Selective estrogen receptor modulators as a new therapeutic drug group: concept to reality in a decade.
This article provides an overview of the historical development, current research, clinical benefits, and potential future applications of the selective estrogen receptor modulators (SERMs), tamoxifen and raloxifene. The understanding of the mechanism of action of SERMs led not only to the development of tamoxifen, the first widely used antiestrogen for breast cancer treatment, but also to its application as a chemopreventive agent. The SERM principle of antiestrogenic actions in the breast but estrogenlike actions in bone is reviewed in clinical practice through analysis of the current applications and the potential for expanding the role of SERMs. The current view of the molecular mechanism of SERM action is summarized to identify potential target sites for future research. The clinical success of tamoxifen and raloxifene for the prevention and treatment of breast cancer and osteoporosis, respectively, has encouraged the development of a range of new agents that target breast cancer, osteoporosis, coronary heart disease, and endometrial safety.
Gajdos
Csaba
C
Robert H. Lurie Comprehensive Cancer Center, Northwestern University Medical School, 303 E. Chicago Avenue, Chicago, IL 60611, USA.
Jordan
V Craig
VC
D016588:Anticarcinogenic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000401:mortality / Q000473:pathology; D002934:Cinnamates / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D015195:Drug Design; D005544:Forecasting; D006801:Humans; D008967:Molecular Biology; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D011759:Pyrrolidines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D020849:Raloxifene Hydrochloride / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D020845:Selective Estrogen Receptor Modulators / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D013267:Stilbenes / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D013764:Tetrahydronaphthalenes / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D017312:Toremifene / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D016896:Treatment Outcome
D016588:Anticarcinogenic Agents; D000972:Antineoplastic Agents, Phytogenic; D002934:Cinnamates; D010880:Piperidines; D011759:Pyrrolidines; D020845:Selective Estrogen Receptor Modulators; D013267:Stilbenes; D013764:Tetrahydronaphthalenes; D013876:Thiophenes; D013629:Tamoxifen; C087550:3-(4-(1,2-diphenylbut-1-enyl)phenyl)acrylic acid; C111332:Lasofoxifene; C012121:ritetronium; C071362:idoxifene; D020849:Raloxifene Hydrochloride; D017312:Toremifene; C115121:LY 353381