BAY 2731954 (LOXO-195)

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Characteristics

LOXO-195, a is a novel, selective and highly potent TRK inhibitor that is being initially developed for use in patients who have progressed or are intolerant to prior TRK inhibitor therapy [1-3]. BAY 2731954 (LOXO-195) can be dosed orally and twice daily [4].

References

  1. Blake J, Kolakowski GR, Tuch B et al. The development of LOXO-195, a second generation TRK kinase inhibitor that overcomes acquired resistance to 1st generation inhibitors observed in patients with TRK-fusion cancers. European Journal of Cancer 2016; 69: S144-S145.
  2. Drilon A, Nagasubramanian R, Blake JF et al. A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors. Cancer Discov 2017; 7: 963-972.
  3. Cocco E, Scaltriti M, Drilon A. NTRK fusion-positive cancers and TRK inhibitor therapy. Nat Rev Clin Oncol 2018; 15: 731-747.
  4. Hyman D, Kummar S, Farago A et al. Phase I and expanded access experience of LOXO-195 (BAY 2731954), a selective next-generation TRK inhibitor (TRKi). Presented at: AACR Annual Meeting: March 29 to April 3, 2019; Atlanta, GA. Abstract CT127. 2019.