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Specific Androgen Receptor Modulators (SARM's)

Testosterone and dihydroxytestosterone (DHT) are two hormones (androgens) produced in the testes and adrenal glands. Among other activities, these hormones bind to specific receptors in the cells of the prostate. A normal function of this binding is to regulate the growth of the prostate cells, however, in cancer cells this regulation is compromised. The androgens bind to the receptors in cancer cells and contribute to their growth and division.

Anti-androgen molecules have been created, that can enter cells and prevent the binding of testosterone to the receptor proteins. This occurs via the preferential binding of the drug molecule to the androgen receptors. The binding of the drug prevents the androgens from binding and therefore reduces their pro-growth activities.(1)

Bicalutamide(Casodex®)
Flutamide (Eulexin®)
Nilutamide (Nilandron®, Anandron®)

The drugs are frequently used in combination with surgery to cause the maximal reduction in androgen levels.(2) Additional drugs are also being studied for their ability to reduce androgen levels in prostate cancer patients and to overcome the drug resistance seen in some patients. (3)(2)

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Last Modified: 11/18/2011 Print Email Page Share
References for this page:
  1. Nguyen MM, Wang Z. Manipulation of androgens and alterations in the androgen receptor axis in prostate cancer. Minerva Urol Nefrol. 2008 Mar;60(1):15-29. [PUBMED]
  2. Klotz L. Maximal androgen blockade for advanced prostate cancer. Best Pract Res Clin Endocrinol Metab. 2008 Apr;22(2):331-40. [PUBMED]
  3. Chen Y, Clegg NJ, Scher HI. Anti-androgens and androgen-depleting therapies in prostate cancer: new agents for an established target. Lancet Oncol. 2009 Oct;10(10):981-91. [PUBMED]
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