Lofitinib is an oral inhibitor of various kinases, including receptor tyrosine kinase asexual lymphoma kinase (ALK), c-ros tumor gene 1 (ROS1), neurotrophic tyrosine receptor kinase (NTRK) types 1, 2, and 3, oncogene SRC, and focal adhesion kinase (FAK), with potential anti-tumor activity. After oral administration, rapatinib binds to wild-type, point mutants, and fusion proteins of ALK, ROS1, NTRK1-3, SRC, and FAK and inhibits them to a lesser extent, while inhibiting other kinases. Inhibiting these kinases can lead to the disruption of downstream signaling pathways and inhibit the cell growth of tumors with overexpression, rearrangement, or mutation of these kinases.