Toremifene--a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy.

Abstract

Deregulation of the estrogen axis in humans prompts a series of tissue-specific events. In the breast and prostate, alterations in estrogen signalling lead to genotypic and phenotypic molecular alterations that result in dysplastic cellular appearance, deregulated cell growth and carcinoma. In bone, decreased estrogen leads to increased osteoclastogenesis and bone resorption, decreased bone mineral density and a significant fracture risk. Toremifene is a selective estrogen receptor modulator that exerts pharmacological activity in the breast, bone and prostate. An intense interest in developing this agent for prostate cancer chemoprevention is based on the reduction of premalignant and malignant prostate lesions in a transgenic model of prostate cancer. Biological and clinical activity was demonstrated in Phase II trials by the prevention of progression to prostate cancer in men with high-grade prostate intraepithelial neoplasia and through suppression of bone turnover biomarkers and increased bone mineral density in men on androgen deprivation therapy for prostate cancer.

• Authors: Samir S Taneja, Matthew R Smith, James T Dalton, Sharan Raghow, Gary Barnette, Mitchell Steiner, Karen A Veverka
• Journal: Expert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 15 Issue 3 Pg. 293-305 (Mar 2006) ISSN: 1744-7658 [Electronic] England
• PMID: 16503765 (Publication Type: Journal Article, Review)

Chemical References

• Androgen Antagonists
• Androgens
• Antineoplastic Agents, Hormonal
• Selective Estrogen Receptor Modulators
• Toremifene

Topics

• Androgen Antagonists (chemistry, therapeutic use)
• Androgens (deficiency)
• Antineoplastic Agents, Hormonal (chemistry, therapeutic use)
• Humans
• Male
• Prostatic Neoplasms (blood, prevention & control)
• Selective Estrogen Receptor Modulators (chemistry, therapeutic use)
• Toremifene (chemistry, therapeutic use)