Table 2. Tissue and Plasma PK of Niraparib and Olaparib in OVC134 Ovarian PDX Model.
| PARPi | Tumor PK | Brain PK | Plasma PK | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cmax(μg/g) | tmax(h) | AUC0-last(μg/g·h) | Dose normalizedAUC0-24h (μM·h/mg) | Cmax(μg/g) | tmax(h) | AUC0-last(μg/g·h) | Dose normalizeAUC0-24h (μM·h/mg) | Cmax(μg/mL) | tmax(h) | AUC0-last(μg/mL·h) | Dose normalizedAUC0-24h (μM·h/mg) | |
| Niraparib(50 mg/kg qd 2 days) | 10.80 | 4 | 83.14 | 5.19 | 0.65 | 4 | 8.31 | 0.52 | 3.24 | 4 | 25.50 | 1.59 |
| Olaparib(67mg/kg bid 2 days) | 6.17 | 0.5 | 9.73 | 0.33 | 0.52 | 0.5 | 0.45 | 0.02 | 15.04 | 0.5 | 15.59 | 0.53 |
| Dose normalizedAUCnir/ola ratio | - | - | - | 16 | - | - | - | 34 | - | - | - | 3 |
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 AUC0–12h; nir=niraparib; ola=olaparib.