Binimetinib
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Binimetinib is a medication used to treat metastatic melanoma with specific mutations.
Binimetinib is a medication used to treat metastatic melanoma with specific mutations.
Binimetinib, noncompetitive with ATP, binds reversibly to and inhibits the activity of mitogen-activated extracellular signal-regulated kinase (MEK) 1 and 2. The inhibition of MEK1/2 prevents the activation of MEK1/2-dependent effector proteins and transcription factors, resulting in the inhibition of growth factor-mediated cell signaling such as the downstream extracellular signal-related kinase (ERK) pathway. This may lead to the inhibition of tumor cell proliferation and an inhibition in the production of various inflammatory cytokines including interleukin-1, -6, and tumor necrosis factor. MEK1/2 are themselves threonine and tyrosine kinases that possess a dual specificity. They subsequently contribute critically to the activation of the RAS/RAF/MEK/ERK pathway and are typically upregulated in a number of different tumor cell types.
⑴与encorafenib联合，用于治疗经检测到的BRAF V600E或V600K突变的不可切除或转移性黑色素瘤患者。 ⑵与安可非尼联合，用于治疗具有BRAFV600E突变的转移性癌症（非小细胞肺癌）的成年患者。
每项发明一条，涵盖美国、欧洲、PCT 与中国的同族专利。
