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  1. OncologyPRO
  2. Oncology in Practice
  3. Anti-Cancer Agents and Biological Therapy
  4. Targeting NTRK Gene Fusions
  5. Overview of Cancers with NTRK Gene Fusion
  6. TRK Inhibitors

Repotrectinib

Overview of Cancers With NTRK Gene Fusion

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Characteristics

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.

References

  1. 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.
  2. Cocco E, Scaltriti M, Drilon A. NTRK fusion-positive cancers and TRK inhibitor therapy. Nat Rev Clin Oncol 2018; 15: 731-747.

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