Table 3. Tissue Distribution of Niraparib and Olaparib.
| Model | PARPi | Tumor AUC0-last(μg/g·h) | Brain AUC0-last(μg/g·h) | Bone MarrowAUC0-last (μg/g·h) | Plasma AUC0-last(μg/mL·h) | AUC0-lastTumor:Plasma | AUC0-lastBrain:Plasma | AUC0-lastTumor:Bone Marrow |
|---|---|---|---|---|---|---|---|---|
| MDA-MB-436 | Niraparib(75 mg/kg qd 5 days) | 213.96 | 18.72 | 2.82 | 65.08 | 3.3 | 0.29 | 75.9 |
| Olaparib(100 mg/kg qd 5 days) | 7.59 | 0.34 | LLOQ | 11.28 | 0.7 | 0.03 | ND | |
| OVC134 | Niraparib(50 mg/kg qd 2 days) | 83.14 | 8.31 | - | 25.50 | 3.3 | 0.33 | - |
| Olaparib(67 mg/kg bid 2 days) | 9.73 | 0.45 | - | 15.59 | 0.6 | 0.03 | - |
AUC0–last=area under the plasma concentration–time curve from 0 to the time of the last PK sampling post-dose, for niraparib AUC0–last is AUC0–24h, for olaparib AUC0–last is AUC0–24h in MDA-MB-436 model and AUC0–12h in OVC134 model; LLOQ=lower limit of quantification; ND= not determined.