APG-2449

APG-2449 is a novel, orally active, small molecule multi-targeted tyrosine kinase inhibitor that selectively inhibits focal adhesion kinase (FAK), anaplastic lymphoma kinase (ALK), and ROS1 kinases with nanomolar potency. It is classified as a third-generation ALK/ROS1 tyrosine kinase inhibitor and also acts as a FAK inhibitor. APG-2449 has demonstrated potent antitumor activity in preclinical models of non-small cell lung cancer (NSCLC) and ovarian cancer, both as monotherapy and in combination with other agents. The drug is being developed primarily for the treatment of advanced solid tumors, including NSCLC resistant to second-generation ALK inhibitors, treatment-naïve ALK-positive NSCLC, ovarian cancer, esophageal cancer, and vaginal cancer. Clinical trials have shown manageable safety profiles and promising efficacy in patients with TKI-naïve or TKI-resistant NSCLC[1][3][4][5][6][7][8].