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Chemical compound From Wikipedia, the free encyclopedia
Bazedoxifene, used as bazedoxifene acetate, is a medication for bone problems and possibly (pending more study) for cancer.[2] It is a third-generation selective estrogen receptor modulator (SERM).[3] Since late 2013 it has had U.S. FDA approval for bazedoxifene as part of the combination drug Duavee in the prevention (not treatment) of postmenopausal osteoporosis. It is also being studied for possible treatment of breast cancer and pancreatic cancer.[4]
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Trade names | Conbriza, Duavee, Duavive, Viviant |
Other names | TSE-424; WAY-140424; WAY-TSE-424 |
AHFS/Drugs.com | International Drug Names |
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Routes of administration | By mouth |
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ECHA InfoCard | 100.232.728 |
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Formula | C30H34N2O3 |
Molar mass | 470.613 g·mol−1 |
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Bazedoxifene is used in the prevention of postmenopausal osteoporosis.
Bazedoxifene is marketed both alone and in combination with conjugated estrogens.[5]
Bazedoxifene is a selective estrogen receptor modulator (SERM), or a mixed agonist and antagonist of the estrogen receptor (ER) in different tissues.
Medication | Breast | Bone | Liver | Uterus | Vagina | Brain | ||||||||
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Lipids | Coagulation | SHBG | IGF-1 | Hot flashes | Gonadotropins | |||||||||
Estradiol | + | + | + | + | + | + | + | + | + | + | ||||
"Ideal SERM" | – | + | + | ± | ± | ± | – | + | + | ± | ||||
Bazedoxifene | – | + | + | + | + | ? | – | ± | – | ? | ||||
Clomifene | – | + | + | ? | + | + | – | ? | – | ± | ||||
Lasofoxifene | – | + | + | + | ? | ? | ± | ± | – | ? | ||||
Ospemifene | – | + | + | + | + | + | ± | ± | – | ± | ||||
Raloxifene | – | + | + | + | + | + | ± | – | – | ± | ||||
Tamoxifen | – | + | + | + | + | + | + | – | – | ± | ||||
Toremifene | – | + | + | + | + | + | + | – | – | ± | ||||
Effect: + = Estrogenic / agonistic. ± = Mixed or neutral. – = Antiestrogenic / antagonistic. Note: SERMs generally increase gonadotropin levels in hypogonadal and eugonadal men as well as premenopausal women (antiestrogenic) but decrease gonadotropin levels in postmenopausal women (estrogenic). Sources: See template. |
The drug is a member of the 2-phenylindole group of SERMs, along with zindoxifene and pipendoxifene.[6]
The drug was approved in the European Union by the European Medicines Agency on April 27, 2009.[7]
Bazedoxifene is marketed alone under the brand names Conbriza and Viviant and in combination with conjugated estrogens under the brand names Duavee and Duavive.[5]