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Raloxifene: a selective estrogen-receptor modulator for postmenopausal osteoporosis - a clinical update on efficacy
Chad L Deal1, Michael W Draper
1Center for Osteoporosis and Metabolic Bone Disease, Department of Rheumatic and Immunology Diseases/A50, The Cleveland Clinic Foundation, Cleveland, OH 44195, USA. dealc@ccf.org.
Abstract:
Selective estrogen-receptor modulators are molecules with specific estrogen-receptor binding affinity. Each selective estrogen-receptor modulator induces a unique conformation in the ligand-receptor complex, which leads to transcriptional activation and/or inhibition. Raloxifene 60 mg/day, a benzothiophene selective estrogen-receptor modulator, is approved for the prevention and treatment of postmenopausal osteoporosis. This article provides an update on new studies and further analyses of clinical trial data for raloxifene. The Multiple Outcomes of Raloxifene Evaluation (MORE) trial of women with osteoporosis has described the efficacy of raloxifene in decreasing vertebral fracture risk over 4 years. The Continuing Outcomes Relevant to Evista((R)) (CORE) trial, designed to assess the effects of raloxifene on breast cancer prevention, is a 4-year continuation of MORE. The skeletal and cardiovascular effects of raloxifene in the CORE study were similar to those observed in MORE. The relative risk of developing breast cancer was significantly decreased in women treated with raloxifene, compared with placebo, after 4 years in MORE and 8 years in the CORE trial. The incidence of uterine bleeding, endometrial hyperplasia and endometrial cancer was similar between raloxifene and placebo after 8 years of treatment. Raloxifene use is associated with a higher incidence of hot flashes and leg cramps, and an increased risk of venous thromboembolic events.
Insights
Selective estrogen-receptor modulators like raloxifene effectively prevent osteoporosis and reduce breast cancer risk. Long-term studies confirm raloxifene
Area of Science:
- Pharmacology
- Endocrinology
- Oncology
Background:
- Selective estrogen-receptor modulators (SERMs) exhibit unique estrogen receptor binding affinities, influencing gene transcription.
- Raloxifene, a SERM, is FDA-approved for preventing and treating postmenopausal osteoporosis.
Purpose of the Study:
- To provide an updated analysis of clinical trial data for raloxifene.
- To evaluate the long-term efficacy and safety of raloxifene in postmenopausal women.
Main Methods:
- Analysis of data from the Multiple Outcomes of Raloxifene Evaluation (MORE) trial and its continuation, the Continuing Outcomes Relevant to Evista (CORE) trial.
- Assessment of raloxifene's effects on skeletal health, cardiovascular events, and breast cancer incidence over 4 and 8 years.
Main Results:
- Raloxifene significantly decreased vertebral fracture risk in osteoporotic women.
- A significant reduction in breast cancer risk was observed in women treated with raloxifene compared to placebo.
- Raloxifene showed similar skeletal and cardiovascular effects to placebo, with no increased risk of uterine pathologies.
- Adverse events included increased hot flashes, leg cramps, and a higher risk of venous thromboembolic events.
Conclusions:
- Raloxifene is effective for osteoporosis prevention and treatment and reduces breast cancer risk in postmenopausal women.
- Long-term use of raloxifene demonstrates sustained efficacy with a manageable safety profile, though risks of VTE and vasomotor symptoms exist.
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