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repotrectinib
- Development stage
- Approved
- Lead developer
- Bristol Myers Squibb
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Repotrectinib is a next-generation, small-molecule macrocyclic tyrosine kinase inhibitor developed for the treatment of certain cancers. It selectively inhibits proto-oncogene tyrosine-protein kinase ROS1 (ROS1) and tropomyosin receptor kinases TRKA, TRKB, and TRKC. By blocking these kinases, repotrectinib disrupts abnormal signaling pathways that drive tumor cell proliferation in cancers with ROS1 fusions or NTRK gene fusions. Repotrectinib is approved for adults with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC), as well as for adults and children aged 12 years and older with solid tumors harboring NTRK gene fusions that are locally advanced or metastatic and have progressed following prior therapy or have no satisfactory alternative treatments.
- Brand names
- Augtyro
- Other names
- repotrectinibMultikinase Inhibitor TPX-0005Multi-kinase Inhibitor TPX-0005ALK/ROS1/NTRK/SRC/FAK Multikinase Inhibitor TPX-0005
02
Targets
ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)NTRK2 (Tropomyosin-related kinase receptor type B)JAK2 (Janus kinase 2)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)NTRK3 (Tropomyosin receptor kinase C)NTRK1 (Tropomyosin-related receptor kinase A)
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