Table 3.
Summary of pharmacokinetic parameters following single and multiple dosing of resminostat.
| Resminostata pharmacokinetic parameter values following single oral administration (day 1) | |||||
|---|---|---|---|---|---|
| Dose | 100 mg | 200 mg | 400 mg | 600 mg | 800 mg |
| N of patients | 3 | 3 | 3 | 3 | 7 |
| Half-life (h) | 3.77 (3.21 - 4.41) |
3.12 (2.75 - 3.53) |
3.44 (3.22 - 3.67) |
2.84 (2.74 - 2.94) |
2.81 (2.35 - 3.37) |
| Clearance (mL/h) | 80900 (51600, 127000) |
53800 (45000, 64300) |
52500 (50600, 54400) |
41400 (32200, 53300) |
37700 (29500, 48200) |
| Cmax (ng/mL) | 487 (331, 716) |
1470 (915, 2370) |
2160 (1720, 2710) |
4100 (3060, 5480) |
4970 (3540, 6980) |
| AUCinf (h × ng/mL) | 1236 (788, 1936) |
3718 (3110, 4445) |
7626 (7355, 7906) |
14480 (11260, 18620) |
21200 (16580, 27090) |
| Resminostata pharmacokinetic parameter values following multiple oral administration (day 5) | |||||
| Dose | 100 mg | 200 mg | 400 mg | 600 mg | 800 mg |
| N of patients | 3 | 3 | 3 | 3 | 6 |
| tmax (h) | 2.00 (0.75 - 2.50) |
2.00 (1.50 - 5.00) |
2.50 (1.50 - 4.00) |
2.50 (1.50 - 4.00) |
1.75 (1.50 - 6.00) |
| Clearance (mL/h) | 75100 (51000, 110000) |
59500 (45500, 77800) |
49300 (39900, 61000) |
31100 (27100, 35600)b |
41200 (29900, 56800) |
| Cmax (ng/mL) | 373 (222, 627) |
1060 (536, 2080) |
2270 (1650, 3130) |
3000 (1640, 5460) |
4510 (2280, 8940) |
| AUCss (h × ng/mL) | 1332 (905.1, 1961) |
3362 (2572, 4395) |
8108 (6559, 10020) |
19310 (16860, 22110)b |
19430 (14100, 26780) |
a
free-base
b
n = 2
Abbreviations: tmax = time of peak plasma concentration, Cmax = peak plasma concentration, AUCss = area under the curve for steady state levels
Geometric means (68% range) have been provided except for tmax where median values (min/max) have been presented instead.