zidesamtinib

Zidesamtinib is an orally available, selective small molecule inhibitor of the receptor tyrosine kinase c-ros oncogene 1 (ROS1). It is designed to target and inhibit wild-type ROS1 as well as point mutants and fusion proteins of ROS1, including resistance mutations such as G2032R, S1986Y/F, L2026M, and D2033N. Zidesamtinib demonstrates high potency against a variety of ROS1 alterations and is brain-penetrant. Its mechanism disrupts downstream signaling pathways critical for tumor cell growth in cancers where ROS1 is overexpressed or mutated. The drug has shown durable responses in heavily pretreated patients with ROS1-positive non-small cell lung cancer (NSCLC) and other solid tumors. Zidesamtinib was granted FDA breakthrough therapy designation in February 2024 for patients with metastatic NSCLC previously treated with two or more ROS1 TKIs[1][5][6][7].

Other names

2739829-00-4