Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells

In Vivo. 2019 Sep-Oct;33(5):1439-1445. doi: 10.21873/invivo.11622.

Abstract

Background: Endocrine therapy is clinically administered in hormone-responsive breast cancer. Combinations of fluoropyrimidine S-1 and an aromatase inhibitor or anti-estrogen are considered beneficial in Japan. Herein we assessed new combinations of S-1 and fulvestrant.

Patients and methods: Cytotoxicity of fulvestrant and 5-fluorouracil (5-FU) was assessed in hormone-responsive (MCF-7) and non-responsive (MDA-MB-231) breast cancer cell cultures. Fulvestrant and S-1 were evaluated for antitumor activity in mice and their effects on estrogen receptor (ER)-α and progesterone receptor (PgR) levels in MCF-7 xenografts using immunohistochemical methods.

Results: Fulvestrant inhibited growth of MCF-7, but not of MDA-MB-231 xenografts. Combinations of 5-FU and fulvestrant were superior to monotherapy in vitro. In vivo antitumor activity of S-1/fulvestrant combination therapy was significantly (p<0.05) enhanced compared to that of both monotherapies. Fulvestrant partially down-regulated expression of ERα and PgR, but in combination with S-1, it almost completely blocked their expression.

Conclusion: Chemo-endocrine combination therapy using S-1 and fulvestrant is beneficial in estrogen-responsive breast cancer.

Keywords: Breast cancer; S-1; chemo-endocrine combination therapy; chemotherapy; endocrine therapy; estrogen receptor; fulvestrant; progesterone receptor.

MeSH terms

  • Animals
  • Antineoplastic Agents, Hormonal / pharmacology*
  • Breast Neoplasms / metabolism*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Resistance, Neoplasm / drug effects
  • Drug Synergism
  • Estrogen Receptor Antagonists / pharmacology*
  • Estrogens / metabolism*
  • Estrogens / pharmacology
  • Female
  • Fulvestrant / pharmacology*
  • Humans
  • Mice
  • Pyrimidines / pharmacology*

Substances

  • Antineoplastic Agents, Hormonal
  • Estrogen Receptor Antagonists
  • Estrogens
  • Pyrimidines
  • Fulvestrant
  • pyrimidine