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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

From: Phase I dose-escalation study of chiauranib, a novel angiogenic, mitotic, and chronic inflammation inhibitor, in patients with advanced solid tumors

 

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)

  1. 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