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The Past, Present, and Future of Selective Estrogen Receptor Modulation
Author(s) -
JORDAN V. CRAIG
Publication year - 2001
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1111/j.1749-6632.2001.tb04004.x
Subject(s) - raloxifene , selective estrogen receptor modulator , tamoxifen , osteoporosis , estrogen receptor , medicine , estrogen receptor alpha , antiestrogen , breast cancer , estrogen , toremifene , pharmacology , bioinformatics , endocrinology , cancer , biology
A bstract : The recognition of selective estrogen receptor modulation in the mid‐1980s provided a unique opportunity to develop multifunctional drugs. Tamoxifen, the first selective estrogen receptor modulator (SERM), is the first antiestrogen to be tested successfully for the prevention of breast cancer in high‐risk women. However, the recognition that SERMs maintain bone density and lower circulating cholesterol suggested that the prevention of osteoporosis and coronary heart disease would be beneficial side effects of tamoxifen treatment. This hypothesis has not been pursued in clinical trial, but an alternate hypothesis, that SERMs could be developed to prevent osteoporosis and potentially reduce the risk of breast cancer, has been pursued with raloxifene. Current molecule modeling of the SERM‐ER complex has identified the reason for the promiscuous estrogen‐like actions of tamoxifen compared with raloxifene. Future studies of the signal transduction pathways of the ER alpha (α)‐ and beta (β)‐SERM complexes hold the promise of new drug discoveries and a menu of preventive medicine in clinical practice.