In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer

T. L. Taras, G. T. Wurz, M. W. DeGregorio

Research output: Contribution to journalArticle

67 Citations (Scopus)

Abstract

Ospemifene (FC-1271a) is a novel selective estrogen receptor modulator under development for osteoporosis prevention. In the present paper, we examine both the in vitro and in vivo effects of FC-1271a in breast cancer models. In vitro, the growth inhibitory effects of FC-1271a and its main metabolite are investigated in MCF-7 and MDA-MB-231 human breast cancer cells at doses ranging from 0.1 to 10 μM. Modulation of pS2 expression, an indicator of estrogen activity, was also examined in all experiments using reverse transcription-polymerase chain reaction. In vivo, the effects of treatment with 10, 25, 50, or 100 mg/kg FC-1271a on MCF-7 and MDA-MB-231 human tumor xenografts in athymic, ovariectomized mice were determined. For MCF-7 cells, FC-1271a and its main metabolite, toremifene VI (TOR VI) displayed anti-estrogenic effects in vitro as shown through growth inhibition and decreased expression of pS2. Treatment with FC-1271a in vivo inhibited MCF-7 tumor growth, compared with control (P ≤ 0.05). FC-1271a and TOR VI did not inhibit the growth of MDA-MB-231 cells in vitro, and no clear effects of FC-1271a treatment were seen on MDA-MB-231 tumor growth in vivo. In conclusion, FC-1271a appears to exert anti-estrogenic effects dependent on estrogen receptor positivity in vitro and in vivo on the growth of MCF-7 cells.

Original languageEnglish (US)
Pages (from-to)271-279
Number of pages9
JournalJournal of Steroid Biochemistry and Molecular Biology
Volume77
Issue number4-5
DOIs
StatePublished - 2001

Fingerprint

Breast Neoplasms
Growth
Toremifene
Tumors
Estrogens
MCF-7 Cells
Metabolites
Ospemifene
In Vitro Techniques
Selective Estrogen Receptor Modulators
Neoplasms
Polymerase chain reaction
Transcription
Heterografts
Nude Mice
Estrogen Receptors
Osteoporosis
Reverse Transcription
Cells
Modulation

Keywords

  • FC-1271a
  • MCF-7
  • MDA-MB-231
  • Metabolites
  • Ospemifene
  • pS2
  • SERMs

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology

Cite this

In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer. / Taras, T. L.; Wurz, G. T.; DeGregorio, M. W.

In: Journal of Steroid Biochemistry and Molecular Biology, Vol. 77, No. 4-5, 2001, p. 271-279.

Research output: Contribution to journalArticle

Taras, T. L. ; Wurz, G. T. ; DeGregorio, M. W. / In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer. In: Journal of Steroid Biochemistry and Molecular Biology. 2001 ; Vol. 77, No. 4-5. pp. 271-279.
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