后续研究和治疗提供参考。

Melanoma is a type of malignant tumor that develops from the melanocytes. November 10 th,2015,FDA approved cobimetinib（ Cotellic ,GDC-0973,XL518） for the treatment of people with B-RAF^V600 Eor B-RAF^V600 Kmutation-positive unresectable or metastatic melanoma in combination with vemurafenib（ Zelboraf ,PLX4032）. Cobimetinib and vemurafenib are respectively used as B-RAF inhibitor and MEK inhibitor,but they are not used to treat melanoma with a normal B-RAF gene. In this paper,we review the mechanism of action,pharmacodynamics,pharmacokinetics,clinical trials and adverse reactions of cobimetinib,thus provide a reference for the advanced research and clinical treatment.