Phase I Trial to Evaluate the Tolerance, Pharmacokinetics and Efficacy of the Broad-Spectrum ErbB Family Inhibitor Larotinib Mesylate in Patients With Advanced Solid Tumors

Background: The presented phase I, first-in-human study evaluated the tolerance, pharmacokinetics, and preliminary efficacy of larotinib mesylate in patients with advanced solid tumors. Methods: Cancer were assigned to receive at 50–400 mg dose levels until disease progression or intolerance. Dose-limiting toxicities assessed during Cycles 0 1. Pharmacokinetic evaluations performed after first steady-state. Results: Twenty-five tumors enrolled dose-escalation study. No DLTs observed. Acne-like rash (68.0%), diarrhea (48.0%), paronychia anemia (48.0%) most reported treatment-related adverse events. clear linear pharmacokinetic characteristic could be drawn, obvious accumulation was Two non-small cell lung cancer experienced a partial response, 15 had stable treatment. Conclusion: Continuous oral administration daily demonstrated favorable safety profile, anti-tumor activity observed