Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer.

Journal Article (Journal Article)

Drugs that inhibit estrogen receptor alpha (ERα) or that block the production of estrogens remain frontline interventions in the treatment and management of breast cancer at all stages. However, resistance to endocrine therapies, especially in the setting of advanced disease, remains an impediment to durable clinical responses. Although the mechanisms underlying resistance to existing agents are complex, preclinical studies suggest that selective estrogen receptor downregulators (SERDs), molecules which eliminate ERα expression, may have particular utility in the treatment of breast cancers that have progressed on tamoxifen and/or aromatase inhibitors. The discovery and development of orally bioavailable SERDs provide the opportunity to evaluate the utility of eliminating ERα expression in advanced metastatic breast cancers.

Full Text

Duke Authors

Cited Authors

  • McDonnell, DP; Wardell, SE; Norris, JD

Published Date

  • June 25, 2015

Published In

Volume / Issue

  • 58 / 12

Start / End Page

  • 4883 - 4887

PubMed ID

  • 26039356

Pubmed Central ID

  • PMC4708081

Electronic International Standard Serial Number (EISSN)

  • 1520-4804

Digital Object Identifier (DOI)

  • 10.1021/acs.jmedchem.5b00760


  • eng

Conference Location

  • United States