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

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Taneja SS, Smith MR, Dalton JT, Raghow S, Barnette G, Steiner M, Veverka KA

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

Expert Opin Investig Drugs. 2006 Mar;15(3):293-305.

PubMed ID

16503765 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Drugs

Toremifene

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Toremifene	Estrogen receptor alpha	Protein	Humans	Yes	Modulator	Details

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Toremifene	Cytochrome P450 3A4	Protein	Humans	Unknown	Substrate Inhibitor	Details