repotrectinib (Pending FDA Approval)

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Dosing & Uses

Non-small Cell Lung Cancer

Pending FDA approval for patients with ROS1-positive locally advanced or metastatic non–small cell lung cancer (NSCLC)

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Pharmacology

Mechanism of Action

Orally available inhibitor of multiple kinases, including receptor tyrosine kinase anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), neurotrophic tyrosine receptor kinase (NTRK) types 1, 2 and 3, proto-oncogene SRC, and focal adhesion kinase (FAK)

Binds to and inhibits wild-type, point mutants and fusion proteins of ALK, ROS1, NTRK1-3, SRC, FAK and, to a lesser extent, other kinases

Inhibition of these kinases disrupts downstream signaling pathways and inhibits cell growth of tumors in which these kinases are overexpressed, rearranged, or mutated

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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.