From the Guidelines
Raloxifene is a selective estrogen receptor modulator (SERM) medication primarily used to prevent and treat osteoporosis in postmenopausal women, and it is also used to reduce the risk of invasive breast cancer in postmenopausal women with osteoporosis or at increased risk of breast cancer. It is marketed under the brand name Evista and is typically prescribed as a 60 mg tablet taken once daily with or without food 1. Raloxifene works by selectively binding to estrogen receptors throughout the body, acting as an estrogen agonist in some tissues (like bone) while functioning as an antagonist in others (like breast tissue) 1. This selective action allows it to provide the beneficial effects of estrogen on bone density without stimulating breast or uterine tissue, thereby reducing the risk of breast cancer and not causing uterine growth.
Some key points to consider when prescribing raloxifene include:
- It is contraindicated in women with a history of venous thromboembolism, during pregnancy, or in premenopausal women 1.
- Common side effects include hot flashes, leg cramps, and an increased risk of blood clots, particularly deep vein thrombosis 1.
- Treatment duration is typically long-term, often continuing for several years to maintain its protective effects on bone health 1.
- Raloxifene may be used for longer than 5 years in women with osteoporosis in whom breast cancer risk reduction is an additional potential benefit 1.
- The risk/benefit ratio for raloxifene use in postmenopausal women at increased risk for breast cancer is influenced by age and comorbid conditions 1.
Overall, raloxifene is a valuable option for the prevention and treatment of osteoporosis and the reduction of breast cancer risk in postmenopausal women, but its use should be carefully considered on an individual basis, taking into account the potential benefits and risks 1.
From the FDA Drug Label
Raloxifene hydrochloride is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM) that belongs to the benzothiophene class of compounds. The biological actions of raloxifene are largely mediated through binding to estrogen receptors. Raloxifene appears to act as an estrogen agonist in bone. It decreases bone resorption and bone turnover, increases bone mineral density (BMD) and decreases fracture incidence Preclinical data demonstrate that raloxifene is an estrogen antagonist in uterine and breast tissues.
Raloxifene is a Selective Estrogen Receptor Modulator (SERM), which acts as an estrogen agonist in bone and an estrogen antagonist in uterine and breast tissues. It is used to prevent and treat osteoporosis in postmenopausal women by decreasing bone resorption and increasing bone mineral density. 2 2 2
From the Research
Definition and Mechanism of Raloxifene
- Raloxifene is a Selective Estrogen Receptor Modulator (SERM) that acts as an estrogen agonist in the skeleton and on lipid metabolism, and as an estrogen antagonist in breast and endometrial tissue 3, 4, 5.
- It is used for the prevention and treatment of osteoporosis in postmenopausal women, and has been shown to maintain bone mineral density (BMD) and prevent new vertebral fractures 3, 5.
- Raloxifene also has a beneficial effect on lipid metabolism, reducing total cholesterol and low-density lipoprotein (LDL) cholesterol levels 5.
Efficacy in Breast Cancer Prevention
- Raloxifene has been shown to reduce the risk of invasive breast cancer in postmenopausal women, particularly estrogen receptor-positive breast cancer 4, 6, 7.
- The Multiple Outcomes of Raloxifene Evaluation (MORE) study found that raloxifene reduced the risk of invasive breast cancer by 76% during 3 years of treatment 4.
- Raloxifene's mechanism of action in breast cancer prevention is thought to be related to its estrogen antagonist effects on breast tissue, as well as its ability to inhibit breast tissue proliferation through mechanisms independent of the estrogen receptor 6.
Safety and Adverse Events
- Raloxifene has been associated with an increased risk of venous thromboembolism, including deep vein thrombosis and pulmonary embolism 3, 4, 5.
- It has also been associated with an increased risk of hot flashes and leg cramps 5.
- However, raloxifene has not been shown to increase the risk of endometrial cancer or hyperplasia 4, 5.
Clinical Use and Recommendations
- Raloxifene is recommended for the prevention of vertebral fractures in women with osteopenia or osteoporosis who are not at high risk of non-vertebral fractures and who do not have a past history of venous thromboembolism 5.
- It may also be considered for the reduction of invasive breast cancer risk in postmenopausal women, particularly those with a high risk of breast cancer 7.