Casodex (bicalutamide): overview of a new antiandrogen developed for the treatment of prostate cancer.

Casodex TM (bicalutamide, Zeneca Ltd), has been developed for prostate cancer therapy. Its preclinical, pharmacokinetic, pharmacodynamic, clinical efficacy and tolerability data are described. Casodex is a potent and specific non-steroidal antiandrogen. Clinical studies indicated that Casodex is orally bioavailable and well absorbed, with a plasma half-life of around 1 week. A Casodex dose of 50 mg daily decreased prostatic acid phosphatase comparable with castration. This dose was, therefore, evaluated initially as monotherapy and later as a component of maximal androgen blockade. Using prostate specific antigen as an end point, Casodex 150 mg daily was well-tolerated with demonstrable evidence of activity. Casodex 150 mg monotherapy was less effective than castration in terms of efficacy in patients with metastatic disease at entry. However, in patients non-metastatic at entry, Casodex 150 mg monotherapy appeared to be equivalent to castration in terms of time to death (data immature). Casodex was well-tolerated. In combination treatment, Casodex at 50 mg daily was at least as effective as 750 mg flutamide (Eulexin TM , Schering-Plough International) with respect to time to treatment failure, equivalent in terms of survival, and better tolerated with respect to diarrhoea. In conclusion, Casodex is a good option for the antiandrogen component of maximal androgen blockade.