# Repotrectinib

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

## TL;DR

A ROS1 and NTRK pill that also works after other ROS1 drugs fail, with dizziness as its signature side effect.

## Summary

Repotrectinib is a compact macrocyclic ROS1 and TRK inhibitor whose small size lets it bind kinases carrying solvent-front mutations such as ROS1 G2032R, the usual escape route from crizotinib and entrectinib. It is used in ROS1-positive non-small-cell lung cancer both in patients who have never had a ROS1 drug and in those whose disease has progressed on one, and in NTRK-fusion solid tumours of any type. In TRIDENT-1 the response rate was 79% in TKI-naive and 38% in TKI-pretreated ROS1-positive NSCLC. It was approved in November 2023 for ROS1 and June 2024 for NTRK fusions (tumour-agnostic). Dizziness and other neurological effects from TRK inhibition are its signature toxicity, and zidesamtinib (2026) offers a TRK-sparing alternative with fewer neurologic effects. In short, it is the ROS1 pill that still works after other ROS1 drugs fail.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-06
- Brand: Augtyro
- Modality: Small-molecule kinase inhibitor (ROS1 / NTRK)
- Mechanism: Compact macrocyclic ROS1/TRK inhibitor active against solvent-front mutations.
- Approvals: US 2023: ROS1+ locally advanced or metastatic NSCLC; US 2024: NTRK-fusion solid tumours (tumour-agnostic); EU 2025: ROS1+ NSCLC; NTRK+ solid tumours; 13 Jan 2025 (conditional)

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Repotrectinib
- FDA label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Repotrectinib

## Connected records

- biomarkers: [NTRK1/2/3 gene fusion](https://onco.cc/biomarkers/ntrk-fusion/), [ROS1 fusion (ROS1-positive)](https://onco.cc/biomarkers/ros1-fusion/)
- cancers: [Inflammatory myofibroblastic tumour (IMT)](https://onco.cc/cancers/inflammatory-myofibroblastic-tumour/), [KRAS wild-type pancreatic ductal adenocarcinoma](https://onco.cc/cancers/kras-wild-type-pdac/), [Lung cancer (all types)](https://onco.cc/cancers/lung-cancer/), [Non-small-cell lung cancer](https://onco.cc/cancers/nsclc/), [NTRK fusion-positive non-small-cell lung cancer](https://onco.cc/cancers/ntrk-fusion-nsclc/), [Pancreatic ductal adenocarcinoma](https://onco.cc/cancers/pancreatic/), [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: [NTRK](https://onco.cc/targets/ntrk/), [ROS1](https://onco.cc/targets/ros1/)
- drugs: [Zidesamtinib](https://onco.cc/drugs/zidesamtinib/)
- companies: [Bristol Myers Squibb](https://onco.cc/companies/bms/), [Zai Lab](https://onco.cc/companies/zai-lab/)
- trials: [A Study of Repotrectinib (TPX-0005) in Patients With Advanced Solid Tumors Harboring ALK, ROS1, or NTRK1-3 Rearrangements](https://onco.cc/trials/nct03093116/), [A Study of Repotrectinib in Pediatric and Young Adult Subjects Harboring ALK, ROS1, OR NTRK1-3 Alterations](https://onco.cc/trials/nct04094610/), [A Study of Repotrectinib Versus Crizotinib in Participants With Locally Advanced or Metastatic Tyrosine Kinase Inhibitor (TKI)-naïve ROS1-positive Non-Small Cell Lung Cancer (NSCLC) (TRIDENT-3)](https://onco.cc/trials/nct06140836/), [PROFILE 1001 ROS1 expansion cohort](https://onco.cc/trials/profile-1001-ros1/), [Repotrectinib in ROS1-positive Non-small Cell Lung Cancer Patients With Active Brain Metastasis](https://onco.cc/trials/nct06315010/)
- people: [Alexander Drilon](https://onco.cc/people/alexander-drilon/), [Dong-Wan Kim](https://onco.cc/people/kim-dong-wan/)
- key papers: [TRIDENT-1: repotrectinib in ROS1 fusion-positive non-small-cell lung cancer](https://onco.cc/key-papers/paper-trident-1-repotrectinib-nejm-2024/)
- pathways: [Thyroid cancer (KEGG map)](https://onco.cc/pathways/thyroid-cancer-signalling/)

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