Selective estrogen receptor modulators (SERMS) and their roles in breast cancer prevention.
Tamoxifen has not only proved to be a valuable treatment for estrogen receptor (ER)-positive breast cancer, but is also a pioneering medicine for chemoprevention in high-risk pre- and postmenopausal women. Insights into the pharmacology and toxicology of tamoxifen have led to the recognition of selective ER modulators (SERMs) with estrogen-like actions in maintaining bone density and in lowering circulating cholesterol, but antiestrogenic actions in the breast. Raloxifene, a related SERM, is now available to treat osteoporosis and is also being tested as a preventive for breast cancer and coronary heart disease. Emerging knowledge about the action of SERMs will provide clues for the design of mechanism-based medicines.
Park
Woo-Chan
WC
Lynn Sage Breast Cancer Research Program, Robert H. Lurie Comprehensive Cancer Center, Olson Pavilion 8258, 303 E. Chicago Avenue, Chicago, IL 60611, USA.
Jordan
V Craig
VC
D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy / Q000378:metabolism* / Q000517:prevention & control*; D002986:Clinical Trials as Topic; D005260:Female; D006801:Humans; D010024:Osteoporosis / Q000517:prevention & control; D020849:Raloxifene Hydrochloride / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D011960:Receptors, Estrogen / Q000378:metabolism; D020845:Selective Estrogen Receptor Modulators / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use*; D013629:Tamoxifen / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; D013629:Tamoxifen; D020849:Raloxifene Hydrochloride