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Nexavar emerged from our collaboration with Bayer focused on identifying and developing inhibitors of inappropriate growth signaling in the RAS pathway. Nexavar is the first compound to target both the RAF/MEK/ERK signaling pathway to inhibit cell proliferation and the VEGFR-2/PDGFR-ß signaling cascade to inhibit tumor angiogenesis. RAF kinase is a specific enzyme in the RAS pathway. Mutations in the RAS gene occur in approximately 20 percent of all human cancers, including 90 percent of pancreatic cancer, 50 percent of colon cancer and 30 percent of non-small cell lung cancer. Recently, researchers found that a specific RAF kinase, BRAF, is mutated in two-thirds of melanomas and a low percentage of colorectal and other solid tumors. VEGFR-2 and PDGFR-ß are receptors of vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF), which play key roles in angiogenesis.
Nexavar is approved in the U.S. and E.U. for patients with advanced kidney cancer. In addition, due to positive interim results, we recently halted a Phase 3 study early in advanced liver cancer. Other pivotal trials in metastatic melanoma and in non-small cell lung cancer are being conducted. Nexavar is also being evaluated in single-agent Phase 2 clinical trials in lung, breast, and other cancers, along with several Phase 1/2 clinical trials studying the agent in combination with a range of standard chemotherapeutics and other anticancer agents.
Nexavar emerged from our collaboration with Bayer focused on identifying and developing inhibitors of inappropriate growth signaling in the RAS pathway. Nexavar is the first compound to target both the RAF/MEK/ERK signaling pathway to inhibit cell proliferation and the VEGFR-2/PDGFR-ß signaling cascade to inhibit tumor angiogenesis. RAF kinase is a specific enzyme in the RAS pathway. Mutations in the RAS gene occur in approximately 20 percent of all human cancers, including 90 percent of pancreatic cancer, 50 percent of colon cancer and 30 percent of non-small cell lung cancer. Recently, researchers found that a specific RAF kinase, BRAF, is mutated in two-thirds of melanomas and a low percentage of colorectal and other solid tumors. VEGFR-2 and PDGFR-ß are receptors of vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF), which play key roles in angiogenesis.
Nexavar is approved in the U.S. and E.U. for patients with advanced kidney cancer. In addition, due to positive interim results, we recently halted a Phase 3 study early in advanced liver cancer. Other pivotal trials in metastatic melanoma and in non-small cell lung cancer are being conducted. Nexavar is also being evaluated in single-agent Phase 2 clinical trials in lung, breast, and other cancers, along with several Phase 1/2 clinical trials studying the agent in combination with a range of standard chemotherapeutics and other anticancer agents.
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