Dr. med. Dirk Manski

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Bicalutamide: Hormonal Treatment of Advanced Prostate Cancer

Indications for Bicalutamide

Anti-androgen hormone treatment of prostate cancer with bicalutamide is a therapeutic option against prostate cancer in the following situations:

Mechanism of Action of Bicalutamide

Bicalutamide is a nonsteroidal anti-androgen drug, which shows competitive antagonism in relation to the androgen receptor. The central inhibition of androgen receptors leads to an increase in LH, testosterone and estrogen.

Pharmacokinetics of Bicalutamide

Side Effects of Bicalutamide

Interactions with Bicalutamide

Increased effect of warfarin (displacement from the plasma protein binding), terfenadine or cisapride (inhibition of cytochromes).

Contraindications for Bicalutamide

Increased liver enzymes warrant dose reduction and regular laboratory monitoring. Bicalutamide should be stopped in progressive elevation of liver transaminases without evidence of liver metastases. Further contraindications are allergy, bicalutamide has no indications in women and children.

Dosage of Bicalutamide

In the EU and some other countries, two dosages of bicalutamide for oral administration are approved: 50 mg/day or 150 mg/day. In the USA, the usage of bicalutamide is only approved for the 50 mg indication:

150 mg/day bicalutamide is recommended for antiandrogenic monotherapy (as an alternative to treatment with GnRH modulators or surgical castration).

50 mg/day bicalutamide is sufficient to prevent the testosterone flare at the beginning of GnRH agonist therapy or in combination with GnRH agonist treatment (maximal androgen blockade, MAB).

Index: 1–9 A B C D E F G H I J K L M N O P Q R S T U V W X Y Z


Anderson 2003 ANDERSON, J.: The role of antiandrogen monotherapy in the treatment of prostate cancer.
In: BJU Int
91 (2003), Nr. 5, S. 455–61.

Diamond u.a. 2004 DIAMOND, T. H. ; HIGANO, C. S. ; SMITH, M. R. ; GUISE, T. A. ; SINGER, F. R.: Osteoporosis in men with prostate carcinoma receiving androgen-deprivation therapy: recommendations for diagnosis and therapies.
In: Cancer
100 (2004), Nr. 5, S. 892–9.

Fradet u.a. 2007 FRADET, Yves ; EGERDIE, Blair ; ANDERSEN, Morten ; TAMMELA, Teuvo L J. ; NACHABE, Mahmoud ; ARMSTRONG, Jon ; MORRIS, Thomas ; NAVANI, Sunil: Tamoxifen as prophylaxis for prevention of gynaecomastia and breast pain associated with bicalutamide 150 mg monotherapy in patients with prostate cancer: a randomised, placebo-controlled, dose-response study.
In: Eur Urol
52 (2007), Jul, Nr. 1, S. 106–114.

Loblaw u.a. 2004 LOBLAW, D. A. ; MENDELSON, D. S. ; TALCOTT, J. A. ; VIRGO, K. S. ; SOMERFIELD, M. R. ; BEN-JOSEF, E. ; MIDDLETON, R. ; PORTERFIELD, H. ; SHARP, S. A. ; SMITH, T. J. ; TAPLIN, M. E. ; VOGELZANG, N. J. ; WADE, Jr. ; BENNETT, C. L. ; SCHER, H. I.: American Society of Clinical Oncology recommendations for the initial hormonal management of androgen-sensitive metastatic, recurrent, or progressive prostate cancer.
In: J Clin Oncol
22 (2004), Nr. 14, S. 2927–41.

Miyamoto u.a. 2004 MIYAMOTO, H. ; MESSING, E. M. ; CHANG, C.: Androgen deprivation therapy for prostate cancer: current status and future prospects.
In: Prostate
61 (2004), Nr. 4, S. 332–53.

Perdona u.a. 2005 PERDONA, S. ; AUTORINO, R. ; DPLACIDO, S. ; D’ARMIENTO, M. ; GALLO, A. ; DAMIANO, R. ; PINGITORE, D. ; GALLO, L. ; DSIO, M. ; BIANCO, A. R. ; DLORENZO, G.: Efficacy of tamoxifen and radiotherapy for prevention and treatment of gynaecomastia and breast pain caused by bicalutamide in prostate cancer: a randomised controlled trial.
In: Lancet Oncol
6 (2005), Nr. 5, S. 295–300.

Sieber u.a. 2004 SIEBER, P. R. ; KEILLER, D. L. ; KAHNOSKI, R. J. ; GALLO, J. ; MCFADDEN, S.: Bicalutamide 150 mg maintains bone mineral density during monotherapy for localized or locally advanced prostate cancer.
In: J Urol
171 (2004), Nr. 6 Pt 1, S. 2272–6, quiz 2435

Smith u.a. 2004b SMITH, M. R. ; GOODE, M. ; ZIETMAN, A. L. ; MCGOVERN, F. J. ; LEE, H. ; FINKELSTEIN, J. S.: Bicalutamide monotherapy versus leuprolide monotherapy for prostate cancer: effects on bone mineral density and body composition.
In: J Clin Oncol
22 (2004), Nr. 13, S. 2546–53.

Tyrrell u.a. 2004 TYRRELL, C. J. ; PAYNE, H. ; TAMMELA, T. L. ; BAKKE, A. ; LODDING, P. ; GOEDHALS, L. ; VAN ERPS, P. ; BOON, T. ; VAN DBEEK, C. ; ANDERSSON, S. O. ; MORRIS, T. ; CARROLL, K.: Prophylactic breast irradiation with a single dose of electron beam radiotherapy (10 Gy) significantly reduces the incidence of bicalutamide-induced gynecomastia.
In: Int J Radiat Oncol Biol Phys
60 (2004), Nr. 2, S. 476–83.

Widmark u.a. 2003 WIDMARK, A. ; FOSSA, S. D. ; LUNDMO, P. ; DAMBER, J. E. ; VAAGE, S. ; DAMBER, L. ; WIKLUND, F. ; KLEPP, O.: Does prophylactic breast irradiation prevent antiandrogen-induced gynecomastia? Evaluation of 253 patients in the randomized Scandinavian trial SPCG-7/SFUO-3.
In: Urology
61 (2003), Nr. 1, S. 145–51.

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