Ensartinib (X-396)

Agent Description

Ensartinib is a small molecule, ALK inhibitor that potently inhibits ALK and most of its alternations (fusions, mutants). It is also a potent EphA2 inhibitor with modest selectivity with respective to other Ephrin isoforms. It is orally bioavailable and supplied in capsules.

Mechanism of Action

Inhibition of ALK whose aberration causes cancers

Classification

ALK inhibitor

Molecular Targets

ALK, TrkA, TrkC, ROS, EphA2, c-MET

Monograph

Ensartinib has shown very good efficacy in ALK positive non-small cell lung cancer (NSCLC) patients who progressed on crizotinib in the Phase 1/2 trial. Currently, it is in Phase 3 trial comparing to crizotinib in ALK positive NSCLC patients.

Studies of Interest

New indications as an ALK inhibitor, EphA2 inhibitor. Combination studies.

Information collaborator would like included in investigator proposals

N/A