Pipendoxifene -: Treatment of breast cancer -: Estrogen receptor modulator

Breast cancer is the most commonly diagnosed malignancy and the second cause of death in women. In addition to environmental factors, genetic factors appear to play a major role in the development of breast cancer and the risk is high in those individuals with a history of the disease among relatives. Because breast cancer is hormonally dependent and requires low levels of circulating estrogen to thrivel, hormonal manipulation to block estrogen-stimulated growth can be an effective treatment against certain forms of breast carcinoma. Available therapies to reduce the detrimental effects of prolonged exposure to estrogen include antiestrogens (also called selective estrogen receptor modulators[SERMs]), nonsteroidal SERMs and selective estrogen enzyme modulators (SEEMs). Although several SERMs with distinct agonist and antagonist pharmacological profiles have been discovered in the last decade the search continues for compounds with increasingly selective profiles. Pipendoxifene is a a new 2-phenyl indole SERM that exhibits an excellent preclinical pharmacological profile and was selected for further development as a treatment for metastatic breast cancer.