Clinical Pharmacokinetics of the Antiandrogens and Their Efficacy in Prostate Cancer

  title={Clinical Pharmacokinetics of the Antiandrogens and Their Efficacy in Prostate Cancer},
  author={Ch. Mahler and Johan A. Verhelst and Louis J. Denis},
  journal={Clinical Pharmacokinetics},
Prostatic cancer is the second most common cause of cancer death in males. Treatment by radical prostatectomy and radiotherapy is useful in the early stages of the disease. Whenever metastases occur, patients are usually treated by surgical (orchidectomy) or medical [gonadotropin releasing hormone (GnRH) analogue] castration. This form of treatment is, however, associated with unwanted adverse effects, such as flushing, loss of libido and potency and all patients ultimately escape therapy after… 

The role of antiandrogen monotherapy in the treatment of prostate cancer

Current data are inadequate to draw conclusions on the comparative efficacy of flutamide and castration, while nilutamide is not licensed for monotherapy, and bicalutamide has a more favourable side‐effect profile than the other antiandrogens and is more likely to promote compliance.

Non-steroidal anti-androgens in prostate cancer - current treatment practice

The benefits of NSAA in monotherapy, intermittent or neoadjuvant therapy are not clear at present, and better designed, larger cohort clinical trial may be necessary to clarify the confusion.

An evaluation of bicalutamide in the treatment of prostate cancer

Mature survival data from men with previously untreated, locally-advanced prostate cancer reveal that bicalutamide monotherapy provides survival benefits that do not differ significantly from castration, while offering important advantages with respect to the maintenance of physical capacity and sexual interest.

Androgen deprivation therapy for the treatment of prostate cancer: a focus on pharmacokinetics

Second-line agents, traditionally reserved for CRPC, are being studied in metastatic castrate-sensitive prostate cancer, and may offer practice-changing evidence supporting their use.

Retrospective Analysis of Clinical Efficacy of Luteinizing Hormone-Releasing Hormone Antagonist as Compared to Agonists with Combined AntiAndrogen Blockade ( CAB ) in Advanced Prostate Cancer

In this retrospective analysis, there did not find a significant difference in PSA PFS between an LHRH antagonist and agonists when used with Combined Anti-androgen Blockade (CAB).

Bicalutamide (Casodex®) in the treatment of prostate cancer

  • Y. Fradet
  • Medicine
    Expert review of anticancer therapy
  • 2004
Nonsteroidal antiandrogens such as bicalutamide (Casodex®) offer an effective alternative to castration with potential quality-of-life benefits in men with prostate cancer.

Recent developments in antiandrogens and selective androgen receptor modulators

Male breast adenocarcinoma in a prostate cancer patient following prolonged anti-androgen monotherapy.

This case report illustrates that PrCa patients receiving anti-androgen monotherapy may be at risk of BrCa, in the event of the concomitant presence of other genetically-determined predisposing factors, and indicates the importance of exercising caution against indiscriminate and prolonged use of anti- androgens monotherapy in patients with risk factors for male BrCa.



Defining the role of antiandrogens in the treatment of prostate cancer.

A controlled trial of leuprolide with and without flutamide in prostatic carcinoma.

Treatment with le uprolide and flutamide is superior to treatment with leuprolide alone in patients with advanced prostate cancer, and Symptomatic improvement was greatest during the first 12 weeks of the combined androgen blockade.

New approach in the treatment of prostate cancer: Complete instead of partial withdrawal of androgens

The present data show that complete withdrawal of androgens by combined hormonal therapy with the LHRH agonist (or castration) and a pure antiandrogen leads to a positive objective response in more than 95% of cases as opposed to 60%‐70% as reported by many groups using the previous partial hormonal therapy.

Withdrawal phenomenon with the antiandrogen casodex.

  • P. Nieh
  • Medicine
    The Journal of urology
  • 1995
The observations in this report would suggest that the initial and sustained exposure to an antiandrogen is the more important factor in the withdrawal phenomenon rather than the low androgen environment alone that occurs with initial luteinizing hormone-releasing hormone analogue monotherapy, orchiectomy or combination lute inizing hormones-re releasing hormone analogue and anti androgen.

Cyproterone acetate–‐mechanism of action and clinical effectiveness in prostate cancer treatment

The usefulness of CPA in the management of prostate cancer, especially in total androgen blockade regimens, recently has been challenged by findings in experimental systems that suggest that CPA is androgenic.

Ocular toxicity of Anandron in patients treated for prostatic cancer.

The availability of a compound such as flutamide that has no side effect other than those due to hypoandrogenicity should greatly facilitate compliance by the patients and the success of the treatment of prostatic cancer.

Indications for Antiandrogen Treatment in Prostate Cancer

The modern concept of antiandrogenic activity in prostate cancer has its origin in the development of cyproterone acetate (CPA) in 1962. Antiandrogens were first defined by Dorfman as substances that

Combination Therapy with Flutamide: The Therapy of Choice from Early to Advanced Stages of Prostate Cancer

A high rate of positive responses is already quite impressive since, as will be discussed later, testicular androgens account for only 60% of total androgens in 65-year-old men, thus leaving approximately 40% of androgens free to continue to stimulate prostate cancer.