Repotrectinib (repotrectinib, TPX-0005) is an orally-available multi-kinase inhibitor designed to overcome resistance due to solvent-front substitutions involving TRKA, TRKB, and TRKC proteins as well as those involving ROS1, and ALK [1, 2]. Repotrectinib is smaller than most other TRK/ROS/ALK protein inhibitors and can cross the blood–brain barrier, thereby suggesting potential CNS activity.
- Drilon A, Ou SI, Cho BC et al. Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations. Cancer Discov 2018; 8: 1227-1236.
- Cocco E, Scaltriti M, Drilon A. NTRK fusion-positive cancers and TRK inhibitor therapy. Nat Rev Clin Oncol 2018; 15: 731-747.