Summary of pharmacokinetic parameters for MS-275
| Dose, mg/m2 . | No. of patients . | Cmax, ng/mL (range) . | AUC, ng h/mL (range) . | CL/F, L/h (range) . | T1/2, h (range) . | Tmax, h (range) . |
|---|---|---|---|---|---|---|
| 4 | 7 | 4.74 ± 3.41 (2.20-10.7) | 208 ± 86.1 (106-324) | 40.9 ± 17.2 (24.7-75.8) | 36.6 ± 18.6 (16.2-64.2) | 12 (2-24) |
| 6 | 7 | 4.85 ± 1.76 (2.10-7.60) | 351 ± 121* (206-470) | 34.4 ± 11.5* (25.5-48.7) | 43.8 ± 16.4* (28.3-69.3) | 12 (2-36) |
| 8 | 15 | 53.1 ± 92.4 (2.71-302) | 328 ± 168† (86.0-620) | 66.7 ± 54.5† (25.8-209) | 33.4 ± 12.7† (16.7-53.3) | 1 (0.5-24) |
| 10 | 6 | 53.2 ± 58.0 (4.55-164) | 312 ± 78.8‡ (217-404) | 68.2 ± 25.4‡ (48.7-103) | 30.4 ± 13.9‡ (14.6-49.5) | 1 (0.5-2) |
| All doses | 35 | NA | NA | 54.0 ± 37.2§ (24.7-209) | 35.6 ± 15.0§ (14.6-69.3) | 2 (0.5-36) |
| Dose, mg/m2 . | No. of patients . | Cmax, ng/mL (range) . | AUC, ng h/mL (range) . | CL/F, L/h (range) . | T1/2, h (range) . | Tmax, h (range) . |
|---|---|---|---|---|---|---|
| 4 | 7 | 4.74 ± 3.41 (2.20-10.7) | 208 ± 86.1 (106-324) | 40.9 ± 17.2 (24.7-75.8) | 36.6 ± 18.6 (16.2-64.2) | 12 (2-24) |
| 6 | 7 | 4.85 ± 1.76 (2.10-7.60) | 351 ± 121* (206-470) | 34.4 ± 11.5* (25.5-48.7) | 43.8 ± 16.4* (28.3-69.3) | 12 (2-36) |
| 8 | 15 | 53.1 ± 92.4 (2.71-302) | 328 ± 168† (86.0-620) | 66.7 ± 54.5† (25.8-209) | 33.4 ± 12.7† (16.7-53.3) | 1 (0.5-24) |
| 10 | 6 | 53.2 ± 58.0 (4.55-164) | 312 ± 78.8‡ (217-404) | 68.2 ± 25.4‡ (48.7-103) | 30.4 ± 13.9‡ (14.6-49.5) | 1 (0.5-2) |
| All doses | 35 | NA | NA | 54.0 ± 37.2§ (24.7-209) | 35.6 ± 15.0§ (14.6-69.3) | 2 (0.5-36) |
Data are shown as mean ± SD, with observed range in parentheses, except for Tmax (median with range in parentheses).
Cmax indicates peak plasma concentration; AUC, area under the plasma concentration versus time curve extrapolated to infinity; CL/F, apparent oral clearance; T1/2, half-life of the terminal phase; Tmax, time to Cmax; and NA, not applicable.
n = 5.
n = 10.
n = 5.
n = 27.