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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)