raloxifene

Last reviewed 05/2023

Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women.

• first selective oestrogen receptor modulator to be launched for the prevention of vertebral fractures in postmenopausal women
• short term studies suggest a beneficial effect with treatment on the surrogate endpoints for bone and cardiovascular disease
• raloxifene is an additional therapeutic option for postmenopausal women at risk of osteoporosis but not wanting to have a restoration of monthly cyclical bleeding
• raloxifene will not alter the symptoms of the menopause and should not be given to women before the menopause
• raloxifene may be more acceptable than HRT if breast tenderness or pain is a problem (1)
• raloxifene reduces the risk of oestrogen receptor positive breast tumours
  • the MORE trial showed a reduction in vertebral fracture risk and breast cancer risk in women treated with raloxifene
  • a more recent study has provided evidence that, whatever the prior self-reported HRT of the women involved, raloxifene reduced vertebral fractures and breast cancer in postmenopausal women with osteoporosis (2)
  • in comparison to tamoxifen (3)
    • raloxifene is as effective as tamoxifen in reducing the risk of invasive breast cancer and has a lower risk of thromboembolic events and cataracts but a nonstatistically significant higher risk of noninvasive breast cancer
    • risk of other cancers, fractures, ischemic heart disease, and stroke is similar for both drugs
• there is no data currently available on the long term efficacy and safety of raloxifene
• raloxifene in osteoporosis
  • raloxifene inhibits bone resorption
    • it is approved for the treatment and prevention of osteoporosis in postmenopausal women, at a dose of 60 mg daily
    • has been shown to reduce vertebral fracture risk but reduction in non-vertebral and hip fractures has not been demonstrated
    • raloxifene is taken as a single daily dose (60 mg) and may be taken at any time without regard to meals
  • NICE state that (5)
    • raloxifene (along with strontium ranelate) is recommended as alternative treatment options for the secondary prevention of osteoporotic fragility fractures in postmenopausal women:
    • recommended as an alternative treatment option for the secondary prevention of osteoporotic fragility fractures in postmenopausal women:
      • who are unable to comply with the special instructions for the administration of alendronate and either risedronate or etidronate, or have a contraindication to or are intolerant of alendronate and either risedronate or etidronate and
      • who also have a combination of T-score, age and number of independent clinical risk factors for fracture
        
        
        • T-scores (SD) at (or below) which strontium ranelate and raloxifene is recommended when alendronate and either risedronate or etidronate cannot be taken

          • Age (years)	0 independent clinical risk factors for fracture	1 independent clinical risk factors for fracture	2 independent clinical risk factors for fracture
            50-54	Treatment strontium ranelate or raloxifene is not recommended	-3.5	-3.5
            55-59	-4.0	-3.5	-3.5
            60-64	-4.0	-3.5	-3.5
            65-69	-4.0	-3.5	-3.0
            70-74	-3.0	-3.0	-2.5
            75 or older	-3.0	-2.5	-2.5

• with respect to use of raloxifene in patients at increased cardiovascular disease risk (6):
  • raloxifene did not significantly affect the risk of coronary heart disease. There was an increased risk of venous thromboembolism and fatal stroke associated with use of raloxifene

Reference:

• 1. Drug and Therapeutics Bulletin 1999; 37 (5): 33-6.
• 2. Johnell O et al. Raloxifene reduces risk of vertebral fractures and breast cancer in postmenopausal women regardless of prior hormone therapy. J Fam Pract 2004;53:789-96
• 3. Vogel VG et al. Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial. JAMA. 2006 Jun 21;295(23):2727-41
• 4. National Osteoporosis Society (2008). Guideline for the diagnosis and management of osteoporosis in postmenopausal women and men from the age of 50 years in the UK
• 5. NICE (January 2011). Alendronate, etidronate, risedronate, raloxifene, strontium ranelate and teriparatide for the secondary prevention of osteoporotic fragility fractures in postmenopausal women
• 6. Barrett-Connor E et al. Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women. N Engl J Med. 2006 Jul 13;355(2):125-37.