Ensartinib

Definition

An orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK), with potential antineoplastic activity. Upon oral administration, ensartinib binds to and inhibits ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. In addition, ensartinib inhibits various other kinases, including the receptor tyrosine kinase c-Met (hepatocyte growth factor receptor; HGFR; MET) and the receptor tyrosine kinase C-ros oncogene 1 (ROS1). ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK is not expressed in healthy adult human tissue but ALK dysregulation and gene rearrangements are associated with a series of tumors; ALK mutations are associated with acquired resistance to small molecule tyrosine kinase inhibitors.

Also known as 6-Amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]- N-{4-[(3R,5S)-3,5-dimethylpiperazine- 1-carbonyl]phenyl}pyridazine-3-carboxamide, ENSARTINIB, X 396, X-396, X396 — per NCIT

Also identified as

• NCIT NCIT:C102754 per NCIT
• UNII SMA5ZS5B22 per RXNORM

Indications

Organ Effects

1 entry above is marked DERIVED: Atlas Médico inferred it by combining two sourced claims, and no source asserts this link directly. Treat it as a navigation aid, not as a clinical statement.