Table 3.
Mean Pharmacokinetics of Free VEGF Trap After Intravenous Administration of Aflibercept
| Dose Level (mg/kg) | Pharmacokinetic Parameters |
|||||
|---|---|---|---|---|---|---|
| Cmax (μg/mL) | Clast (μg/mL) | AUC (day × μg/mL) | T1/2λz (day) | Vss (L) | Cl (L/d) | |
| 0.3 (n = 3) | ||||||
| Coefficient of variation | 4.00 | 0.147 | 9.34 | 1.70 | 4.51 | 1.95 |
| % | 9 | 38 | 15 | 21 | 29 | 42 |
| 1.0 (n = 7) | ||||||
| Coefficient of variation | 17.9 | 0.659 | 50.9 | 2.58 | 5.88 | 1.87 |
| % | 31 | 116 | 54 | 50 | 22 | 51 |
| 2.0 (n = 6) | ||||||
| Coefficient of variation | 34.5 | 2.36 | 125 | 3.76 | 5.58 | 1.13 |
| % | 11 | 71 | 35 | 42 | 21 | 31 |
| 3.0 (n = 7) | ||||||
| Coefficient of variation | 48.7 | 4.06 | 226 | 6.18 | 7.74 | 1.14 |
| % | 30 | 63 | 34 | 38 | 33 | 48 |
| 4.0 (n = 7) | ||||||
| Coefficient of variation | 97.4 | 11.0 | 293 | 5.51 | 7.88 | 1.10 |
| % | 43 | 51 | 15 | 18 | 38 | 38 |
| 5.0 (n = 4) | ||||||
| Coefficient of variation | 86.8 | 9.63 | 428 | 7.43 | 9.89 | 1.27 |
| % | 34 | 28 | 64 | 38 | 31 | 65 |
| 7.0 (n = 12) | ||||||
| Coefficient of variation | 159 | 14.4 | 605 | 5.14 | 6.12 | 0.915 |
| % | 21 | 55 | 46 | 37 | 29 | 39 |
Abbreviations: VEGF, vascular endothelial growth factor; Cmax, maximum observed plasma concentration; Clast, last measurable (non-zero) plasma concentration; AUC, area under the curve extrapolated to infinity; tλz, apparent terminal half-life; Vss, volume of distribution at steady-state; Cl, total body clearance.