The therapeutic role of fulvestrant in the management of patients with hormone receptor-positive breast cancer

Breast. 2014 Jun;23(3):201-8. doi: 10.1016/j.breast.2014.01.016. Epub 2014 Mar 1.

Abstract

Although selective estrogen receptor modulators (SERMs), such as tamoxifen, or aromatase inhibitors (AIs), such as anastrozole, are the preferred endocrine treatment approach for most patients with hormone receptor-positive breast cancer, many patients progress despite this therapy or become resistant. Fulvestrant is a selective estrogen receptor down-regulator (SERD) that has demonstrated activity and efficacy in patients with hormone receptor-positive breast cancer previously untreated or treated with hormonal therapy. The efficacy of fulvestrant has been demonstrated in the neoadjuvant and metastatic settings, either alone or in combination with other therapies such as anastrozole or targeted drugs. Additionally, 500 mg of fulvestrant have been shown to be more effective than 250 mg, without significant differences in the toxicity profile. In this review, the unique mode of action of fulvestrant and the clinical data for different dosing regimens both alone or in combination with other drugs is critically assessed.

Keywords: Aromatase inhibitor; Endocrine treatment; Fulvestrant; Hormone receptor-positive breast cancer; Selective estrogen receptor down-regulators; Selective estrogen receptor modulators.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents, Hormonal / pharmacology
  • Antineoplastic Agents, Hormonal / therapeutic use
  • Antineoplastic Combined Chemotherapy Protocols
  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / metabolism
  • Dose-Response Relationship, Drug
  • Estradiol / analogs & derivatives*
  • Estradiol / pharmacology
  • Estradiol / therapeutic use
  • Estrogen Receptor Antagonists / pharmacology
  • Estrogen Receptor Antagonists / therapeutic use
  • Female
  • Fulvestrant
  • Humans
  • Outcome Assessment, Health Care
  • Receptors, Estrogen / metabolism*
  • Selective Estrogen Receptor Modulators / therapeutic use

Substances

  • Antineoplastic Agents, Hormonal
  • Estrogen Receptor Antagonists
  • Receptors, Estrogen
  • Selective Estrogen Receptor Modulators
  • Fulvestrant
  • Estradiol