Table 2.
Parameter | Unit | 1,25(OH)2D3 | 1,25(OH)2D3 + CTA091 | +/− CTA091 Ratio |
---|---|---|---|---|
Plasma | ||||
AUC0–8h | ng/mL•h | 67.4 | 97.3 | 1.4 |
AUC0-inf | ng/mL•h | 69.1 | 102 | 1.5 |
Cmax | ng/mL | 21.6 | 33.7 | 1.6 |
Tmax | h | 0.25 | 0.5 | 2 |
Vd/F | L/kg | 0.592 | 0.469 | 0.79 |
Kel | h−1 | 0.489 | 0.419 | 0.86 |
t1/2 | h | 1.42 | 1.66 | 1.2 |
Cl/F | L/h/kg | 0.289 | 0.196 | 0.68 |
Tumor | ||||
AUC0–8h | ng/g•h | 8.39 | 21.7 | 2.6 |
AUC0-inf | ng/g•h | 9.18 | 22.9 | 2.5 |
Cmax | ng/g | 1.70 | 4.43 | 2.6 |
Tmax | h | 2 | 2 | 1 |
kel | h−1 | 0.355 | 0.460 | 1.3 |
t1/2 | h | 1.95 | 1.51 | 0.77 |
Tumor/plasma | ||||
AUC0–h | - | 0.125 | 0.22 | 1.8 |
Cmax | - | 0.079 | 0.13 | 1.7 |
Concentration versus time data were obtained after i.p. administration of 20 µg/kg 1,25(OH)2D3 either alone or in combination with 250 µg/kg of CTA091 to mice bearing subcutaneous H292 lung tumors. AUC0–8h, area under the concentration versus time curve from 0 to 8 h; AUC0-inf, area under the concentration versus time curve from 0 to infinity; Cmax, maximum concentration; Tmax, time of Cmax; Vd/F, apparent volume of distribution; kel, elimination rate constant; t½, half-life; Cl/F, apparent clearance.