Bazedoxifene

Bazedoxifene

ファイル:Bazedoxifene.svg
ファイル:Bazedoxifene-3D-balls.png
Systematic (IUPAC) name
1-[4-[2-(azepan-1-yl)ethoxy]benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol
Clinical data
Trade names	Conbriza, Duavee, Duavive, Viviant
AHFS/Drugs.com	International Drug Names
Licence data	EMA:[[[:テンプレート:EMA-EPAR]] Link]
Pregnancy cat.	?
Legal status	℞ Prescription only
Routes	By mouth
Identifiers
CAS number	198481-32-2 Y
ATC code	G03XC02
PubChem	CID 154257
IUPHAR ligand	7355
DrugBank	DB06401
ChemSpider	135921 Y
UNII	Q16TT9C5BK Y
ChEMBL	CHEMBL46740 Y
Synonyms	TSE-424; WAY-140424; WAY-TSE-424
Chemical data
Formula	C30H34N2O3
InChI 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 Y Key:UCJGJABZCDBEDK-UHFFFAOYSA-N Y
N (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 prevention of postmenopausal osteoporosis.

Osteoporosis represents a major public health concern, especially as the number of postmenopausal women continues to rise. As a result, the need for innovative treatments has become increasingly important. Bazedoxifene (BZA) has emerged as a promising option for postmenopausal osteoporosis due to its demonstrated effectiveness in reducing bone loss and fractures, as well as its strong safety and tolerability profile. For women who cannot or prefer not to use bisphosphonates, owing to gastrointestinal side effects, safety risks, or contraindications, selective estrogen receptor modulators (SERMs) like BZA may serve as a suitable alternative. SERMs may also benefit younger women who are at higher risk of fractures and require long-term treatment.

Furthermore, BZA has been paired with conjugated estrogens (TSEC) for both osteoporosis prevention and the management of menopausal symptoms. Given its positive safety record and efficacy in preventing fractures, BZA is becoming an increasingly important option within the current landscape of osteoporosis therapies.

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.

Chemistry

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

History

Approval

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

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

• Bazedoxifene/conjugated estrogens