PMID: 2142231Jun 22, 1990Paper

Review of the pharmacological properties of toremifene

Journal of Steroid Biochemistry
L Kangas

Abstract

New compounds were synthesized with the aim to develop new anti-estrogenic antitumor drugs. The biological properties of the molecules were screened by (1) estrogen receptor (ER) binding, (2) effect on MCF-7 cells, (3) uterotrophic effect and inhibition of estradiol induced uterotropic effect and (4) antitumor effect in DMBA induced rat mammary cancer. One of the molecules, Fc-1157a = toremifene, exhibited the following characteristics: competitive inhibition of [3H]estradiol binding to ER (IC50 = 0.3 mumol/l), inhibition of MCF-7 cell growth in a concentration-dependent manner and cell-killing effect at higher than 3 mumol/l concentrations. Minimal estrogenic dose of toremifene on rat uterus weight was about 40 times higher than that of tamoxifen. Toremifene had statistically significant effect against DMBA-induced rat mammary cancer. Further screening consisted of antitumor, pharmacokinetic and safety studies. Toremifene inhibited the growth of ER-negative, glucocorticoid sensitive, mouse uterine sarcoma in a dose-dependent manner. Pharmacokinetics and metabolism of toremifene resembled closely those of tamoxifen, but since the chlorine atom of the toremifene molecule was not metabolically cleaved tamoxifen and toremifene did...Continue Reading

References

Jun 22, 1990·Journal of Steroid Biochemistry·H SipiläM Anttila
Jun 22, 1990·Journal of Steroid Biochemistry·M AnttilaJ Mäenpää
Jan 1, 1986·Cancer Chemotherapy and Pharmacology·S KallioR Toivola
May 1, 1970·The Journal of Clinical Endocrinology and Metabolism·S G Korenman, B A Dukes
Oct 4, 1974·Nature·J H ClarkJ N Anderson

Citations

Nov 1, 1995·Critical Reviews in Oncology/hematology·E Lønning, E A Lien
Jun 14, 2005·Molecular and Cellular Endocrinology·Sanjay KansraNira Ben-Jonathan
Jun 1, 1997·Molecular Aspects of Medicine·V C Jordan, W J Gradishar
Mar 2, 2011·Cancer Biotherapy & Radiopharmaceuticals·Ayfer Yurt KilcarCumhur Gunduz
Jan 10, 2014·Endocrine-related Cancer·Adam W NelsonJason S Carroll
Jul 9, 2004·Drug Metabolism Reviews·Sung Yeon KimShinya Shibutani
Jan 15, 2010·International Journal of Cancer. Journal International Du Cancer·Y R Santosh LaxmiShinya Shibutani
Sep 9, 2010·International Journal of Cancer. Journal International Du Cancer·Naomi SuzukiShinya Shibutani
Jan 25, 2005·The Journal of Steroid Biochemistry and Molecular Biology·Pirkko L Härkönen, Sari I Mäkelä
Oct 11, 2007·Differentiation; Research in Biological Diversity·William A RickeGerald R Cunha
Mar 25, 2006·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·Frank DombrowskiMatthias Evert
Nov 1, 1996·Drug and Chemical Toxicology·S KarlssonG M Williams
Feb 24, 2012·Expert Opinion on Drug Metabolism & Toxicology·Luigi GennariRanuccio Nuti
Jan 21, 2014·Clinical Breast Cancer·Charles L VogelDeborah Braccia
Apr 1, 1996·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·A HowellE Anderson
May 18, 2000·Cancer Treatment Reviews·E A Lien, P E Lønning
Jun 1, 1995·Clinical Pharmacology and Therapeutics·M AnttilaE A Sotaniemi
Jun 10, 2016·Molecular Diversity·M S R MurtyR S Prakasham

Related Concepts

Estrogen Antagonists
Zitazonium
Toremifene, (E)-Isomer