Raloxifene hcl Raloxifene HCL Raloxifene hydrochloride
Raloxifene (marketed as Evista by Eli Lilly and Company) is an oralselective 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.
In 2006, the National Cancer Institute announced that raloxifene was as effective as tamoxifen in reducing the incidence of breast cancer in postmenopausal women at increased risk. A major adverse effect of tamoxifen is uterine cancer; raloxifene caused fewer cases of uterine cancer. Tamoxifen increased the risk of cataracts, but raloxifene did not. Both groups had more blood clots in veins and the lungs, but that side effect was more common with tamoxifen than raloxifene.[2][3][4] On September 14, 2007, the U.S. Food and Drug Administration announced approval of raloxifene for reducing the risk of invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer.[5]
An editorial in Lancet Oncology criticized the way that information about the drug was released.[6]
Systematic (IUPAC) name | |
---|---|
[6-hydroxy-2-(4-hydroxyphenyl)- benzothiophen-3-yl]- [4-[2-(1-piperidyl)ethoxy]phenyl] -methanone | |
Clinical data | |
Trade names | Evista |
AHFS/Drugs.com | monograph |
MedlinePlus | a698007 |
Licence data | EMA:Link, US FDA:link |
Pregnancy cat. | X (AU) X (US) |
Legal status | Prescription only |
Routes | Oral |
Pharmacokinetic data | |
Bioavailability | 2% |
Protein binding | 95% |
Metabolism |
Gut glucuronidation[1] CYP system not involved |
Half-life | 27.7 hours |
Excretion | Fecal |
Identifiers | |
CAS number | 84449-90-1 |
ATC code | G03XC01 |
PubChem | CID 5035 |
IUPHAR ligand | 2820 |
DrugBank | DB00481 |
ChemSpider | 4859 |
UNII | YX9162EO3I |
ChEBI | CHEBI:8772 |
ChEMBL | CHEMBL81 |
Chemical data | |
Formula | C28H27NO4S |
Mol. mass | 473.584 g/mol |
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