Esaxerenone (XL-550) is a highly potent and selective non-steroidal antagonist of the mineralocorticoid receptor.

After Esaxerenone (0.1, 0.3, 1, and 3?mg/kg, intravenous administration) treatment, 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. After Esaxerenone (0.1, 0.3, 1, and 3?mg/kg, single oral administration) treatment, 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 of Esaxerenone ranges from 2.0 to 4.5?h. After 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].