SERMs in Clinical Practice : New Options for the Management of Postmenopausal Health Risks
Daniel Thiebaud *
Affiliation : * Department of Internal Medicine, University Hospital, Lausanne, CH-1011, Switzerland
Following menopause, women face the difficult decision of whether to take long-term
hormone replacement therapy to attain clear health benefits such as preventing heart disease and
osteoporosis, but with potential added risks for uterine and breast cancer. Raloxifene, a selective
estrogen receptor modulator (SERM) molecule designed to provide a new choice for women
to maintain good health throughout their postmenopausal life.
In phase III clinical trials, raloxifene prevented bone loss and significantly increased
bone mineral density in postmenopausal women 2 to 3 per cent more than calcium-supplemented
placebo at all skeletal sites (hip, spine and total body) after two years of treatment. Raloxifene
also significantly lowered total cholesterol (6 to 7o/c ), LDL-cholesterol (II to 12o/r), Lp (a)
( 49c ), and fibrinogen ( 12 to 139c ), and raised HDL-2 cholesterol (15 to 169() without raising
triglycerides or total HDL cholesterol after six months of treatment.
In the uterus, raloxifene
did not induce bleeding or spotting, nor increase endometrial proliferation (assessed by both
transvaginal ultrasonography and conventional biopsy) and was indistinguishable from placebo
in all trials.
Unlike estrogen. raloxifene did not stimulate breast tissue in postmenopausal
women.
Raloxifene was similar to placebo with regard to breast swelling, tenderness, and
pain, and did not increase the risk for breast cancer.
Raloxifene is similar to estrogen
regarding an increased risk for thromboembolic events, especially in patients with well-
established risk factors for this low-frequency disease.
The most commonly observed side
eff~ct of raloxifene was hot flashes, occurring in 24% of raloxifene patients Versus 18% of
placebo patients.
However, the onset, severity, duration, and drop-out rate for this mild side
effect were identical for both placebo and raloxifene.
In conclusion, raloxifene prevents
bone loss, lowers cholesterol, and is safe in the uterus and breast, thus providing a single solu-
tion for the multiple long-term health concerns of millions of postmenopausal women world-
wide.
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