Entrectinib is an indazole derivative substituted with [4-(4-methylpiperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)benzoyl]amino at position 3 and 3,5-difluorobenzyl at position 5. It is a potent inhibitor of TRKA, TRKB, TRKC, ROS1, and ALK (IC50: 0.1–1.7 nM) and is used to treat NTRK, ROS1, and ALK gene fusion-positive solid tumors. It functions as an antineoplastic agent, a receptor protein-tyrosine kinase inhibitor (EC 2.7.10.1), an antibacterial agent, and an apoptosis inducer. It is classified as a difluorobenzene, an indazole, a benzamide, an N-methylpiperazine, an oxane, a secondary amino compound, and a secondary carboxamide.
