Nuvalent’s lead compound, NVL-520, is an oral, brain-penetrant, TRK-sparing, and potential best-in-class ROS1 kinase inhibitor that recently entered Ph. II of the ARROS-1 trial (NCT05118789) in patients with advanced ROS1-positive NSCLC. This article highlights what makes the Nuvalent’s NVL-520 program scientifically notable, including what gives it a potential best-in-class profile as a ROS1 inhibitor, the emerging toxicology of hard-to-avoid off-targets, an interesting synthetic route to the small macrocycle, and more.
NVL-520: A Next-Generation, TRK-Sparing, Brain-Penetrant ROS1 Inhibitor
oral brain-penetrant ROS1-selective TKI Ph. I/II for NSCLC and other solid tumors rationally designed (SBDD) from known starting point Press Release, September 2023 Nuvalent Inc., Cambridge, MA