SERMs mimic estrogen in some tissues and have anti-estrogen activity in
Raloxifene (Sedovesta) belongs to a class of drugs called selective
estrogen receptor modulators (SERMs).
Raloxifene hydrochloride (HCl) has the empirical formula C28H27NO4S-HCl,
which corresponds to a molecular weight of 510.05 g/mol. Raloxifene HCl
is an off-white to pale-yellow solid that is very slightly soluble in
Mode of action:
SERMs work like estrogen in some tissues but as an anti-estrogen in
other tissues. The SERMs are developed to reap the benefits of estrogen
while avoiding the potential side effects of estrogen. Thus, raloxifene
can act like estrogen on bone, but as an anti-estrogen on the lining of
Raloxifene (Sedovesta) is as effective as tamoxifen in reducing the
incidence of breast cancer in certain high risk groups of females, which
blocks the stimulative effect of estrogen on breast tissue. Tamoxifen
has proven valuable in women who have had cancer in one breast in
preventing cancer in the second breast.
Raloxifene (Sedovesta) is the second SERM to be approved by the FDA.
Raloxifene has been approved for the prevention and treatment of
osteoporosis in postmenopausal women. In a three year study involving
some 600 postmenopausal women, raloxifene was found to increase bone
density and lower LDL cholesterol, while having no stimulative effect on
the uterine lining (which means that it is unlikely to cause uterine
Because of its anti-estrogen effects, the most common side effects with
raloxifene are hot flashes.
Conversely, because of its estrogenic effects, raloxifene increases the
risk of blood clots, including deep vein thrombosis (DVT) and pulmonary
embolism (blood clots in the lung). The greatest increase in risk occurs
during the first 4 months of use. Patients taking raloxifene should
avoid prolonged periods of immobility during travel, when blood clots
are more prone to occur. The risk of deep vein thrombosis with
raloxifene is probably comparable to that of estrogen, about 2 to 3
times higher than the usual low occurrence rate.
Raloxifene (Sedovesta) decreases the risk of spine fractures in
postmenopausal women with osteoporosis, but the benefit in decreasing
hip fracture risk is not yet known. (The only agents that are definitely
proven to decrease hip fracture risk are bisphosphonates.)
Raloxifene is indicated for the treatment and prevention of osteoporosis
in postmenopausal women.
For either osteoporosis treatment or prevention, supplemental
and/or vitamin D should be added to the diet if daily intake is
The selective estrogen-receptor modulator (SERM) Raloxifene (Sedovesta)
, reduces the risk of hormone-positive breast cancer and vertebral
fractures "without a shadow of a doubt," but its effects on
cardiovascular disease remain less certain, according to the results of
the Raloxifene (Sedovesta) for Use of the Heart (RUTH) study published
in the July 13, 2006 issue of the New England Journal of Medicine by Dr
Elizabeth Barrett-Connor (University of California, San Diego) and
In the trial, in women with coronary heart disease (CHD) or multiple
risk factors for CHD, Raloxifene (Sedovesta) had no significant effect
on the primary end point, coronary events, but it did significantly
increase the risk of venous thromboembolism (VTE). And although the drug
had no effect on stroke, there was a seemingly paradoxical significant
increase in death from stroke.