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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)

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BMC Cancer

ISSN: 1471-2407

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