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Table 2 Noncompartmental Mean Pharmacokinetic Parameters of Apatinib After Single or Multiple Oral Doses Administration

From: Safety and pharmacokinetics of novel selective vascular endothelial growth factor receptor-2 inhibitor YN968D1 in patients with advanced malignancies

PK parameter

Single Oral Dose

Multiple Oral Dose of 750 mg

 

500 mg

(n= 8)

750 mg

(n= 12)

850 mg

(n= 8)

Day 1

(n= 11)

Day 6

(n= 11)

Day 28

(n= 11)

Day 56

(n= 11)

C max , ng/ml

   Geometric mean

1,521

2,379

2,833

2,421

2,553

2,210

1,854

   CV%

75.1

55.9

90.0

68.5

52.8

45.5

51.2

t max , hour

   Median

3.5

3.0

4.0

3.0

4.0

4.0

3.0

   Range

3.0-8.0

2.0-4.0

1.5-8.0

2.0-8.0

3.0-8.0

2.0-6.0

2.0-6.0

AUC0-24, ng·h/ml

   Geometric mean

11,295

18,172

21,975

19,399

25,449

19,946

15,629

   CV%

69.7

59.3

80.8

60.5

59.2

43.2

63.2

t 1/2λz, hours

   Mean

8.1

9.0

9.1

8.9

11.0

11.3

8.3

   CV%

30.7

15.1

33.1

25.8

56.7

66.5

61.0

  1. Abbreviations: C max , maximum plasma concentration; CV, coefficient of variation; t max , time to reach C max ; AUC0-24, area under plasma concentration-time curve from 0 to 24 hour; t 1/2λz, half-life associated with terminal slope of a semilogarithmic concentration-time curve.
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BMC Cancer

ISSN: 1471-2407

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