After single oral administration of Esaxerenone at 0.1, 0.3, 1, and 3mg/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 4.5h. After intravenous administration of Esaxerenone at 0.1, 0.3, 1, and 3mg/kg, the total body clearance (CL) and distribution volume at steady state (Vss) are 3.53 to 6.69mL/min/kg and 1.47 to 2.49L/kg, respectively, in rats, and 2.79 to 3.69mL/min/kg and 1.34 to 1.54L/kg, respectively, in cynomolgus monkeys. Up to 168h 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 168h is 11.5% in urine, 82.3% in feces, and 93.9% in total[1].
