Article
LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer.
Oncotarget - 7 Feb 2017
Vakana Eliza, Pratt Susan, Blosser Wayne, Dowless Michele, Simpson Nicholas, Yuan Xiu-Juan, Jaken Susan, Manro Jason, Stephens Jennifer, Zhang Youyan, Huber Lysiane, Peng Sheng-Bin, Stancato Louis F
Abstract excerpt
Activating mutations in the KRAS and BRAF genes, leading to hyperactivation of the RAS/RAF/MAPK oncogenic signaling cascade, are common in patients with colorectal cancer (CRC). While selective BRAF inhibitors are efficacious in BRAFmut melanoma, they have limited efficacy in BRAFmut CRC patients. In a RASmut background, selective BRAF inhibitors are contraindicated due to paradoxical activation of the MAPK...
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