bazedoxifene (Duavee) Report issue

Small molecule Approved FDA
AACT ChEMBL DrugBank Drug Central KEGG MeSH PubChem repoDB

Active Ingredient History

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Bazedoxifene acetate (WAY-140424; TSE-424) is an oral, nonsteroidal, indole-based selective estrogen-receptor modulator developed by Ligand Pharmaceuticals in collaboration with Wyeth Pharmaceuticals (NJ, USA) (now Pfizer) . It was developed using raloxifene as a template with the benzothiophene core substituted by an indole ring in order to obtain favorable effects on the skeleton and lipid metabolism with the additional improvement of a neutral effect on hot flushes and without stimulating the uterus or the breast. The drug is approved as a monotherapy for the prevention and treatment of osteoporosis and in combination with conjugated estrogens for the treatment of menopausal symptoms and prevention of osteoporosis. Bazedoxifene binds to both ERalpha and ERbeta with high affinity. Bazedoxifene acts as both a receptor agonist and/or antagonist, depending upon the cell and tissue type and target genes. Bazedoxifene decreases bone resorption and reduces biochemical markers of bone turnover to the premenopausal range. These effects on bone remodeling lead to an increase in bone mineral density (BMD), which in turn contributes to a reduction in the risk of fractures. Bazedoxifene functions primarily as an estrogen-receptor antagonist in uterine and breast tissues.   NCATS

Chemistry

  • SMILES: Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12
  • InChIKey: UCJGJABZCDBEDK-UHFFFAOYSA-N
  • Mol. Mass: 470.61
  • ALogP: 6.33
  • ChEMBL Molecules:
    bazedoxifene  
    bazedoxifene acetate  
More Chemistry

Pharmacology

Alternative names

baxedoxifene | bazedoxifene | bazedoxifene acetate | bazedoxifene/conjugated estrogens | conbriza | duavee | oestrogens conjugated / bazedoxifene | tse424 | tse 424 | tse-424 | way-140424

Organizations (33)

Research & Development (33)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (2)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (25)

Approved Indications (2)


 

Hot Flashes (approved 2013)

Osteoporosis, Postmenopausal

Experimental Indications - Clinical Trial Phases 1-4 (24)


 

Arthritis, Rheumatoid (Phase 4)

Atherosclerosis (Phase 2)

Blood Glucose (Phase 4)

Breast Neoplasms (Phase 2)

Cognitive Dysfunction (Phase 2)

Depression (Phase 4)

Endometrial Hyperplasia (Phase 3)

Endometriosis (Phase 4)

Healthy Volunteers (Phase 1)

Menopause (Phase 4)

Multiple Sclerosis (Phase 2)

Multiple Sclerosis, Relapsing-Remitting (Phase 2)

Obesity (Phase 4)

Osteoporosis (Phase 3)

Osteoporosis, Postmenopausal (Phase 4)

Oxidative Stress (Phase 3)

Postmenopause (Phase 4)

Prediabetic State (Phase 2)

Psychotic Disorders (Phase 4)

Risk Reduction Behavior (Phase 2)

Schizophrenia (Phase 4)

Sleep (Phase 1)

Sleep Apnea Syndromes (Phase 3)

Vaginal Diseases (Phase 3)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 45
  • # of Trial Organizations: 33

Trials by Phase

Trial Phase Start Date Organizations Indications

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