Pharmacokinetic variables for vorinostat and metabolites on day 1 of treatment
Dose (mg) | No. patients | Cmax (μmol/L) | Tmax (h) | AUC (μmol/L × h) | t1/2 (h) | Clapp (L/min) |
---|---|---|---|---|---|---|
Vorinostat | ||||||
200 | 1 | 1.45 | 0.5 | 2.4 | 1.8 | 5.2 |
300 | 8 | 1.36 ± 0.52 | 1.38 ± 0.52 | 3.54 ± 1.31 | 1.37 ± 0.42 | 5.73 ± 2.04 |
400 | 15 | 1.81 ± 0.70 | 1.27 ± 0.42 | 4.67 ± 2.33 | 1.45 ± 0.56 | 6.19 ± 1.88 |
Vorinostat glucuronide | ||||||
200 | 1 | 2.81 | 1 | 6.9 | 2.1 | NA |
300 | 8 | 3.67 ± 2.09 | 2.19 ± 1.03 | 11.7 ± 11.3 | 1.56 ± 0.21 | NA |
400 | 15 | 3.62 ± 1.22 | 1.50 ± 0.38 | 12.8 ± 7.2 | 2.08 ± 1.36 | NA |
4-Anilino-4-oxobutanoic acid | ||||||
200 | 1 | 3.82 | 1 | 15.3 | 5.9 | NA |
300 | 8 | 4.87 ± 1.99 | 2.75 ± 1.13 | 27.2 ± 10.8 | 6.6 ± 5.0 | NA |
400 | 15 | 5.14 ± 1.42 | 2.23 ± 1.03 | 23.5 ± 6.9 | 4.2 ± 1.8 | NA |
Abbreviations: t1/2, half-life; NA, not applicable.