Selective Estrogen-Receptor Modulators for Primary Prevention of Breast Cancer
2005; Lippincott Williams & Wilkins; Volume: 23; Issue: 8 Linguagem: Inglês
10.1200/jco.2005.11.005
ISSN1527-7755
AutoresCarol J. Fabian, Bruce F. Kimler,
Tópico(s)Cancer Risks and Factors
ResumoSelective estrogen receptor modulators (SERMs) impact a variety of biologic processes regulated by activated estrogen receptor (ER). Depending on the target tissue, physiologic conditions, and their structure, SERMs may exhibit either estrogen antagonist or estrogen agonist effects. SERMs have a long history in the treatment of breast cancer, based on estrogen antagonist activity in ER-positive breast cancer cells. Beginning with tamoxifen, SERMs have moved to the prevention arena, where their partial estrogen effects may provide other organ benefits, particularly for postmenopausal women. It is because of these partial estrogen agonist effects on organs such as the bone, vagina, CNS, and cardiovascular system that SERMs are likely to remain preferable to pure antiestrogens as primary breast cancer prevention agents in the context of total women’s health. The ideal SERM should function as an antiestrogen in the breast and uterus and a partial estrogen agonist in skeletal, cardiovascular, CNS, gastrointestinal tract, and vagina. Further, this ideal SERM should be devoid of procoagulant effects and should not be associated with an increase in perimenopausal symptoms. Although several generations of SERMs have been developed, the ideal SERM for prevention remains elusive. We will review progress to date for SERMs as single agents and potential for combination therapy in the future. BIOLOGY BEHIND THE MULTIFACETED ACTION OF SERMs
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