TABLE 2.
Estimated PK parameters of apatinib and gefitinib
| Dose Level | Apatinib 500 mg | Apatinib 250 mg | Gefitinib 250 mg | |||
|---|---|---|---|---|---|---|
| PK parameter | Day 1 (n = 5) | Day 15 (n = 5) | Day 1 (n = 6) | Day 15 (n = 6) | Day 1 (n = 11) | Day 15 (n = 11) |
| Mean (SD) | ||||||
| T1/2 (h) | 10 (3) | 9 (2) | 17 (20) | 11 (3) | 21 (14) | 30 (17) |
| Median (range) | ||||||
| Tmax (h) | 3 (1‐6) | 3 (2‐3) | 3 (1‐4) | 3 (1‐4) | 3 (3‐6) | 4 (3‐6) |
| Geometric Mean (%CV) | ||||||
| Cmax, ng/mL | 456 (51) | 468 (73) | 318 (71) | 389 (44) | 272 (31) | 465 (28) |
| Geometric Mean (%CV) | ||||||
| AUC0‐24, hr*ng/mL | 3807 (57) | 3945 (79) | 2477 (79) | 3898 (91) | 3436 (20) | 7978 (29) |
| Geometric Mean (%CV) | ||||||
| AUC0‐∞, hr*ng/mL | 4664 (63) | 4666 (89) | 3507 (70) | 4998 (104) | 6397 (35) | 18101 (62) |
| Mean (SD) | ||||||
| Vd (L) | 1714 (1006) | 1977 (1558) | 2154 (2563) | 1063 (469) | 1100 (275) | 1331 (675) |
| Mean (SD) | ||||||
| CL (L/h) | 144 (133) | 1537 (102) | 85 (57) | 73 (31) | 41 (12) | 32 (9) |
Abbreviations: T1/2, half‐life; Tmax, time to reach Cmax; Cmax, maximum plasma concentration; AUC0‐24, area under plasma concentration‐time curve from 0 to 24 hour; Vd, volume of distribution; CL, clearance rate; SD, standard deviation.