4. PK parameters and PARP inhibition following single fluzoparib dose.
| PK parameter | 80 mg (n=10) | 100 mg (n=13) | 150 mg (n=13) | ||||||||
| Mean | SD | CV (%) | Mean | SD | CV (%) | Mean | SD | CV (%) | |||
| PK, pharmacokinetic; PARP, poly(ADP-ribose) polymerases; Tmax, time to Cmax; Cmax, peak concentration; AUC0−t, area under the cueve from time 0 to last quantifiable concentration; AUC0−∞, AUC from time 0 extrapolated to infinity; λz, first-order rate constant of terminal phase; t1/2z, terminal half-life; MRT, mean retention time; Vz/F, apparent volume of distribution; CL/F, apparent total clearance of the drug; SD, standard deviation; CV, coefficient of variation. | |||||||||||
| Tmax (h) | 3.00 (1.50−4.00) | − | − | 3.00 (1.50−6.00) | − | − | 2.50 (1.00−6.00) | − | − | ||
| Cmax(μg/mL) | 2.53 | 0.67 | 26.7 | 3.55 | 1.52 | 42.9 | 4.77 | 1.21 | 25.4 | ||
| AUC0−t(h·μg/mL) | 42.1 | 15.8 | 37.5 | 53.0 | 31.8 | 59.9 | 78.7 | 30.6 | 39.0 | ||
| AUC0−∞ (h·μg/mL) | 46.5 | 20.7 | 44.5 | 58.2 | 36.5 | 62.7 | 82.8 | 33.9 | 40.9 | ||
| λz(1/h) | 0.0633 | 0.0214 | 33.8 | 0.0696 | 0.0260 | 37.4 | 0.0722 | 0.0191 | 26.5 | ||
| t1/2z(h) | 12.3 | 4.9 | 39.7 | 11.3 | 4.1 | 36.5 | 10.2 | 2.4 | 23.6 | ||
| MRT0−∞(h) | 17.8 | 6.8 | 38.1 | 16.3 | 6.3 | 38.8 | 15.1 | 3.2 | 21.3 | ||
| Vz/F (L) | 33.3 | 13.4 | 40.2 | 35.9 | 15.5 | 43.0 | 29.3 | 8.3 | 28.3 | ||
| CL/F (L/h) | 2.04 | 0.86 | 42.2 | 2.71 | 1.90 | 70.1 | 2.19 | 1.09 | 50.0 | ||