Drug Overview
Ensartinib is a second-generation anaplastic lymphoma kinase (ALK) inhibitor developed by Xcovery. In approximately 3–5% of all non-small cell lung cancer (NSCLC) patients, abnormal ALK configuration leads to the production of proteins that promote and maintain the malignant behavior of cancer cells. In particular, inversions in chromosome 2 cause ALK to fuse to echinoderm microtubule-associated protein-like 4. This activates the ALK kinase domain and downstream signaling pathways responsible for excess cancer cell proliferation. Early-phase trials of second-generation ALK inhibitors such as ensartinib have demonstrated their ability to cross the blood-brain barrier and act on tumors in the central nervous system, a common site for distant metastases in ALK-positive NSCLC.
Ensartinib is a second-generation anaplastic lymphoma kinase (ALK) inhibitor developed by Xcovery. In approximately 3–5% of all non-small cell lung cancer (NSCLC) patients, abnormal ALK configuration leads to the production of proteins that promote and maintain the malignant behavior of cancer cells. In particular, inversions in chromosome 2 cause ALK to fuse to echinoderm microtubule-associated protein-like 4. This activates the ALK kinase domain and downstream signaling pathways responsible for excess cancer cell proliferation. Early-phase trials of second-generation ALK inhibitors such as ensartinib have demonstrated their ability to cross the blood-brain barrier and act on tumors in the central nervous system, a common site for distant metastases in ALK-positive NSCLC.
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