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 Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonist/antagonists (ERAAs), are a class of drugs that act on the estrogen receptor (ER). A characteristic that distinguishes these substances from pure ER agonists a ...

(SERM). Since late 2013 it has had U.S.

FDA The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food s ...

approval for bazedoxifene as part of the combination drug

Duavee Bazedoxifene/conjugated estrogens, sold under the brand name Duavee in the US and Duavive in the EU, is a fixed-dose combination medication for the treatment of menopause symptoms and postmenopausal osteoporosis. It contains the selective estro ...

in the prevention (not treatment) of postmenopausal

osteoporosis Osteoporosis is a systemic skeletal disorder characterized by low bone mass, micro-architectural deterioration of bone tissue leading to bone fragility, and consequent increase in fracture risk. It is the most common reason for a broken bone ...

. It is also being studied for possible treatment of breast cancer and

pancreatic cancer Pancreatic cancer arises when cell (biology), cells in the pancreas, a glandular organ behind the stomach, begin to multiply out of control and form a Neoplasm, mass. These cancerous cells have the malignant, ability to invade other parts of t ...

Medical uses

Bazedoxifene is used in the treatment of postmenopausal

Available forms

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

Pharmacology

Pharmacodynamics

Bazedoxifene is a

(SERM), or a mixed

agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...

and

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

of the estrogen receptor (ER) in different tissues.

Chemistry

The drug is a member of the 2-phenylindole group of SERMs, along with

zindoxifene Zindoxifene (INN; former developmental code names D-16726, NSC-341952) is a nonsteroidal selective estrogen receptor modulator (SERM) that was under development in the 1980s and early 1990s for the treatment of breast cancer but was not marketed ...

and

pipendoxifene Pipendoxifene (INN) (developmental code name ERA-923) is a nonsteroidal selective estrogen receptor modulator (SERM) that was under development by Ligand Pharmaceuticals and Wyeth-Ayerst Laboratories (now Wyeth) for the treatment of breast cancer ...

History

Development

Bazedoxifene was developed by Pfizer following the completion of their takeover of

Wyeth Pharmaceuticals Wyeth, LLC was an American pharmaceutical company. The company was founded in Philadelphia, Pennsylvania, in 1860 as ''John Wyeth and Brother''. It was later known, in the early 1930s, as American Home Products, before being renamed to Wyeth in ...

. It is the result of an exclusive research collaboration between

and Ligand Pharmaceuticals.

Approval

The drug was approved in the European Union by the

European Medicines Agency The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of medicinal products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products or Euro ...

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.

References

{{Other sex hormones and modulators of the genital system Azepanes Indoles Phenol ethers Phenols Selective estrogen receptor degraders Selective estrogen receptor modulators