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Brigatinib + binimetinib is an investigational **oral combination therapy consisting of brigatinib, an anaplastic lymphoma kinase (ALK) inhibitor, and binimetinib, a selective inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2)**. Brigatinib blocks ALK-mediated and mutant epidermal growth factor receptor (EGFR) signaling, inhibiting tumor cell proliferation and survival in ALK-positive cancers. Binimetinib targets MEK1/2 to interrupt the RAS/RAF/MEK/ERK signaling cascade and reduce tumor cell proliferation. The combination is under investigation for unresectable or metastatic non-small cell lung cancer (NSCLC), especially for ALK-positive or resistant cases, aiming to address resistance mechanisms to ALK inhibition.
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