Repotrectinib is a tyrosine kinase inhibitor used to treat locally active or metastatic non-small cell lung cancer. ROS1 mutations are one of the defined oncogenic drives of NSCLC, and the solvent-front mutation ROS1 G2032R is responsible for 50 to 60% of crizotinib-resistant cases.
- Mechanism
- Curator reviewed · 1 reference
Repotrectinib is an inhibitor of proto-oncogene tyrosine-protein kinase ROS1 (ROS1) and of the tropomyosin receptor tyrosine kinases (TRKs) TRKA, TRKB, and TRKC.
- Primary indication
- Repotrectinib is indicated for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC).Curator reviewed · 3 structured indications
- Formula / weight
- C18H18FN5O2 · 355.373 g/mol (avg)
- First approval
- Canada, 2025 · United States, 2023 · European Union, 2025
- Also known as
- (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 · (7S,13R)-11-Fluoro-7,13-Dimethyl-6,7,13,14-Tetrahydro-1,15-Ethenopyrazolo[4,3-F][1,4,8,10]Benzoxatriazacyclotridecin-4(5H)-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)-
- Code names
- BMS-986472 · TPX-0005
- Brand names
Resolves to
Clinical / RWD
Structure
InChIKey
FIKPXCOQUIZNHB-WDEREUQCSA-NSMILESC[C@H]1CNC(=O)C2=C3N=C(N[C@H](C)C4=CC(F)=CC=C4O1)C=CN3N=C2Transporters
What you can answer from here — as of June 15, 2026
4Protein targetsEach mapped to UniProt, with action and pharmacological actionListed above
4TransportersSubstrate / inhibitor direction, not just membershipListed above
Which drugs share a target with Repotrectinib, and which of those have an active Phase 3 trial?
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