Bazedoxifene

Bazedoxifene, used as bazedoxifene acetate, is a medication for bone problems and possibly (pending more study) for cancer.[1] It is a third-generation selective estrogen receptor modulator (SERM).[2] 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.[3]

Medical uses

Bazedoxifene is used in the prevention of postmenopausal osteoporosis.[4]

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.[4]

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.[4]

Available forms

Bazedoxifene is marketed both alone and in combination with conjugated estrogens.[5]

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.[6]

History

Approval

The drug was approved in the European Union by the European Medicines Agency on April 27, 2009.[7]

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.[5]

See also

References

  1. DUAVEE® (conjugated estrogens/bazedoxifene) tablets for oral use U.S. Food and Drug Administration, October 2013^
  2. Update on bazedoxifene: a novel selective estrogen receptor modulator Clinical Interventions in Aging, 2007^
  3. Osteoporosis drug stops growth of breast cancer cells, even in resistant tumors Duke University Medical Center, June 15, 2013^
  4. Bazedoxifene: the evolving role of third-generation selective estrogen-receptor modulators in the management of postmenopausal osteoporosis Therapeutic Advances in Musculoskeletal Disease, February 2012^
  5. Bazedoxifene drugs.com^
  6. Heterocyclic Scaffolds II:: Reactions and Applications of Indoles Springer Science & Business Media, 9 October 2010^
  7. EPARs for authorised medicinal products for human use - Conbriza European Medicines Agency, 26 May 2009, retrieved 2009-07-08^