LAUSR

Belumosudil is a selective Rho‐associated, coiled‐coil‐containing protein kinase‐2 inhibitor. In this crossover design thorough QT/QTc study, single therapeutic (200 mg) and supratherapeutic (1000 mg) oral doses of belumosudil, moxifloxacin (positive control), and placebo were administered to 34 subjects. Twelve‐lead electrocardiograms and serial pharmacokinetic sampling were acquired. The effect of belumosudil on the placebo‐corrected, change‐from‐baseline QTcF was small, and an effect exceeding 10 ms could be excluded across all time points with both doses. Using concentration–QTc analysis, an effect on ΔΔQTcF >10 ms can be excluded up to belumosudil concentrations of ≈12 080 ng/mL, more than 2‐fold above mean Cmax after the supratherapeutic dose. There was no clinically relevant effect on heart rate or cardiac conduction (ie, the PR and QRS intervals) for belumosudil. No differences in safety were noted between belumosudil and placebo treatment. Assay sensitivity was demonstrated by moxifloxacin's effect on the QTc interval. In conclusion, belumosudil at therapeutic and supratherapeutic doses did not have a clinically meaningful effect on electrocardiogram parameters.