{"entity":{"id":"taletrectinib","kind":"drug","name":"Taletrectinib","aka":[],"tldr":"A ROS1 lung-cancer pill approved in 2025 that works in the brain and after crizotinib, with fewer dizziness-type side effects than repotrectinib.","summary":"Taletrectinib is a selective, CNS-penetrant ROS1 tyrosine kinase inhibitor active against G2032R and other solvent-front mutations that cause resistance to crizotinib. It has limited TRK inhibition, which means fewer of the dizziness and neurological effects seen with repotrectinib. In the TRUST-I (China) and TRUST-II (global) studies, response rates were about 85 to 90% in TKI-naive patients and 50 to 60% after crizotinib, with intracranial responses and activity against G2032R. China approved it in January 2025 and the FDA in June 2025 for locally advanced or metastatic ROS1-positive NSCLC, developed by Nuvation Bio; hepatotoxicity and gastrointestinal effects are the main toxicities. Sequencing against crizotinib, entrectinib and repotrectinib is not settled. In short, taletrectinib is a ROS1 pill that works in the brain and after resistance, with fewer neurological side effects.","status":"approved","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/Taletrectinib","links":[{"label":"FDA novel approvals 2025","url":"https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2025"}],"tags":["gap-fill"],"related":["ros1-fusion"],"cancers":["nsclc","ros1-positive-nsclc"],"sections":[],"technologies":["kinase-inhibitors"],"targets":["ros1"],"drugs":[],"companies":["nuvation-bio","innovent"],"institutions":[],"pathways":[],"terms":["gene-fusion"],"trials":["nct07154706","nct06564324","nct04919811"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Ibtrozi","modality":"Small-molecule ROS1 TKI (next generation, CNS-penetrant)","mechanism":"Selective ROS1 inhibitor active against G2032R and other solvent-front mutations with limited TRK inhibition (fewer neurologic effects).","approvals":[{"region":"CN","year":2025,"indication":"ROS1-positive NSCLC"},{"region":"US","year":2025,"indication":"Locally advanced or metastatic ROS1-positive NSCLC"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},"route":"/drugs/taletrectinib/","neighbours":{"biomarker":[{"id":"ros1-fusion","kind":"biomarker","name":"ROS1 fusion (ROS1-positive)","route":"/biomarkers/ros1-fusion/"}],"cancer":[{"id":"lung-cancer","kind":"cancer","name":"Lung cancer (all types)","route":"/cancers/lung-cancer/"},{"id":"nsclc","kind":"cancer","name":"Non-small-cell lung cancer","route":"/cancers/nsclc/"},{"id":"ros1-positive-nsclc","kind":"cancer","name":"ROS1-positive non-small-cell lung cancer","route":"/cancers/ros1-positive-nsclc/"}],"technology":[{"id":"kinase-inhibitors","kind":"technology","name":"Small-molecule kinase inhibitors","route":"/technologies/kinase-inhibitors/"}],"target":[{"id":"ros1","kind":"target","name":"ROS1","route":"/targets/ros1/"}],"company":[{"id":"innovent","kind":"company","name":"Innovent Biologics","route":"/companies/innovent/"},{"id":"nuvation-bio","kind":"company","name":"Nuvation Bio","route":"/companies/nuvation-bio/"},{"id":"omega-funds","kind":"company","name":"Omega Funds","route":"/companies/omega-funds/"}],"term":[{"id":"gene-fusion","kind":"term","name":"Gene fusion","route":"/terms/gene-fusion/"}],"trial":[{"id":"nct06564324","kind":"trial","name":"A Phase III Study Comparing Taletrectinib With Standard Therapy in ROS1 Positive Locally Advanced or Metastatic Non-small Cell Lung Cancer Patients","route":"/trials/nct06564324/"},{"id":"nct07154706","kind":"trial","name":"Phase 3 Study of Taletrectinib vs Placebo as an Adjuvant Therapy in ROS1 Positive NSCLC (TRUST-IV)","route":"/trials/nct07154706/"},{"id":"nct04919811","kind":"trial","name":"Taletrectinib Phase 2 Global Study in ROS1 Positive NSCLC","route":"/trials/nct04919811/"}]}}