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Antiandrogens: a summary review of pharmacodynamic properties and tolerability in prostate cancer therapy.

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This article provides a summary of the pharmacodynamic properties of major antiandrogens as well as an extensive review of their tolerability. Presently there are two classes of androgen receptor antagonists: the so-called pure, non-steroidal antiandrogens which include flutamide, nilutamide and the

Bicalutamide: a new antiandrogen for use in combination with castration for patients with advanced prostate cancer.

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Maximum androgen blockade, a relatively recent development in the treatment of prostate cancer, combines medical or surgical castration with antiandrogen therapy. A large randomized study comparing the non-steroidal antiandrogen, bicalutamide, with flutamide, each in combination with luteinizing

Tolerability of Nonsteroidal Antiandrogens in the Treatment of Advanced Prostate Cancer.

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This review compares the tolerability profiles of the three currently available nonsteroidal antiandrogens, flutamide, bicalutamide and nilutamide. Pharmacological effects associated with blockade of the androgen receptor are frequent with all three drugs. Gynecomastia and breast pain are seen more

What implications do the tolerability profiles of antiandrogens and other commonly used prostate cancer treatments have on patient care?

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OBJECTIVE Increased awareness of prostate cancer has led to earlier initiation of therapy, and the potential for a longer duration of treatment has led to a stronger emphasis on tolerability. Historically, the mainstay of treatment of hormone-sensitive prostate cancer has been castration-based

[Clinical evaluation of flutamide, a pure antiandrogen, in prostatic cancer phase II dose-finding study].

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The phase II study of flutamide, a pure anti-androgen, was performed to estimate the clinical doses on 165 hormone untreated or treated patients with prostatic cancer. The hormone-untreated patients were given orally flutamide of 90, 375, 750 or 1,125 mg/day in three divided doses daily for 12

Which is the optimal antiandrogen for use in combined androgen blockade of advanced prostate cancer? The transition from a first- to second-generation antiandrogen.

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Many physicians use combined androgen blockade in the form of a luteinizing hormone-releasing hormone analog or bilateral orchiectomy in combination with a non-steroidal antiandrogen to offer patients a potentially more effective treatment than castration alone. Three non-steroidal anti-androgens

Flutamide: an antiandrogen for advanced prostate cancer.

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Flutamide is a nonsteroidal pure antiandrogen that acts by inhibiting the uptake and/or binding of dihydrotestosterone to the target cell receptor, thus interfering with androgen action. Flutamide is well absorbed orally and extensively metabolized; its active metabolite, 2-hydroxyflutamide, is

Efficacy and safety of combined androgen blockade with antiandrogen for advanced prostate cancer.

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Combined androgen blockade (cab) is a promising treatment modality for prostate cancer (pca). In the present meta-analysis, we compared the efficacy and safety of first-line cab using an antiandrogen (aa) with castration monotherapy in patients with advanced

Steroid hormones and Tourette's syndrome: early experience with antiandrogen therapy.

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We report here the first use in Tourette's syndrome of the nonsteroidal androgen receptor blocking agent flutamide. One man and one woman underwent open trials of the medication, and a second man participated in a placebo-controlled, double-blind crossover trial. Improvement in tic symptoms ranged

Enzalutamide: a novel antiandrogen for patients with castrate-resistant prostate cancer.

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Enzalutamide (MDV3100, Xtandi, Medivation\Astellas) is an oral inhibitor of androgen receptor signaling that blocks androgen receptor interaction, inhibits translocation of the androgen receptor to the nucleus, impairs androgen receptor binding to DNA, and inhibits coactivator recruitment and

Efficacy of peripheral androgen blockade in prostate cancer patients with biochemical failure after definitive local therapy: results of Cancer and Leukemia Group B (CALGB) 9782.

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BACKGROUND The treatment for prostate cancer patients with biochemical failure after local therapy remains controversial. Peripheral androgen blockade using a combination of a 5-alpha reductase inhibitor and an antiandrogen may allow control of the prostate-specific antigen (PSA). Because

Flutamide versus orchidectomy in the treatment of metastatic prostate carcinoma.

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OBJECTIVE To compare in a randomized clinical trial the therapeutic efficacy of the nonsteroidal antiandrogen flutamide 250 mg tid to testicular androgen suppression by orchidectomy in patients with metastatic prostate cancer. METHODS Between 1989 and 1991, 104 patients aged 74 +/- 8 years with

Complete androgen blockade as treatment for advanced prostate cancer: clinical response and side-effects.

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Treatment of advanced prostatic cancer is currently based on hormonal manipulation. In 1982 Labrié supported a new concept of hormonal treatment based on complete androgen blockade. The objective of this study was to evaluate the effects of total androgen suppression, achieved by the combination of

Flutamide in treatment of benign prostatic hypertrophy.

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A multicenter, randomized, double-blind study was undertaken to evaluate the efficacy of the antiandrogen flutamide in treating patients with urinary obstruction caused by benign prostatic hypertrophy (BPH). Patients were randomized to either flutamide (750 mg/d) or a placebo. Prostate size

[The role of bicalutamide in the treatment of prostate cancer].

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Bicalutamide is an effective, non-steroidal antiandrogen, suitable for oral, once daily administration. Bicalutamide 50 mg plus LHRHa is at least as effective as flutamide plus LHRHa in terms of survival and time to progression. Monotherapy with bicalutamide 150 mg once daily has similar survival

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