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. 2020 Dec 28;16(1):59–68. doi: 10.1007/s11523-020-00780-4

Table 3.

Pharmacokinetic (PK) data for rucaparib with and without bevacizumab co-administration

PK parameter, mean (±SD) Rucaparib first administration Rucaparib at steady state
Day −7 Day 1 Day 21
Rucaparib
400 mg BID
Rucaparib
500 mg BID
Rucaparib
600 mg BID
Rucaparib
400 mg BID
Rucaparib
500 mg BID
Rucaparib
600 mg BID
Rucaparib
400 mg BID
Rucaparib
500 mg BID
Rucaparib
600 mg BID
n 3 3 3 3 3 3 2a 3 2b
Cmax (µg/mL) 0.7 ± 0.1 0.9 ± 0.6 1.0 ± 0.2
CmaxSS (µg/mL) 2.4 ± 0.2 2.6 ± 0.5 2.6 ± 0.5 2.6 ± 0.9 2.3 ± 0.4 2.5 ± 1.3
Cmin (µg/mL) 0.2 ± 0.1 0.4 ± 0.1 0.3 ± 0.2
CminSS (µg/mL) 1.4 ± 0.3 1.6 ± 0.7 1.4 ± 0.3 1.3 ± 0.4 1.5 ± 0.5 1.6 ± 1.2
Tmax (h) 3.4 ± 0.7 1.9 ± 0.1 3.4 ± 1.2 4.6 ± 2.9 1.7 ± 1.2 3.0 ± 1.0 3.0 ± 1.3 2.0 ± 1.0 5.0 ± 1.4
AUC0–8h (µg/mL*h) 3.4 ± 0.8 4.7 ± 1.9 4.9 ± 1.6
AUCSS (µg/mL*h) 15.5 ± 0.8 16.7 ± 4.6 14.9 ± 2.6 14.8 ± 3.1 14.2 ± 3.2 15.8 ± 9.6
Ctrough (µg/mL)c 1.6 ± 0.1 1.8 ± 0.7 1.6 ± 0.1 1.5 ± 0.3 2.0 ± 0.6 2.1 ± 0.3

AUC0–8h area under the concentration–time curve from zero to 8 hours, BID twice daily, Cmin minimum plasma concentration, Cmax maximum plasma concentration, Ctrough trough concentration, SD standard deviation, SS steady state, Tmax time to Cmax

aPatient 0001-002 was not included in the calculation of the mean of the PK parameters because rucaparib administration was suspended for the whole week before day 21

bPatient 0001-008 was not included in the calculation of the mean of the PK parameters because rucaparib was suspended on day 21 for dose-limiting toxicity

cMean Ctrough is calculated by mediating the rucaparib concentration values on day 1 and 21 of the cycle