Analogs of Cabergoline Lessen Side Effects (20120228, Dr. Peter Dosa)

Technology No. 20120228
IP Status: Issued US Patent; Application #: 14/443,576

Cabergoline Analogs without 5-HT2B Agonism

Analogs of cabergoline have been developed that have little or no agonism to the 5-HT2B receptor. Specifically, the analogs incorporate two novel side chain modifications, which appear to bypass the negative side effects, cardiac valve regurgitation (CVR), of the parent molecule. This technology has the potential to be a safe and effective treatment for sexual dysfunction, without causing the harm associated with other sexual dysfunction medications.

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Treatment for Parkinson’s Disease, Cushing’s Disease and Sexual Dysfunction

Cabergoline is a prescription drug used to lower levels of the prolactin hormone. Clinically, it is used to treat prolactinomas, Parkinson’s disease, Cushing’s disease, and male patients suffering from sexual dysfunction. However, clinical use decreased in 2007 when studies from the New England Journal of Medicine implicated cabergoline in causing cardiac valve regurgitation (CVR). This potentially fatal complication is associated with drugs that are 5-HT2B agonists. There exists a need for safe analogs of cabergoline that do not have this dangerous effect.

BENEFITS AND FEATURES OF CABERGOLINE:

  • Novel cabergoline side chain modifications bypass potentially fatal side effects
  • Treats patients suffering from male sexual dysfunction; lowers an elevated level of prolactin, which is a risk factor
Researchers
Peter Dosa, PhD
Research Assistant Professor, Department of Medicinal Chemistry; Associate Program Director, Institute for Therapeutics Discovery and Development (ITDD)
External Link (www.pharmacy.umn.edu)
Suck Won Kim, MD
Professor Emeritus, Department of Psychiatry
Michael Walters, PhD
Research Associate Professor, Department of Medicinal Chemistry; Director - Lead and Probe Discovery Core, Institute for Therapeutics Discovery and Development (ITDD)
External Link (www.pharmacy.umn.edu)

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