Table 1.
Pharmacodynamic/pharmacokinetic parameters of PARP inhibitors in solid tumors.
Drug | Cmax (ng/mL)(25) | AUC (ng/mL·h)(25) | Mean T1/2 (h)(25) | PARP-1 Inhibition IC50 (nM)(24) |
PARP Inhibition IC50* (nM) in PC(18) |
---|---|---|---|---|---|
Olaparib | 5700~9500 | 33300~62100 | 6.52~11.9 | 1.94 | 18 |
Niraparib | 1399~2071 | 19540~27852 | 36.2~36.45 | / | / |
Rucaparib | 1940~2650 | 16900~47507 | 12.6 | 1.98 | 18 |
Talazoparib | 16.4~32.84 | 208~244 | 50.0~50.73 | 0.57 | 11 |
* PARP inhibition in DU145 PC cell line.