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Fulvestrant, a selective estrogen receptor down-regulator, sensitizes estrogen receptor negative breast tumors to chemotherapy.

Abstract
Drug resistance frequently results in poor prognosis and high 5-year recurrence rate in estrogen receptor-negative (ER-) breast cancer patients. Herein, we examined the reversal effects of fulvestrant on multidrug resistance (MDR) in ER- breast cancer cells. Co-administration of fulvestrant significantly sensitized ER- MDR tumors to paclitaxel both in vitro and in vivo. Further analyses indicated that fulvestrant did not affect P-gp expression, but could inhibit P-gp function and subsequently reverse P-gp mediated drug resistance in ER- breast cancer cells. These results showed that combination of fulvestrant and chemotherapeutic agents might provide an effective treatment for ER- MDR breast cancers.
AuthorsDonghai Jiang, Yuan Huang, Ning Han, Mingjie Xu, Liang Xu, Lin Zhou, Shu Wang, Weimin Fan
JournalCancer letters (Cancer Lett) Vol. 346 Issue 2 Pg. 292-9 (May 01 2014) ISSN: 1872-7980 [Electronic] Ireland
PMID24462822 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2014 Elsevier Ireland Ltd. All rights reserved.
Chemical References
  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Antineoplastic Agents, Hormonal
  • Estrogen Receptor Modulators
  • Receptors, Estrogen
  • Fulvestrant
  • Estradiol
  • Paclitaxel
Topics
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 (antagonists & inhibitors, metabolism)
  • Animals
  • Antineoplastic Agents, Hormonal (pharmacology)
  • Antineoplastic Combined Chemotherapy Protocols (pharmacology)
  • Apoptosis (drug effects)
  • Breast Neoplasms (drug therapy, metabolism, pathology)
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm
  • Drug Synergism
  • Estradiol (administration & dosage, analogs & derivatives, pharmacology)
  • Estrogen Receptor Modulators (pharmacology)
  • Female
  • Fulvestrant
  • Humans
  • Mice
  • Mice, Nude
  • Mitosis (drug effects)
  • Paclitaxel (administration & dosage, pharmacology)
  • Random Allocation
  • Receptors, Estrogen (deficiency, metabolism)
  • Xenograft Model Antitumor Assays

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