Skip to main content

Table 2 Pharmacokinetic parameters for each drug alone and in combination

From: Pharmacokinetic interactions of esaxerenone with amlodipine and digoxin in healthy Japanese subjects

Parameter Study 1 Study 2 Study 3
Esaxerenone 2.5 mg Amlodipine 2.5 mg Digoxin 0.25 mg/day
Alone (n = 22) + Amlodipine 10 mg/day (n = 22) Alone (n = 18) + Esaxerenone 5 mg/day (n = 18) Alone (n = 19) + Esaxerenone
5 mg/day (n = 19)
Cmax, ng/mL 35.5 ± 6.3 33.9 ± 5.0 2.09 ± 0.47 2.28 ± 0.46 1.54 ± 0.53 1.77 ± 0.73
Ctrough, ng/mL 0.533 ± 0.089 0.583 ± 0.116
AUClast, ng·h/mL 560 ± 106 644 ± 111 87.2 ± 22.3 102 ± 20
AUCinf, ng·h/mL 575 ± 111 674 ± 127 102 ± 29 122 ± 29
AUCtau, ng·h/mL 15.3 ± 2.5 16.5 ± 3.3
tmax, ha 2.00 (1.00–4.00) 2.50 (1.50–4.00) 5.00 (3.00–9.00) 6.00 (5.00–7.00) 1.50 (0.50–4.00) 1.00 (0.50–3.00)
t1/2, h 18.5 ± 3.2 20.9 ± 3.1 40.5 ± 6.8 43.5 ± 6.7 NA NA
CL/F, L/h 4.49 ± 0.79 3.83 ± 0.67 26.8 ± 8.9 21.8 ± 5.9
CLss/F, L/h 16.8 ± 3.2 15.8 ± 3.5
  1. Unless stated otherwise, values are means±standard deviations
  2. NA, not assessable because the elimination rate constant was not appropriately estimated
  3. AUCinf area under the plasma concentration–time curve up to infinity, AUClast AUC up to the last quantifiable time, AUCtau AUC over the dosing interval, CL/F apparent total body clearance, CLss/F apparent total body clearance at steady state, Cmax peak plasma concentration, Ctrough trough plasma concentration, t1/2 terminal elimination half-life, tmax time to reach maximum plasma concentration
  4. aMedian value (range)