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 |