Table 5. Pharmacokinetic Parameters of Sorafenib, Sunitinib, and Sunitinib Metabolite With and Without Trebananib.
Sorafenib | Sorafenib | Sunitinib | Sunitinib | Sunitinib Metabolite | Sunitinib Metabolite | |||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
| ||||||||||||
Trebananib Dose | Without | 3 mg/kg | Without | 10 mg/kg | Without | 3 mg/kg | Without | 10 mg/kg | Without | 3 mg/kg | Without | 10 mg/kg |
Tmax (hr)a | ||||||||||||
Mean | 1.1 | 1.0 | 1.0 | 1.0 | 8.0 | 8.0 | 8.1 | 8.3 | 8.1 | 8.0 | 8.0 | 8.0 |
%CV | 100 | 200 | 37 | NA | 24 | 46 | 35 | 54 | 34 | 39 | 64 | 49 |
Cmax (μg/mL) | ||||||||||||
Mean | 0.466 | 0.507 | 0.559 | 0.541 | 0.0642 | 0.0703 | 0.0618 | 0.0676 | 0.0212 | 0.0274 | 0.0133 | 0.025 |
%CV | 75.9 | 40.6 | 53.2 | NA | 25.9 | 20.2 | 42.9 | 47.0 | 88.1 | 36.5 | 51.6 | 37.7 |
AUCa (hr·μg/mL) | ||||||||||||
Mean | 2.58 | 3.18 | 3.13 | 3.92 | 1.30 | 1.337 | 1.25 | 1.41 | 0.448 | 0.566 | 0.268 | 0.486 |
%CV | 68.1 | 89.7 | 12.2 | NA | 23.4 | 24.5 | 40.4 | 49.6 | 64.0 | 34.1 | 48.1 | 39.2 |
CL (μg/mL) | ||||||||||||
Mean | 20.9 | 173 | 14.2 | 78.7 | 44.8 | 54.3 | 46.6 | 50.7 | 14.1 | 20.7 | 10.5 | 19.2 |
%CV | 79.6 | 159 | 50.7 | NA | 21.7 | 24.6 | 42.1 | 57.6 | 70.4 | 34.4 | 44.1 | 44.4 |
Abbreviations: AUC = Area under the concentration-time curve; Cmax = Maximum observed concentration after IV infusion of trebananib; CL = Clearance; CV = coefficient of variation; NA = Not applicable; Tmax = Time of maximum concentration after IV infusion of trebananib.
Sorafenib AUC0-12; sunitinib AUC0-24.