Drug

Repotrectinib

Approved · EMA

ClassProto-oncogene tyrosine-protein kinase ROS inhibitorEmerging researchLate-stage development

Also known as Augtyro, (3R,6S,)-45-FLUORO-3,6-DIMETHYL-5-OXA-2,8-DIAZA-1(5,3)-PYRAZOLO(1,5-A)PYRIMIDINA-4(1,2)-BENZENANONAPHAN-9-ONE, 1,15-ETHENO-1H-PYRAZOLO(4,3-F)(1,4,8,10)BENZOXATRIAZACYCLOTRIDECIN-4(5H)-ONE, 11-FLUORO-6,7,13,14-TETRAHYDRO-7,13-DIMETHYL-, (7S,13R)-.

RxNorm2670644 ChEMBLCHEMBL4298138 ATCL01EX28UNII08O3FQ4UNP

Research papers

Active clinical trials

Protein targets

Regulatory events

Latest activity

beta

Recent clinical, regulatory, research and industry developments relating to this drug.

Open-label Phase II Efficacy Study of Repotrectinib in Frail (PS ≥2) and/or Elderly Patients With ROS1-rearranged Advanced NSCLC

Clinical trial2026-07-07Results expected Q3 2031 · ClinicalTrials.gov

Phase 1/2 Study of TPX-0005 (Repotrectinib) in Combination With Chemotherapy in Pediatric and Young Adult Subjects With Advanced or Metastatic Solid Tumors and Primary Central Nervous System Tumors

Clinical trial2026-06-04Results expected Q3 2028 · ClinicalTrials.gov

A Phase 1/2, Open-Label, Multi-Center, First-in-Human Study of the Safety, Tolerability, Pharmacokinetics, and Anti-Tumor Activity of TPX-0005 in Patients With Advanced Solid Tumors Harboring ALK, ROS1, or NTRK1-3 Rearrangements (TRIDENT-1)

Clinical trial2026-05-27Results expected Q1 2028 · ClinicalTrials.gov

Phase I Clinical Study to Assess Safety and Efficacy of Repotrectinib Combined With Osimertinib in Patients With Advanced, Metastatic EGFR Mutant NSCLC (TOTEM).

Clinical trial2026-04-01Primary completion · ClinicalTrials.gov

Phase 1, 2-Cohort, Open-label, Fixed-sequence, Drug-drug Interaction Study to Evaluate the Effect of Repotrectinib on the Pharmacokinetics of Transporter and CYP P450 Probe Substrates in Healthy Adult Participants

Clinical trial2026-03-19Completed · ClinicalTrials.gov

Randomized, Open-label, Multicenter, Phase 3 Trial 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)

Clinical trial2026-03-13Primary completion · ClinicalTrials.gov

A Phase II Study Assessing Safety and Efficacy of REPotrectinib in ROS1-positive Non-small Cell Lung Cancer Patients With Active Brain mEtastasis (REPOSE Study)

Clinical trial2026-02-25Results expected Q1 2027 · ClinicalTrials.gov

A Phase 1 Study to Assess the Effect of Hepatic Impairment on the Pharmacokinetics of Repotrectinib in Advanced Cancer Patients

Clinical trial2025-12-31Withdrawn · ClinicalTrials.gov

Phase II Study of REPotrectinib With or Without Fulvestrant in Patients With Hormone Receptor-positive Human Epidermal Growth Factor 2-negative Metastatic Invasive LObular Carcinoma Who Received a Prior Endocrine Therapy in Combination With Cyclin-dependent Kinase 4 and 6 Inhibitor (REPLOT Trial)

Clinical trial2025-12-08Terminated · ClinicalTrials.gov

A Phase 1/2, Open-Label, Safety, Tolerability, Pharmacokinetics, and Anti-Tumor Activity Study of Repotrectinib in Pediatric and Young Adult Subjects With Advanced or Metastatic Malignancies Harboring ALK, ROS1, NTRK1-3 Alterations

Clinical trial2025-11-19Results expected Q3 2026 · ClinicalTrials.gov

Approval: Augtyro (EMA)

Regulatory2025-01-13EMA

Repotrectinib in <i>ROS1</i> Fusion-Positive Non-Small-Cell Lung Cancer.

Research2024-01-01The New England journal of medicine

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name

Repotrectinib

Aliases & brands

Augtyro(3R,6S,)-45-FLUORO-3,6-DIMETHYL-5-OXA-2,8-DIAZA-1(5,3)-PYRAZOLO(1,5-A)PYRIMIDINA-4(1,2)-BENZENANONAPHAN-9-ONE1,15-ETHENO-1H-PYRAZOLO(4,3-F)(1,4,8,10)BENZOXATRIAZACYCLOTRIDECIN-4(5H)-ONE, 11-FLUORO-6,7,13,14-TETRAHYDRO-7,13-DIMETHYL-, (7S,13R)-

RxNorm CUI

2670644

ChEMBL ID

CHEMBL4298138

ATC codes

L01EX28

UNII

08O3FQ4UNP

Primary mechanism

Proto-oncogene tyrosine-protein kinase ROS inhibitor

Regulatory jurisdictions

ema

Pharmacology & targets

6 targets

Known molecular targets and mechanisms supported by curated pharmacology databases.

Proto-oncogene tyrosine-protein kinase ROS

ROS1 · P08922

INHIBITORProto-oncogene tyrosine-protein kinase ROS inhibitor

High affinity nerve growth factor receptor

NTRK1 · P04629

INHIBITORNerve growth factor receptor Trk-A inhibitor

BDNF/NT-3 growth factors receptor

NTRK2 · Q16620

INHIBITORNeurotrophic tyrosine kinase receptor type 2 inhibitor

NT-3 growth factor receptor

NTRK3 · Q16288

INHIBITORNT-3 growth factor receptor inhibitor

HLA class II histocompatibility antigen gamma chain

CD74 · P04233

INHIBITORCD74-ROS1 inhibitor

Syndecan-4

SDC4 · P31431

INHIBITORROS1-SDC4 inhibitor

Regulatory timeline

1 event

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Earliest approval

2025-01-13

Latest approval

2025-01-13

Authorities

EMA

Total events

emaEuropean Medicines Agency· 1 event

2025-01-13Approval

Approval: Augtyro (EMA)

Indication: Augtyro as monotherapy is indicated for the treatment of adult patients with ROS1-positive advanced non-small cell lung cancer (NSCLC). Augtyro as monotherapy is indicated for the… Show full indication

Augtyro as monotherapy is indicated for the treatment of adult patients with ROS1-positive advanced non-small cell lung cancer (NSCLC). Augtyro as monotherapy is indicated for the treatment of adult and paediatric patients 12 years of age and older with advanced solid tumours expressing a NTRK gene fusion, and who have received a prior NTRK inhibitor, or  have not received a prior NTRK inhibitor and treatment options not targeting NTRK provide limited clinical benefit, or have been exhausted (see sections 4.4 and 5.1)

Evidence ↗

Clinical trials

12 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme

CLINICALTRIALS.GOV · LIVE REGISTRY

registered trials across all phases

LATEST COMPLETION 2026

Active studies

Recruiting

Late-stage (III+)

Completed

Discontinued

PHASE DISTRIBUTIONn = 12

Phase 15Phase 1 / 23Phase 23Phase 31

Late-stage studies

Phase III+ trials still open or recently active — where late-stage evidence is being generated.

Active, not recruitingPH IIIBristol-Myers Squibbn=1902027

Recent completions

Trials that read out recently, adding to the completed evidence base.

CompletedPH IBristol-Myers Squibbn=302026

A Phase 1, Multicenter, Open-label, Single-dose Study to Assess the Pharmacokinetics of Repotrectinib in Healthy Participants and Those With Moderate and Severe Hepatic Impairment

CompletedPH IBristol-Myers Squibbn=182025

A Phase I, Two-part, Single-center, Open-label, Drug-drug Interaction Study to Assess the Effect of Voriconazole (Part 1) and Quinidine (Part 2) on the Pharmacokinetics of a Single Dose of Repotrectinib (BMS-986472) in Healthy Participants

CompletedPH IBristol-Myers Squibbn=322024

Research activity

1 papers

Key research shaping understanding of this drug, combining the latest publications with the most influential evidence.

Most influential

Repotrectinib in <i>ROS1</i> Fusion-Positive Non-Small-Cell Lung Cancer.

The New England journal of medicine · 2024 · 168 cites