Taletrectinib adipateProduct ingredient for Taletrectinib

Taletrectinib is an orally available small molecule kinase inhibitor. It is targeted against ROS1, including resistant mutant forms, and shows some inhibitor activity against tropomyosin receptor kinases (TRKs) TRKA, TRKB, and TRKC.⁵ Gene fusions involving ROS1, a proto-oncogene, have been identified as oncogenic drivers in 1-2% of patients with non-small cell lung cancer (NSCLC), in addition to other cancers at variable frequencies.⁴ As part of the second-generation of ROS1 inhibitors, taletrectinib is significantly more potent against ROS1 resistance mutations - for example, the IC50 for taletrectinib against ROS1 exhibiting the secondary solvent-front mutation G2032R is 400-times lower than that of the previously approved first-generation inhibitors crizotinib and entrectinib.¹

Taletrectinib was approved by the US FDA in June 2025 for use in patients with advanced ROS1-positive NSCLC.^5,6