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. 2021 May 1;110(2):432–442. doi: 10.1002/cpt.2227

Table 1.

Predicted Kp,uu,brain using method 1, i.e., from in vitro ER

Compound Exp. ERTRQ(‐) ERTRQ(+) ERTRQ(‐) ‐ ERTRQ(+) REF Kp,uu,brain,pred(method 1)

Kp,uu,brain,obs

(CI95%)

P/O
Individual Mean ± SD
Verapamil 1 2.94 0.76 2.18 2.20 0.17 0.17 ± 0.03 0.16 (0.13–0.20) 1.02
2 2.97 0.76 2.21 2.39 0.16
3 3.59 0.71 2.88 2.37 0.13
4 3.73 0.83 2.90 1.32 0.21
N‐desmethyl loperamide 1 18.28 0.86 17.42 0.97 0.056 0.043 ± 0.018 0.046 (0.035–0.057) 0.92
2 26.21 0.82 25.39 1.83 0.021
3 55.00 0.98 54.02 0.30 0.058
4 119.43 0.82 118.61 0.23 0.035
Metoclopramide 1 1.87 0.70 1.17 0.30 0.74 0.74 ± 0.08 0.57 (0.46–0.67) 1.30
2 1.79 0.92 0.87 0.36 0.76
3 3.56 1.03 2.53 0.24 0.63
4 2.98 1.68 1.30 0.18 0.81

CI95%, 95% confidence interval; ER, efflux ratio; Exp., experiment; Kp,uu,brain, unbound brain‐to‐plasma concentration ratio; P/O, predicted/observed Kp,uu,brain ratio; REF, relative expression factor (measured by targeted proteomics); TRQ, tariquidar.