Pharmacokineticsa in Cancer Patients | |||||||
---|---|---|---|---|---|---|---|
Dosemg | Cycle/Day | Cmaxng/ml | Tmaxbh | AUC0–∞ng*h/ml | CL l/h | Vdssl | T1/2ch |
10 | 1/1 | 122 | 0.95 | 216 | 47.2 | 89.7 | 2.24 |
(n = 10) | (21.5) | (0.50–1.00) | (26.3) | (27.9) | (35.6) | (1.52–4.85) | |
2/1 | 106 | 0.92 | 192 | 52.2 | 101 | 2.44 | |
(n = 10) | (57.5) | (0.50–1.50) | (48.2) | (48.2) | (43.7) | (1.41–9.30) | |
20 | 1/1 | 246 | 0.98 | 427 | 46.9 | 77.5 | 1.84 |
(n = 5) | (29.0) | (0.50–1.15) | (21.8) | (21.8) | (39.4) | (1.27–3.20) | |
2/1 | 271 | 0.75 | 404 | 49.5 | 71.5 | 1.92 | |
(n = 4) | (62.5) | (0.50–1.00) | (33.2) | (33.2) | (29.4) | (1.17–5.54) | |
40 | 1/1 | 603 | 0.98 | 976 | 41.3 | 79.3 | 3.15 |
(n = 11) | (47.7) | (0.50–1.05) | (42.6) | (42.3) | (28.5) | (1.66–4.56) | |
1/8 | 657 | 1.00 | 938 | 42.6 | 64.1 | 2.68 | |
(n = 9) | (44.1) | (0.50–1.03) | (33.5) | (33.6) | (52.2) | (1.10–6.00) | |
60 | 1/1 | 881 | 0.55 | 1600 | 37.0 | 76.8 | 3.15 |
(n = 5) | (53.3) | (0.50–1.00) | (47.3) | (45.7) | (47.6) | (1.31–5.19) | |
1/8 | 1040 | 0.92 | 1570 | 38.0 | 67.5 | 3.35 | |
(n = 5) | (48.2) | (0.50–1.00) | (36.5) | (36.8) | (37.2) | (1.39–18.0) | |
80 | 1/1 | 898 | 1.00 | 1870 | 44.8 | 86.3 | 2.57 |
(n = 5) | (50.5) | (0.33–1.03) | (76.7) | (77.4) | (63.9) | (1.60–3.60) | |
1/8 | 1150 | 0.98 | 1830 | 45.9 | 66.0 | 2.60 | |
(n = 3) | (27.8) | (0.98–1.00) | (7.84) | (13.9) | (64.3) | (1.51–3.57) | |
120 | 1/1 | 1700 | 0.98 | 3310 | 36.3 | 82.1 | 2.97 |
(n = 3) | (63.2) | (0.98–1.00) | (18.7) | (18.7) | (70.2) | (2.65–3.19) | |
1/8 | 768 | 0.50 | 2190 | 38.3 | 143 | 3.05 | |
(n = 1) | (NA) | (NA) | (NA) | (NA) | (NA) | (NA) |
Renal Clearanced in Cancer Patients | ||||||
---|---|---|---|---|---|---|
Dose mg | n | AUC0–6h/AUC0–∞ | Urine Flow l/day | Parent Recovery (% dose) | CLrenalal/h | CLrenal/GFRunboundfold |
80, 120 | 8 measurements in 5 patients | 91.4 ± 6.4% | 1.6 ± 1.0 | 1.6 ± 0.8 | 0.85 (53.3) | 5.1 ± 2.4 |