# Taletrectinib

Source: https://onco.cc/drugs/taletrectinib/  
OnCo record `taletrectinib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

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.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-08
- Tags: gap-fill
- 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: CN 2025: ROS1-positive NSCLC; US 2025: Locally advanced or metastatic ROS1-positive NSCLC

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Taletrectinib
- FDA novel approvals 2025: https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2025

## Connected records

- biomarkers: [ROS1 fusion (ROS1-positive)](https://onco.cc/biomarkers/ros1-fusion/)
- cancers: [Lung cancer (all types)](https://onco.cc/cancers/lung-cancer/), [Non-small-cell lung cancer](https://onco.cc/cancers/nsclc/), [ROS1-positive non-small-cell lung cancer](https://onco.cc/cancers/ros1-positive-nsclc/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [ROS1](https://onco.cc/targets/ros1/)
- companies: [Innovent Biologics](https://onco.cc/companies/innovent/), [Nuvation Bio](https://onco.cc/companies/nuvation-bio/), [Omega Funds](https://onco.cc/companies/omega-funds/)
- terms: [Gene fusion](https://onco.cc/terms/gene-fusion/)
- trials: [A Phase III Study Comparing Taletrectinib With Standard Therapy in ROS1 Positive Locally Advanced or Metastatic Non-small Cell Lung Cancer Patients](https://onco.cc/trials/nct06564324/), [Phase 3 Study of Taletrectinib vs Placebo as an Adjuvant Therapy in ROS1 Positive NSCLC (TRUST-IV)](https://onco.cc/trials/nct07154706/), [Taletrectinib Phase 2 Global Study in ROS1 Positive NSCLC](https://onco.cc/trials/nct04919811/)

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