Taletrectinib is a potent and selective tyrosine kinase inhibitor primarily developed for the treatment of cancers driven by ROS1 and NTRK gene fusions. It shows significant activity in non-small cell lung cancer (NSCLC) patients with ROS1 rearrangements, including those who have developed resistance to earlier-generation ROS1 inhibitors. Its ability to penetrate the central nervous system makes it particularly effective in managing brain metastases, a common challenge in advanced lung cancer. Clinical trials have demonstrated durable responses and a favorable safety profile, positioning taletrectinib as a promising therapeutic option for patients with limited treatment alternatives. It is also being evaluated in tumors with NTRK fusions, expanding its potential use across various cancer types such as colorectal, ovarian, and sarcomas.