ROS1-TKI

ROS1 tyrosine kinase inhibitors (ROS1-TKIs) are a class of small molecule targeted therapies designed to inhibit the activity of the ROS1 fusion protein, an oncogenic driver found in approximately 1% to 2% of non-small cell lung cancers (NSCLCs) and other solid tumors. By binding to the kinase domain of the rearranged ROS1 receptor tyrosine kinase, these inhibitors block downstream signaling pathways (such as MAPK/ERK, PI3K/AKT, and JAK/STAT) that promote tumor cell survival and proliferation. First-generation ROS1-TKIs, such as crizotinib and entrectinib, have significantly improved patient outcomes but are limited by the development of resistance mutations (e.g., G2032R solvent front mutation) and poor blood-brain barrier penetration. Next-generation ROS1-TKIs, including repotrectinib, taletrectinib, and zidesamtinib (NVL-520), have been developed to overcome these resistance mechanisms and provide superior central nervous system (CNS) activity.

Other names

ROS1 tyrosine kinase inhibitorROS-1 tyrosine kinase inhibitorROS 1 tyrosine kinase inhibitorROS1-TKIsROS-1-TKIsROS 1-TKIs