TABLE 3.
Pharmacokinetic parameters of SHR2285.
| SHR2285 | |||||
|---|---|---|---|---|---|
| 50 mg (n = 3) | 100 mg (n = 6) | 200 mg (n = 6) | 400 mg (n = 6) | ||
| Tmax, h | Median (range) | 4.0 (2.0–4.0) | 4.0 (2.0–5.0) | 3.0 (1.5–4.0) | 3.0 (1.5–5.0) |
| Cmax, ng/mL | Mean ± SD (%CV) | 306 ± 129 (42.1) | 517 ± 164 (31.8) | 789 ± 311 (39.5) | 883 ± 105 (11.9) |
| GeoMean (%CV) | 287 (47.8) | 490 (39.8) | 747 (35.7) | 877 (11.7) | |
| AUC0-last, h*ng/mL | Mean ± SD (%CV) | 2,450 ± 1,140 (46.5) | 5,080 ± 2,570 (50.6) | 7,210 ± 2,290 (31.7) | 8,490 ± 1,230 (14.5) |
| GeoMean (%CV) | 2,260 (52.3) | 4,540 (56.5) | 6,940 (30.6) | 8,420 (14.7) | |
| AUC0-inf, h*ng/mL | Mean ± SD (%CV) | 2,680 ± 1,220 (45.5) | 5,560 ± 2,690 (48.5) | 7,480 ± 2,660 (35.5) | 9,390 ± 1,240 (13.3) |
| GeoMean (%CV) | 2,490 (49.8) | 5,020 (53.8) | 7,140 (34.1) | 9,320 (12.7) | |
| t1/2, h | Mean ± SD | 7.6 ± 2.0 | 13.2 ± 4.9 | 12.6 ± 3.4 | 15.8 ± 7.1 |
| CL/F, L/h | Mean ± SD (%CV) | 21.6 ± 9.9 (45.9) | 22.1 ± 10.8 (48.8) | 29.2 ± 8.6 (29.5) | 43.2 ± 5.1 (11.9) |
| GeoMean (%CV) | 20.1 (49.6) | 19.9 (53.8) | 28.0 (33.8) | 42.9 (12.5) | |
| Vz/F, L | Mean ± SD (%CV) | 251 ± 179 (71.1) | 391 ± 164 (41.8) | 528 ± 174 (33.0) | 996 ± 501 (50.3) |
| GeoMean (%CV) | 214 (76.2) | 360 (49.3) | 494 (47.7) | 870 (68.1) | |
| MRTinf, h | Median (range) | 10.3 (8.7–10.8) | 16.8 (9.0–21.8) | 13.1 (11.7–20.6) | 18.2 (8.1–25.1) |
AUC0-inf, area under the concentration–time curve from zero to time infinity; AUC0-last, area under the concentration–time curve from zero to last time of quantifiable concentration; CL/F, apparent clearance; Cmax, maximum plasma concentration; CV, coefficient of variation; GeoMean, geometric mean; MRT, mean residence time to infinity; t1/2, terminal elimination half-life; Tmax, time to reach maximum plasma concentration; Vz/F, apparent volume of distribution.