After single oral administration of Esaxerenone at 0.1, 0.3, 1, and 3?mg/kg, maximum plasma concentration (Cmax) and the area under the plasma concentration versus time curve (AUC) are increased with dose. Time to reach the maximum plasma concentration (Tmax) of Esaxerenone ranges from 2.0 to 4.5?h. After intravenous administration of Esaxerenone at 0.1, 0.3, 1, and 3?mg/kg, the total body clearance (CL) and distribution volume at steady state (Vss) are 3.53 to 6.69?mL/min/kg and 1.47 to 2.49?L/kg, respectively, in rats, and 2.79 to 3.69?mL/min/kg and 1.34 to 1.54?L/kg, respectively, in cynomolgus monkeys. Up to 168?h after administration, 3.9% and 91.4% of dosed radioactivity are excreted in rat urine and feces, respectively, and 95.2% in total. In monkeys, the excreted radioactivity up to 168?h is 11.5% in urine, 82.3% in feces, and 93.9% in total[1].
