Table 3.
The pharmacokinetic exposure parameters of plasma chiauranib after single and multiple dose of 10, 20, 35, 50, and 65 mg chiauranib capsules in patients with advanced solid tumor
| Tmax (h) | AUC0–24 h (ng h/mL) | AUC0–144 h (ng h/mL) | Cmax (ng/mL) | DF | Ctrough (ng/mL) | Cav (ng/mL) | ||
|---|---|---|---|---|---|---|---|---|
| Day1 | 10 mg (n = 2) | 2.0 | 1998 | 3576 | 201 | / | / | / |
| 20 mg (n = 6) | 2.0 (1–4) | 3454 (1275) | 6815 (3902) | 354 (158) | / | / | / | |
| 35 mg (n = 3) | 1.0 (1–8) | 5762 (3853) | 11859 (8656) | 608 (437) | / | / | / | |
| 50 mg (n = 3) | 1.0 (1–2) | 7417 (1380) | 16429 (5251) | 756 (87) | / | / | / | |
| 65 mg (n = 4) | 1.5 (1–2) | 11015 (3572) | 24823 (12581) | 1275 (358) | / | / | / | |
| Day28 | 10 mg (n = 2) | 2.0 | 4185 | / | 312 | 1.1 (0.4) | 122 (21) | 174 (9) |
| 20 mg (n = 6) | 2.0 | 6175 (1526) | / | 517 (134) | 1.3 (0.6) | 191 (89) | 257 (64) | |
| 35 mg (n = 3) | 4 (1–4) | 11761 (8066) | / | 773 (532) | 0.8 (0.4) | 330 (208) | 490 (336) | |
| 50 mg (n = 3) | 2 (1–2) | 14504 (5650) | / | 1118 (254) | 1.1 (0.3) | 467 (166) | 604 (235) | |
| 65 mg (n = 4) | 2 (1–2) | 24230 (11819) | / | 2238 (1012) | 1.5 (0.8) | 890 (662) | 1010 (492) | |
AUC0–24 h area under the concentration-time curve from 0 to 24 h, AUC 0–144 h area under the concentration-time curve from 0 to 144 h, Cmax maximum plasma concentration, Tmax time to reach maximum plasma concentration