Table 5 Mean (± SD) pharmacokinetic parameter estimates for azacitidine (days 1 and 5) using non-compartmental analysis
Azacitidine (mg/m 2 ) | 20/15 ( n  = 3) | 20/22.5 ( n  = 3) | 20/30 ( n  = 3) | 25/30 ( n  = 3) | 40/30 ( n  = 3) | 50/30 ( n  = 22) | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
Visit | C1D1 | C1D5 | C1D1 | C1D5 | C1D1 | C1D5 | C1D1 | C1D5 | C1D1 | C1D5 | C1D1 | C1D5 |
AUCall (h-ng/ml) | 216.4 (157.1) | 193.1 (108.2) | 428.1 (364.0) | 317.1 (90.7) | 112.5 (118.8) | 143.7 (46.8) | 210.1 (149.7) | 207.7 (146.0) | 97.5 (66.7) | 205.9 (128.8) | 404.5 (191.5) | 426.5 (262.5) |
AUCinf (h-ng/ml) | 220.7 (157.6) | 196.0 (108.7) | 2,328.0 (3,647.5)a | 356.6 (147.7) | 125.3 (108.1) | 145.5 (47.1) | 216.1 (147.2) | 214.3 (144.8) | 100.5 (67.1) | 211.8 (131.8) | 412.1 (195.7) | 431.5 (261.7) |
C max (ng/ml) | 327.0 (258.8) | 333.5 (84.0) | 427.2 (223.8) | 452.4 (214.3) | 206.5 (208.6) | 214.1 (61.5) | 251.9 (116.1) | 273.2 (132.0) | 189.6 (122.2) | 289.0 (138.1) | 581.1 (284.8) | 637.7 (428.6) |
t 1/2 (h) | 0.54 (0.37) | 0.35 (0.18) | 10.89 (18.25) | 1.27 (1.45) | 0.54 (0.44) | 0.34 (0.04) | 0.33 (0.15) | 0.72 (0.37) | 0.16 (0.07) | 0.27 (0.04) | 0.67 (1.03) | 0.42 (0.09) |
CL (l/h/m2) | 167.1 (170.5) | 136.7 (97.0) | 62.7 (53.9) | 62.9 (25.4) | 239.3 (139.2) | 146.1 (40.0) | 168.6 (126.7) | 150.0 (74.6) | 616.6 (525.5) | 253.0 (165.5) | 177.7 (155.9) | 156.2 (80.7) |
V d (l/m2) | 92.3 (58.9) | 61.1 (35.4) | 78.6 (54.4) | 85.4 (69.0) | 226.5 (253.4) | 71.6 (19.0) | 70.3 (35.7) | 132.2 (62.5) | 105.8 (37.0) | 95.6 (57.3) | 120.6 (112.0) | 94.0 (50.7) |