(NEW YORK, NY, June 4, 2011) Researchers at Columbia University Medical Center are honing in on the development of what may be the first non-steroidal, oral contraceptive for men. Tests of low doses of a compound that interferes with retinoic acid receptors (RARs), whose ligands are metabolites of dietary vitamin A, showed that it caused sterility in male mice.
Earlier results of the experiments using this RAR antagonist were published in the June 1st issue of Endocrinology, and an abstract extending the studies to longer drug delivery periods is scheduled for the Late Breaking Oral Session of ENDO 2011: The 93rd Annual Meeting & Expo in Boston, Massachusetts.
(The abstract, titled Meeting Men's Contraceptive NeedsLong-Term Oral-Administered Retinoic Acid Receptor Antagonist Inhibits Spermatogenesis in Mice with a Reversible and Rapid Recovery, will be presented at the session by first author Sanny S. W. Chung, Ph.D., on Saturday, June 4, 11:15 a.m., Room 157ABC, Boston Convention & Exhibition Center).
The researchers found that low doses of the drug stopped sperm production with no apparent side effects. And crucial for a contraceptive, normal fertility was restored soon after drug administration was terminated.
Earlier research had led the investigators to the discovery that manipulating the retinoid receptor pathway could interfere with the process of spermatogenesis, which is necessary for sperm production.
Scientists have known for almost 100 years that depriving an animal of dietary vitamin A causes male sterility. While investigating targeted loss of function of the gene encoding one of the RARs, RARalpha, which results in male infertility, senior author Debra J. Wolgemuth, Ph.D., ran across a paper by Bristol-Myers Squibb on a compound that was being tested for the treatment of skin and inflammatory diseases. The compound seemed to cause changes in the testis similar to the mutation that she an
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Columbia University Medical Center