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F O R P H Y S I C I A N S – resources
Selective Estrogen Receptor Modulators
Other SERMs
Other SERMs currently being investigated in clinical trials are droloxifene and idoxifene, triphenyethylene derivatives. Droloxifene is currently being evaluated as a treatment for breast cancer as well as for the prevention of postmenopausal osteoporosis. It has a greater affinity for the estrogen receptor than tamoxifen and has less agonist and more antagonist activity at the uterus (32). In the breast tissue droloxifene has antiestrogenic effect and preserves bone density by reducing the formation of osteoclasts in the bone marrow through apoptosis of mononuclear precursors (33).
Idoxifene is also being studied for the treatment of advanced breast cancer. Idoxifene has an estrogen receptor binding affinity that is twice that of tamoxifen, but a less potent antiestrogen (34).
SERMs are a class of drugs that help to reduce the risk of osteoporosis and breast cancer and improve serum lipids. These medications have obvious advantages over HRT however more research and development is needed before this therapy becomes mainstay. Many women who initiate HRT commonly cite relief from menopausal symptoms such as hot flushes and night sweats. The currently available SERMs do not alleviate such symptoms and may even exacerbate some limiting their use. There is also no data to address long-term safety and efficacy questions. At this time HRT remains the treatment of choice for osteoporosis and coronary heart disease prevention while SERMs offer an alternative to only a select group of women.
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