Drug Safety

, Volume 28, Issue 8, pp 721–730 | Cite as

Benefit-Risk Assessment of Raloxifene in Postmenopausal Osteoporosis

  • Ann Cranney
  • Jonathan D. Adachi
Review Article


Raloxifene, a nonsteroidal benzothiophene, is a second-generation selective estrogen receptor modulator (SERM) that is an antiresorptive agent. Raloxifene is a non-hormonal agent that binds to the estrogen receptor and results in estrogen agonist effects on bone and the cardiovascular system and estrogen antagonist effects on endometrial and breast tissue. Raloxifene has diverse pharmacodynamic properties due to its differential interactions with the estrogen receptor and tissue selectivity. Raloxifene was the first SERM to be approved for the prevention and treatment of postmenopausal osteoporosis. In this review, we conducted a systematic search of the literature for trials that evaluated the following outcomes: bone density, fractures, quality of life, cardiovascular outcomes, safety and adverse events. Raloxifene at the approved dosage of 60 mg/day increased lumbar spine bone density by 2.5% relative to control after 2 years of therapy. A large fracture prevention trial confirmed that treatment with raloxifene 60 mg/day for 3 years decreased the relative risk of incident vertebral fractures by 30–50% in women with prevalent fractures or osteoporosis. Extraskeletal effects of raloxifene include a reduction in total cholesterol and low density lipoprotein cholesterol levels. Assessment of the safety profile revealed that raloxifene was not associated with endometrial hyperplasia and that there was a 72% reduction in the incidence of invasive breast cancer in raloxifene-treated postmenopausal women with osteoporosis. Adverse events associated with raloxifene included an increase in the absolute risk of venous thromboembolism and an increase in the risk of hot flashes and leg cramps. In comparison to other osteoporosis therapies, raloxifene has a lesser impact on bone mineral density, a similar effect on the occurrence of vertebral fractures, but no effect on the frequency of non-vertebral fractures. 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.


Bone Mineral Density Vertebral Fracture Hormone Replacement Therapy Alendronate Raloxifene 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



Dr J.D. Adachi serves as a consultant for Eli Lilly, Aventis, Procter & Gamble, Novartis, Merck and Servier. Dr A. Cranney has served as a consultant/speaker for Merck and Aventis and as a consultant for Eli Lilly. No sources of funding were used to assist in the preparation of this review.


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Copyright information

© Adis Data Information BV 2005

Authors and Affiliations

  • Ann Cranney
    • 1
  • Jonathan D. Adachi
    • 2
  1. 1.Department of Medicine, C402, Clinical Epidemiology Program, Ottawa Hospital Civic CampusUniversity of OttawaOttawaCanada
  2. 2.Department of MedicineMcMaster UniversityHamiltonCanada

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