Raloxifene
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| Clinical data | |
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| Trade names | Evista |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a698007 |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | 2% |
| Protein binding | 95% |
| Metabolism |
Gut glucuronidation system not involved |
| Biological half-life | 27.7 hours |
| Excretion | Fecal |
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| PDB ligand | |
| ECHA InfoCard | 100.212.655 |
| Chemical and physical data | |
| Formula | C28H27NO4S |
| Molar mass | 473.584 g/mol |
| 3D model (Jmol) | |
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Raloxifene (marketed as Evista by Eli Lilly and Company) is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women and to reduce the risk of invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer.
Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women. It is also used for reduction of risk and treatment of invasive breast cancer, and it also reduces breast density. For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate.
Common adverse events considered to be drug-related were hot flashes and leg cramps.
Raloxifene may infrequently cause serious blood clots to form in the legs, lungs, or eyes. Other reactions experienced include leg swelling/pain, trouble breathing, chest pain, vision changes. Raloxifene is a teratogenic drug, i.e., can cause developmental abnormalities such as birth defects.
Black box warnings were added to the label of raloxifene in 2007 warning of increased risk of death due to stroke for postmenopausal women with documented coronary heart disease or at increased risk for major coronary events, as well as increased risks for deep vein thrombosis and pulmonary embolism.
A report in September 2009 from Health and Human Services' Agency for Healthcare Research and Quality suggests that tamoxifen and raloxifene, used to treat breast cancer, significantly reduce invasive breast cancer in midlife and older women, but also increase the risk of adverse side effects.
A recent human case report in July 2016 suggests that Raloxifene may in fact, at some point, also stimulate breast cancer growth leading to a reduction of advanced breast cancer disease upon the withdrawal of the drug.
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