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Investigational agents in metastatic basal cell carcinoma: focus on vismodegib

机译:转移性基底细胞癌的研究药物:集中于vismodegib

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Abstract: Vismodegib (GDC-0449, 2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide, Erivedge?) is a novel first-in-human, first-in class, orally bioavailable Hedgehog pathway signaling inhibitor of the G-protein coupled receptor-like protein smoothened (SMO) which was approved in the United States on January 2012. This signaling pathway is involved in the carcinogenesis of several types of tumor, as exemplified by basal cell carcinoma. This review focuses on the role of the Hedgehog pathway in the pathogenesis of basal cell carcinoma, the pharmacology and the clinical activity of vismodegib, as well as a brief summary of investigational agents in development targeting this pathway.
机译:摘要:Vismodegib(GDC-0449,2-氯-N-(4-氯-3-(吡啶-2-基)苯基)-4-(甲磺酰基)苯甲酰胺,Erivedge?)是一种新型的人类首创产品, G-蛋白偶联受体样蛋白平滑剂(SMO)的口服生物利用性刺猬信号通路抑制剂的首创,于2012年1月在美国获得批准。该信号通路涉及多种类型肿瘤的致癌作用,如基底细胞癌所示。这篇综述着重于刺猬通路在基底细胞癌的发病机理中的作用,vismodegib的药理作用和临床活性,以及​​针对该通路的研究药物的简要概述。

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