Brigatinib

Brigitanib acts as a tyrosine kinase inhibitor with activity against multiple kinases including ALK, ROS1, insulin-like growth factor 1 receptor and against EGFR deletions and point mutations. It acts by inhibiting ALK phosphorylation and the activation of downstream signaling proteins. It is a highly potent and selective inhibitor of anaplastic lymphoma kinase (ALK). Blocks ALK activity and reduces growth in neuroblastoma cells, mouse xenograft, and Drosophila model systems harboring constitutively active ALK variants. It is potentially useful for the treatment of non-small cell lung cancer (NSCLC). Can be used in combination with anti-EGFR drugs to overcome EGFR mutation resistance.