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Ulixertinib is a novel oral small molecule inhibitor of extracellular signal-regulated kinases 1 and 2 (ERK1/2), which are key components of the mitogen-activated protein kinase (MAPK) signaling pathway. By selectively inhibiting ERK1/2—the terminal node in the MAPK cascade—ulixertinib blocks signals that promote cancer cell growth and survival. This mechanism is particularly relevant for cancers with mutations in upstream components of the MAPK pathway such as BRAF or RAS. Ulixertinib has demonstrated clinical activity across a range of tumor types including glioma, histiocytosis, melanoma (including those with atypical BRAF mutations), pancreatic cancer, and colorectal cancer. It is being developed primarily for patients who have progressed on standard therapies or have tumors harboring specific genetic alterations for which there are limited treatment options.
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