Second generation selective estrogen receptor modulator.
Agonizes estrogen receptors in liver and bone but not in breast and uterus.
Prevents and treats bone loss.
Decreases the risk of invasive breast cancer by 76%.
Does not treat symptoms of estrogen deficiency.
No stimulatory action on the endometrium.
Increases the frequency of pulmonary embolism and deep vein thrombosis by a factor of three.
It is associated with an increased risk of venous thromboembolism but less than that for tamoxifen.
In the Multiple Outcomes of Raloxifene Evaluation (MORE), trial to test the effect of these drugs on bone health showed in postmenopausal women to be associated with a 76% decrease in the risk of invasive breast cancer (Cummings SR et al).
In the NSABP Study of Tamoxifen and Raloxifene,21 postmenopausal women with a mean 5-year BCRAT risk of 4.03% were randomly assigned to either tamoxifen or raloxifene: There was no difference in risk reduction between the drugs in patients with invasive cancer, but there were fewer noninvasive cancers in the tamoxifen arm.
The raloxifene arm had fewer cases of uterine cancer and fewer thrombotic events.
Raloxifene has antiestrogen effects in the breasts and can be used only in postmenopausal women for breast cancer risk reduction.
Decreases total cholesterol by 6% and LDL by 12%.
Reduces the size of leiomyomas.
Decreases fibrinogen and homocysteine levels.
Treatment for a median of 5.6 years did not significantly alter risk of coronary events.
Treatment does not increase risk of coronary events among women with coronary heart disease or among women at high risk for such disease and it does not cause an early increase in the risk of coronary heart disease.
Not a first-line agent for osteoporosis.
Raloxifene can increase bone strength and is approved for the prevention and treatment of osteoporosis.
Reduces risk of vertebral fractures but not non-vertebral fractures.
The SERM raloxifene has been shown to increase BMD in both the spine and hip and to decrease vertebral fracture risk by up to 60%.
It has been shown to decrease non vertebral fractures.