CASODEX(TM) (BICALUTAMIDE) - OVERVIEW OF A NEW ANTIANDROGEN DEVELOPEDFOR THE TREATMENT OF PROSTATE-CANCER

Casodex(TM) (bicalutamide, Zeneca Ltd), has been developed for prostat e cancer therapy. Its preclinical, pharmacokinetic, pharmacodynamic, c linical efficacy and tolerability data are described. Casodex is a pot ent and specific nonsteroidal 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 pr ostatic acid phosphatase: comparable with castration. This dose was, t herefore, evaluated initially as monotherapy and later as a component of maximal androgen blockade. Using prostate specific antigen as an en d point, Casodex 150 mg daily was well-tolerated with demonstrable evi dence 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 m onotherapy appeared to be equivalent to castration in terms of time to death (data immature). Casodex was well-tolerated. In combination tre atment, Casodex at 50 mg daily was at least as effective as 750 mg flu tamide (Eulexin(TM), Schering-Plough International) with respect to ti me to treatment failure, equivalent in terms of survival, and better t olerated with respect to diarrhoea. In conclusion, Casodex is a good o ption for the antiandrogen component of maximal androgen blockade.