TABLE 5.
Pharmacokinetic parameters of BAY 2433334 in plasma and urine on day 12 in Parts A and B of the study. Data are presented as geometric mean/geometric coefficient of variation (%), unless otherwise indicated
| BAY 2433334 25 mg OD n = 9 | BAY 2433334 50 mg OD n = 9 | BAY 2433334 100 mg OD n = 8 | BAY 2433334 25 mg BID n = 9 | |
|---|---|---|---|---|
| AUCτ (μg h L−1) | 6910/11.0 c | 13 800/25.0 c | 29 500/32.7 c | 6180/32.2 d |
| AUCτ/D (h L−1) | 0.277/11.0 c | 0.276/25.0 c | 0.295/32.7 c | 0.247/32.2 d |
| Cmax (μg L−1) | 507/12.7 c | 963/24.8 c | 1950/28.1 c | 646/30.5 d |
| Cmax/D (10−3 L−1) | 20.3/12.7 c | 19.3/24.8 c | 19.5/28.1 c | 25.8/30.5 d |
| tmax a (h) | 4.00 (1.00–6.03) | 3.00 (0.750–6.05) | 4.00 (1.50–6.00) | 1.50 (1.00–6.00) |
| t1/2 (h) | 15.8/18.7 | 17.8/17.0 | 17.7/22.8 | 15.8/24.1 |
| RAAUC | 1.50/8.69 c | 1.54/10.0 c | 1.72/16.6 c | 2.22/18.5 d |
| RACmax | 1.41/13.4 c | 1.43/24.9 c | 1.63/14.3 c | 1.89/18.8 d |
| RLIN | 1.05/11.9 c | 1.03/7.86 c | 1.08/7.58 c | 1.01/10.1 d |
| %AE,ur,τ b (%) | – | 13.4/3.69 c | 10.1/4.21 c | 13.5/3.42 d |
| CLR (L h−1) | – | 0.469/31.5 c | 0.317/69.9 c | 0.528/40.8 d |
Median (range).
Arithmetic mean/standard deviation (range).
τ = 24 h.
τ = 12 h.
%AE,ur,τ, percentage amount of drug excreted in urine within the dosing interval; AUCτ, area under the plasma concentration–time curve within the dosing interval; AUCτ/D, area under the plasma concentration–time curve within the dosing interval divided by dose; CLR, renal clearance; Cmax, maximum plasma concentration; Cmax/D, maximum plasma concentration divided by dose; RAAUC, accumulation ratio calculated from area under the plasma concentration–time curve within the dosing interval after multiple dosing and after single dosing; RACmax, accumulation ratio calculated from maximum plasma concentration after multiple dosing and after single dosing; RLIN, linearity factor calculated from area under the plasma concentration–time curve within the dosing interval after multiple dosing and area under the plasma concentration–time curve after single dosing; t1/2, terminal half‐life; tmax, time to maximum plasma concentration.