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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.