• Alias: LOXO-101; Trk inhibitor
    • An orally available, Trk inhibitor that binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk
    • Phase 2 in relapsed, refractory solid tumors, NHL, or histiocytic disorder with neurotropic tropomyosin receptor kinase (NTRK) fusion
    • Recommended phase 2 dose: 100 mg PO b.i.d. until disease progression
    • Half-life: 3.5 hours
    • Common side effects: Fatigue, dizziness, anemia, dyspnea, neutropenia, constipation (all are grades 1 and 2 toxicities)
    (Laetsch et al., 2017)
    Other topics in Targeted and Immunotherapy Agents