Class/mechanism, from the NCI Drug Dictionary: An orally bioavailable inhibitor of the tyrosine kinases tropomyosin receptor kinases (Trk) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK), with potential antineoplastic activity. Upon administration, entrectinib binds to and inhibits TrkA, TrkB, TrkC, ROS1 and ALK. Inhibition of these kinases may result in a disruption of TrkA-, TrkB-, TrkC-, ROS1-, and ALK-mediated signaling. This leads to an induction of apoptosis and an inhibition of tumor cell proliferation in tumor cells that express these kinases.
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Diseases for which it is used
History of changes in FDA indication
- 8/15/2019: Granted accelerated approval for adults and pediatric patients 12 years of age and older with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory standard therapy. (Based on ALKA, STARTRK-1, and STARTRK-2)
- 8/15/2019: Approved for adults with metastatic non-small cell lung cancer (NSCLC) whose tumors are ROS1-positive. (Based on ALKA, STARTRK-1, and STARTRK-2)
Patient Drug Information
Also known as
- Code name: RXDX-101
- Brand name: Rozlytrek