Table 5.
Lonafarnib | |||||||
---|---|---|---|---|---|---|---|
Lonafarnib+Gemcitabine Dose |
Cycle | No. of subjects |
Cmax (ng/mL) |
Tmax*** (hour) |
AUC (τ) (ng*hr/mL) |
CL/F (nL/min) |
T½ (hour) |
100+750 | 1 | 4 | 717 | 5.0 | 5995 | 504 | 5.21 |
2 | 3 | 757 | 4.0 | 6033 | 571 | 3.50 | |
100+1000 | 1 | 3 | 1007 | 4.0 | 8201 | 577 | 3.80 |
2 | 2 | 645 | 5.5 | 5945 | 370 | 3.79 | |
150+750 | 1 | 2 | 779 | 5.5 | 5790 | 437 | 3.67 |
2 | 1 | 1500 | 8.0 | 15325 | 163 | 6.68 | |
150/100**+1000 | 1 | 6 | 1078 | 6.0 | 8947 | 413 | 5.57 |
2 | 6 | 736 | 5.0 | 5634 | 440 | 4.68 | |
200+600 | 1 | 5 | 2044 | 6.0 | 16812 | 594 | 5.32 |
2 | 4 | 1885 | 5.0 | 14544 | 261 | 4.78 |
Gemcitabine | |||||
---|---|---|---|---|---|
Lonafarnib+Gemcitabine Dose |
Day | No. of subjects |
Cmax (ng/mL) |
Tmax*** (hour) |
AUC (τ) (ng*hr/mL) |
100+750 | 1 | 4 | 11307 | 0.50 | 5382 |
15 | 4 | 14953 | 0.50 | 7889 | |
100+1000 | 1 | 2 | 10163 | 0.38 | 5075 |
15 | 3 | 9797 | 0.25 | 5064 | |
150+750 | 1 | 2 | 12495 | 0.25 | 5948 |
15 | 2 | 11653 | 0.50 | 8005 | |
150/100**+1000 | 1 | 7 | 15083 | 0.50 | 8801 |
15 | 6 | 17471 | 0.50 | 10111 | |
200+600 | 1 | 6 | 7934 | 0.38 | 4141 |
15 | 7 | 11191 | 0.25 | 4966 |
Cmax, peak plasma concentration, Tmax, time to peak concentration, AUC(τ), area under the plasma concentration - time curve over the dosing interval (12 hours), CL/F, apparent total body clearance
Lonafarnib dose (mg) BID + gemcitabine dose (mg/m2)
Lonafarnib dose 150 mg AM, 100 mg PM
Median values