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THE EFFECT OF FOOD ON THE PHARMACOKINETICS OF THE BICALUTAMIDE (‘CASODEX’) ENANTIOMERS

✍ Scribed by I. D. COCKSHOTT; S. D. OLIVER; J. J. YOUNG; K. J. COOPER; D. C. JONES

Publisher
John Wiley and Sons
Year
1997
Tongue
English
Weight
132 KB
Volume
18
Category
Article
ISSN
0142-2782

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✦ Synopsis

Casodex' (bicalutamide) is an orally active, non-steroidal, pure antiandrogen; it is a racemate with antiandrogenic activity residing predominantly in the (R)-enantiomer. Healthy male volunteers (n=15) were administered single oral doses of bicalutamide (50 mg) after food and after fasting as part of a three-treatment, three-period, randomized cross-over study, with a 9 week washout. After fasting, plasma concentrations of (R)-bicalutamide were much higher than those of (S)-bicalutamide; the mean (R)-enantiomer C max (734 ng mL 71 ) was about nine times higher than the (S)enantiomer value (84 ng mL 71 ). The corresponding t max values were 19 and 3 h for (R)and (S)-bicalutamide respectively. Elimination of (R)-bicalutamide from plasma was monoexponential and slow (t 1/2 =5´8 d). Elimination of (S)-bicalutamide was biphasic in some volunteers but monophasic in others (terminal t 1/2 =1´2 d; n=11). There was no signi®cant eect of food on AUC, t max , or t 1/2 data for either enantiomer. The observed slightly higher values of C max for (R)-bicalutamide (14%) and (S)-bicalutamide (19%), when dosing with food, achieved statistical signi®cance. However, dierences of this magnitude are unlikely to be of any clinical relevance. These data indicate that `Casodex' can be taken without reference to meal-times; this may be of particular relevance for its indication in a disease of the elderly. &1997 by John Wiley & Sons, Ltd.

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