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ensartinib
- Development stage
- Approved
- Lead developer
- Xcovery Holdings
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Ensartinib is an orally administered small molecule kinase inhibitor primarily used for the treatment of adults with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer (NSCLC) who have not previously received an ALK inhibitor. It works by selectively inhibiting ALK and its variants, thereby blocking signaling pathways that drive cancer cell proliferation and survival. Ensartinib also inhibits other kinases such as EphA2, TrkA, TrkC, ROS1, and c-MET to varying degrees. The drug is supplied as ensartinib hydrochloride in capsule form and was approved for medical use in the United States in December 2024.
- Brand names
- Ensacove
- Other names
- ensartinib hydrochloride
02
Targets
CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)ABCG2 (Breast cancer resistance protein)EPHA2 (Ephrin type-A receptor 2)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)MET (Mesenchymal-epithelial transition factor receptor)CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)NTRK3 (Tropomyosin receptor kinase C)NTRK1 (Tropomyosin-related receptor kinase A)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)
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