From the Guidelines
Raloxifene should not be used as a first-line treatment for osteoporosis in postmenopausal women, due to its limited efficacy in reducing non-vertebral and hip fractures, and its associated risks of venous thromboembolism and fatal stroke, as noted in the RUTH trial 1. The American College of Physicians recommends against using raloxifene for the treatment of osteoporosis in women, citing moderate-quality evidence 1. Instead, bisphosphonates such as alendronate, risedronate, or zoledronic acid, or denosumab, are preferred for their proven efficacy in reducing the risk of hip and vertebral fractures in women with known osteoporosis. Some key points to consider when evaluating the use of raloxifene for osteoporosis include:
- Raloxifene's efficacy in reducing vertebral fracture risk, but not non-vertebral or hip fracture risk 1
- The increased risk of venous thromboembolism and fatal stroke associated with raloxifene use, particularly in women with a history of coronary artery disease or cardiovascular risk factors 1
- The potential for raloxifene to cause hot flashes, leg cramps, and other side effects, which may impact quality of life 1
- The availability of alternative treatments, such as bisphosphonates and denosumab, which have a more established efficacy and safety profile for osteoporosis treatment 1. Overall, while raloxifene may have some benefits for bone health, its limitations and risks make it a less desirable option for osteoporosis treatment, and it should be used with caution and only in specific clinical scenarios, if at all.
From the FDA Drug Label
- 1 Treatment and Prevention of Osteoporosis in Postmenopausal Women Raloxifene hydrochloride tablets are indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1,14.2)].
The role of Raloxifene (Evista) in the treatment of osteoporosis is for treatment and prevention of osteoporosis in postmenopausal women 2.
- Key benefits: Treatment and prevention of osteoporosis
- Target population: Postmenopausal women The recommended dosage is one 60 mg raloxifene hydrochloride tablet daily 2.
From the Research
Role of Raloxifene in Osteoporosis Treatment
- Raloxifene is a selective estrogen receptor modulator (SERM) approved for the treatment and prevention of osteoporosis in postmenopausal women in Europe and the US 3, 4, 5, 6, 7.
- It reduces the risk of invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer 3, 4, 5.
Mechanism of Action
- Raloxifene has estrogen agonistic effects on bone, reducing biochemical markers of bone turnover to premenopausal levels, increasing bone mineral density (BMD) at the lumbar spine, proximal femur, and total body, and reducing vertebral fracture risk in women with osteopenia or osteoporosis 3, 4, 5.
- It also has estrogen antagonistic effects on breast tissue, reducing the risk of invasive estrogen-receptor positive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer 3, 4, 5.
Clinical Applications
- Raloxifene can be recommended for the prevention of vertebral fractures in women with osteopenia/osteoporosis who are not at high risk of non-vertebral fractures and who do not have a past history of venous thromboembolism 5.
- Postmenopausal women between 50 and 70 years of age without climacteric symptoms with either osteopenia or osteoporosis should be evaluated with regard to their breast cancer risk and considered for treatment with raloxifene within the framework of its contraindications and precautions 3.
- Raloxifene is also approved for the treatment of osteoporosis, and has been shown to increase BMD and decrease fracture risk 6, 7.
Side Effects and Risks
- Raloxifene increases the incidence of hot flushes, the risk of venous thromboembolic events, and the risk of fatal stroke in postmenopausal women at increased risk for coronary heart disease 3, 5.
- Adverse events associated with raloxifene include an increase in the absolute risk of venous thromboembolism and an increase in the risk of hot flashes and leg cramps 5.