Table 3. Pharmacokinetic parameters for entinostat in plasma after Cycle 1, day 1.
Pharmacokinetic parametersa
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Dose (mg m −2 ) | Number of patients | Tmax (h) | Cmax (ng ml −1 ) | Vz/F (l m −2 ) | Cls/F (l h −1 m −2 ) | T1/2 (h) | AUC0−∝ (ng h ml −1 ) |
4 | 14 | 0.50 (0.23–1.50) | 114.3±84.0 | 1368±435b | 16.8±26.3b | 129.7±88.5b | 586.6±401.1b |
5 | 4 | 0.25 (025–1.00) | 109.0±66.0 | 1003±634 | 10.8±8.0 | 77.3±31.9 | 778.4±648.2 |
Total | 18 | 0.42 (0.23–1.50) | 1256±508c | 14.9±22.0c | 113.6±78.2c |
Abbreviations: AUC0−∝=area under the concentration-time curve from time 0 to infinity; Cls/F, Cmax=maximal plasma concentration; Tmax=time of the maximal plasma concentration; T1/2=terminal half-life; VzF=apparent volume of distribution.
Values are median (range) for Tmax and mean±s.d. for AUC0−∝, Cmax, T1/2, and Vz/F.
n=9.
n=13.