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Pfizer brands
Bazedoxifene
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Bazedoxifene

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Bazedoxifene
Bazedoxifene.svg
Bazedoxifene-3D-balls.png
Clinical data
Trade names Conbriza, Duavee, Duavive, Viviant
Other names TSE-424; WAY-140424; WAY-TSE-424
AHFS/Drugs.com International Drug Names
License data
Routes of
administration		 By mouth
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • 1-[4-[2-(azepan-1-yl)ethoxy]benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard 100.232.728
Chemical and physical data
Formula C30H34N2O3
Molar mass 470.613 g·mol−1
3D model (JSmol)
  • Oc1ccc(cc1)c3c(c2cc(O)ccc2n3Cc5ccc(OCCN4CCCCCC4)cc5)C
  • InChI=1S/C30H34N2O3/c1-22-28-20-26(34)12-15-29(28)32(30(22)24-8-10-25(33)11-9-24)21-23-6-13-27(14-7-23)35-19-18-31-16-4-2-3-5-17-31/h6-15,20,33-34H,2-5,16-19,21H2,1H3 checkY
  • Key:UCJGJABZCDBEDK-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Bazedoxifene, used as bazedoxifene acetate, is a medication for bone problems and possibly (pending more study) for cancer. It is a third-generation selective estrogen receptor modulator (SERM). 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.

Medical uses

Bazedoxifene is used in the treatment of postmenopausal osteoporosis.

Available forms

Bazedoxifene is marketed both alone and in combination with conjugated estrogens.

Pharmacology

Pharmacodynamics

Bazedoxifene is a selective estrogen receptor modulator (SERM), or a mixed agonist and antagonist of the estrogen receptor (ER) in different tissues.

Tissue-specific estrogenic and antiestrogenic activity of SERMs
Medication Breast Bone Liver Uterus Vagina Brain
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.

Chemistry

The drug is a member of the 2-phenylindole group of SERMs, along with zindoxifene and pipendoxifene.

History

Development

Bazedoxifene was developed by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. It is the result of an exclusive research collaboration between Wyeth Pharmaceuticals and Ligand Pharmaceuticals.

Approval

The drug was approved in the European Union by the European Medicines Agency on April 27, 2009.

On October 3, 2013, the FDA approved the combination product of bazedoxifene 20 mg with 0.45 mg Premarin (conjugated estrogens) for the treatment of menopausal osteoporosis and the treatment of moderate to severe hot flushes. This is the first approved menopausal hormone therapy product that contains a SERM (bazedoxifene) and an estrogen.

Society and culture

Brand names

Bazedoxifene is marketed alone under the brand names Conbriza and Viviant and in combination with conjugated estrogens under the brand names Duavee and Duavive.

See also


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