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Table 1 Pharmacokinetic parameters for tamoxifen, 4-OHT, and ZB497 following single dose, oral administration

From: Boronic prodrug of 4-hydroxytamoxifen is more efficacious than tamoxifen with enhanced bioavailability independent of CYP2D6 status

  Tamoxifen (1 mg/kg) 4-hydroxytamoxifen (1 mg/kg) ZB497 (1 mg/kg)
tmax (hrs) 2 (Tam) 2 (4-OHT) 2 (4-OHT)
2 (4-OHT) 2 (Endoxifen) 6 (Endoxifen)
t1/2 (hrs) 32.5 (Tam) 31.7 (4-OHT) 39.5 (4-OHT)
22.6 (4-OHT) 19.5 (Endoxifen) 36.5 (Endoxifen)
Cmax (ng/mL) 2.78 (Tam) 3.6 (4-OHT) 114.0 (4-OHT)
0.80 (4-OHT) 5.9 (Endoxifen) 14.4 (Endoxifen)
AUC (ng/mL*h) 160.6 (Tam) 61.5 (4-OHT) 3777.7 (4-OHT)
21.3 (4-OHT) 61.2 (Endoxifen) 767.4 (Endoxifen)