Bicalutamide prostate cancer

In the bicalutamide prostate cancer programme, the adjuvant treatment of patients with advanced prostate carcinoma (T1-T4 NO/NX, MO) with bicalutamide (150 mg, once a day) was evaluated. 4052 patients were randomised to bicalutamide with best standard care (either radiation, prostatectomy or watchful waiting ), whereas 4061 patients received a placebo with best standard care. An initial reduction of prostate cancer recurrence, which was observed in an interim analysis, later was not confirmed [219]. As the survival time in the bicalutamide treatment group was decreased, the study was terminated ahead of time. 

Anti-androgen Hutamide, bicalutamide Prostate cancer... 

Boccardo F, Rubagotti A, Barichello M, et al. Bicalutamide monotherapy versus flutamide plus gosrelin in prostate cancer patients Results of an Italian Prostate Cancer Project study. J Clin Oncol 1999 17 2027-2038. 

Monotherapy with flutamide, bicalutamide, and nilutamide is no longer recommended due to decreased survival as compared with patients treated with LHRH agonist therapy or orchiectomy. Antiandrogens are indicated for advanced prostate cancer only when combined with an LHRH agonist (flutamide and bicalutamide]) or orchiectomy (nilutamide). In combination, antiandrogens can reduce the LHRH agonist-induced flare. 

Androgenic Receptors The antagonists of androgenic receptor, flu-tamide, nilutamide and bicalutamide, have the same m-trifluoromethylaniline moiety (Figures 8.73 and 8.74). They are marketed for hormone-dependent prostatic cancer... 

Antiandrogens such as cyproterone acetate (5.54) or the nonsteroidal flutamide (5.55, a substituted anilide) are competitive antagonists on the cytosol receptor. They do not prevent DHT formation rather, they inhibit the nuclear retention of DHT in the prostate. They cause feminization in male fetuses and decrease libido in males. Cyproterone is also an active progestogen. In men, antiandrogens are used commonly in the treatment of prostatic cancer and uncommonly to inhibit sex drive in hypersexuality in women, antiandrogens are used to treat virilization. Bicalutamide (5.56) and nilutamide (5.57) are potent, orally active antiandrogens that may be used in the treatment of metastatic prostate carcinoma. 

The effect of adding finasteride 5 mg/day to high-dose bicalutamide 150 mg/ day has been studied in 41 men with advanced prostate cancer treated over a mean of 3.9 years (21). The serum prostate-specific antigen (PSA) concentration was measured every 2 weeks until disease progression. At the first nadir of PSA, the median fall from baseline was 96.5% a second nadir occurred in 30 of 41 patients, with a median fall of 98.5% from baseline. The median times to each nadir were 3.7 and 5.8 weeks respectively. The median time to treatment failure was 21 months. Adverse effects were minor, including gynecomastia. Sex drive was normal in 17 of 29 men at baseline and in 12 of 24 men at the second PSA nadir, but one-third of the men had spontaneous erections at both times. The authors concluded that finasteride provided additional intracellular androgen blockade when added to bicalutamide. The duration of control was comparable to that achieved with castration, with preserved sexual function in some patients. 

Fradet Y. Bicalutamide (Casodex) in the treatment of prostate cancer. Exp Rev Anticancer Ther 2004 4 37 18. 

Schellhammer PF, Davis JW. An evaluation of bicalutamide in the treatment of prostate cancer, din Prost Cancer 2004 2 213-9. 

Wirth MP, See WA, McLeod DG, Iversen P, Morris T, Carroll K Casodex Early Prostate Cancer Trialists Group. Bicalutamide 150 mg in addition to standard care in patients with localized or locally advanced prostate cancer results from the second analysis of the early prostate cancer program at median followup of 5.4 years. J Urol 2004 172 1865-70. 

Antiandrogens Bicalutamide Flutamide Nilutamide Inhibits the cellular uptake and effects of androgens in advanced, metastatic prostate cancer Nausea vomiting diarrhea decreased sex drive... 

Bicalutamide (8.e) is a drug used to treat certain forms of prostate cancer. The drug is administered in racemic form, and the two enantiomers behave differently in the body. The inactive 5-enantiomer undergoes rapid glucuronidation. The active R-enantiomer is slowly oxidized. Draw likely structures of both metabolites. 

Bicalutamide is approved for combination therapy with ui LH-RH analogue for treatment of advanced prostate cancer. Its response is measured by decreased prostatc-specific antigen levels. Adverse reactions include gynecoma.stia. breast pain, and inhibition of spermatogenesis. There is an mtetaction with coumadin. " ... 

Scher H, Leibertz C, Kelly W, et al. Bicalutamide for advanced prostate cancer The natural history versus treated history of disease. J Clin Oncol 1997 15 2928-2938. 

Bales G, Chodak G. A controlled trial of bicalutamide versus castration inpatients with advanced prostate cancer. Urology 1996 47 38-43. 

Bohl, C.E., Gao, W Miller, D.D., Bell, C.E. and Dalton, J.T. (2005) Structural basis for antagonism and resistance of bicalutamide in prostate cancer. Proceedings of the National Academy of Sciences of the United States of America, 102, 6201-6206. 

Yoshida, T., Kinoshita, H., Segawa, T., Nakamura, E., Inoue, T., Shimizu, Y., Kamoto, T. and Ogawa, O. (2005) Antiandrogen bicalutamide promotes tumor growth in a novel androgen-dependent prostate cancer xenograft model derived from a bicalutamide-treated patient. Cancer Research, 65, 9611-9616. 

Bevacizumab - monoclonal antibody treatment of colorectal cancer Bezafibrate - lipid lowering drug Bicalutamide - chemotherapy of prostate cancer Bisacodyl - stimulant laxative... 

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