Klin Farmakol Farm. 2005;19(2):124-127

Molecular mechanisms of action of antiandrogen bicalutamide

Jan Bouchal¹, Karl R. N. Baumforth², Michaela Šváchová¹, Paul G. Murray², Erwin von Angerer³, Zdeněk Kolář¹

¹ Laboratoř molekulární patologie a Ústav patologie, LF UP, Olomouc

² Institute for Cancer Studies, University of Birmingham, Velká Británie

³ Institut für Pharmazie, Universität Regensburg, Německo

Androgen deprivation is currently the only effective systemic therapy available for metastatic prostate cancer. Monotherapy by antiandrogens represents for some patients an alternative to castration with respect to lower incidence of side effects. Advantages of antiandrogen bicalutamide include good tolerance, minimal side effects and retention of libido and sexual potency. We review the current knowledge on molecular mechanisms of bicalutamide action and discuss our results regarding telomerase activity, p53 pathway and apoptosis. In particular, the finding of activation of p53 pathway and apoptosis by higher doses of bicalutamide can lead to discussion on their usage in therapy of androgen sensitive carcinomas. Doses of bicalutamide higher than 150 mg daily are not clinically used now because they do not further decrease the levels of prostate specific antigen in comparison to castration. However, doses up to 600 mg daily are well tolerated and with respect to the discussed effects of bicalutamide, these higher doses of bicalutamide could be of bring benefit for patients with androgen sensitive carcinomas.

Keywords: Key words: bicalutamide, telomerase, p53, prostate cancer.

Published: January 1, 2006  Show citation