Table 3.
Brain Penetration of PARP inhibitors in Mice.
| Dose of Compound | AUC1-4h (ng/ml*h or ng/g*h) |
Plasma(ng/mL) or Brain(ng/g) Concentration |
|||
|---|---|---|---|---|---|
| 1 h | 2 h | 4 h | |||
| Pamiparib 10 mg/kg, p.o. | Plasma | 4470 | 3527 | 1333 | 707 |
| Brain | 820 | 613 | 252 | 135 | |
| Brain/Plasma (%) | 18% | 17% | 19% | 19% | |
| Talazoparib 3 mg/kg, p.o. | Plasma | 5628 | 3276 | 2115 | 817 |
| Brain | 85 | 16 | 34 | 26 | |
| Brain/Plasma (%) | 2% | 0% | 2% | 3% | |
| Olaparib 50 mg/kg, p.o. | Plasma | 3160 | 3273 | 771 | 366 |
| Brain | 56 | 45 | 17 | 9 | |
| Brain/Plasma (%) | 2% | 1% | 2% | 2% | |
| Niraparib 50 mg/kg, p.o. | Plasma | 20,214 | 7385 | 7021 | 5990 |
| Brain | 1849 | 428 | 549 | 812 | |
| Brain/Plasma (%) | 9% | 6% | 8% | 14% | |