Table 3.
Mean pharmacokinetic parameters for AT7519.a | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Dose level | Dose | Cmax | t1/2,z | AUC | CL | Vz | Dose | Cmax | t1/2,z | AUC | CL | Vz | |||
Day | (mg/m2) | n | (ng/mL) | (h) | (ng•h/mL) | (L/h/m2) | (L/m2) | (mg/m2) | n | (ng/mL) | (h) | (ng•h/mL) | (L/h/m2) | (L/m2) | |
1 | C0D1 | 40 | 5 | 193 | 10.0 | 780 | 51.3 | 742 | |||||||
(25.4) | (9.0) | (17.1) | (17.1) | (18.9) | |||||||||||
2 | C0D1 | 80 | 17 | 349 | 10.4 | 1486 | 53.8 | 804 | |||||||
(56.5) | (41.2) | (29.0) | (29.0) | (28.2) | |||||||||||
3 | C0D1 | 80 | 5 | 487 | 9.0 | 1677 | 47.7 | 617 | |||||||
(35.5) | (24.6) | (3.3) | (3.3) | (25.6) | |||||||||||
C0D1 | All | 27 | 10.0 | 52.2 | 754 | ||||||||||
(34.1) | (24.1) | (27.5) | |||||||||||||
1 | C1D1 | 40 | 4 | 146 | 9.6 | 621 | 64.4 | 891 | 21 | 4 | 462.8 | 7.48 | 1545 | 13.6 | 146.6 |
(81.1) | (16.0) | (24.2) | (24.2) | (20.5) | (27.8) | (23.0) | (29.7) | (29.7) | (14.4) | ||||||
2 | C1D1 | 80 | 16 | 331 | 8.7 | 1392 | 57.5 | 721 | 21 | 15 | 459.3 | 11.1 | 2300 | 9.13 | 146.3 |
(40.3) | (31.9) | (26.3) | (26.3) | (26.1) | (22.4) | (33.8) | (43.4) | (43.4) | (23.7) | ||||||
3 | C1D1 | 80 | 4 | 331 | 7.4 | 1410 | 56.7 | 606 | 27 | 4 | 602.0 | 9.21 | 2662 | 10.1 | 134.7 |
(26.3) | (56.8) | (11.2) | (11.2) | (54.5) | 27 | 4 | (25.2) | (18.2) | (12.0) | (12.0) | (27.4) | ||||
C1D1 | All | 24 | 8.6 | 58.4 | 725 | All | 23 | 10.0 | 9.97 | 144.3 | |||||
(33.9) | (23.7) | (31.6) | All | 23 | (33.2) | (39.6) | (22.3) | ||||||||
1 | C1D11 | 40 | 2 | 155 | 9.4 | 610 | 65.6 | 855 | |||||||
(10.4) | (3.5) | (3.2) | (3.2) | (5.4) | 21 | 2 | 485.7 | 10.8 | 2105 | 9.98 | 155.9 | ||||
2 | C1D11 | 80 | 11 | 355 | 8.2 | 1280 | 62.5 | 743 | |||||||
(57.2) | (16.7) | (35.8) | (35.8) | (39.6) | 21 | 11 | 508.7 | 10.7 | 2449 | 8.58 | 132.6 | ||||
3 | C1D11 | 80 | 3 | 424 | 6.7 | 1507 | 53.1 | 516 | |||||||
(31.9) | (49.6) | (12.4) | (12.4) | (36.6) | 27 | 2 | 581.1 | 9.38 | 2695 | 10.0 | 135.5 | ||||
C1D11 | All | 16 | 8.1 | 61.0 | 706 | ||||||||||
(24.3) | (30.3) | (38.8) | All | 15 | 10.5 | 8.93 | 135.9 |