Toremifene belongs to a family of compounds called antiestrogens . Antiestrogens are used in cancer therapy by inhibiting the effects of estrogen on target tissues.

Estrogen is a steroid hormone secreted by granulosa cells of a maturing follicle within the female ovary. Depending on the target tissue, estrogen can stimulate the growth of female reproductive organs and breast tissue, play a role in the female menstrual cycle, and protect against bone loss by binding to estrogen receptors on the outside of cells within the target tissue. Antiestrogens act selectively against the effects of estrogen on target cells in a variety of ways, thus they are called selective estrogen receptor modulators (SERMs).

Toremifene selectively inhibits the effects of estrogen on breast tissue, while mimicking the effects of estrogen on bone (by increasing bone mineral density) and uterine tissues. The former makes toremifene an excellent therapeutic agent against breast cancer. Although researchers are unclear of the precise mechanism by which toremifene kills breast cancer cells, it is known to compete with estrogen by binding to estrogen receptors, therefore limiting the effects of estrogen on breast tissue. Toremifene may also be involved in other anti-tumor activities affecting oncogene expression, promotion of apoptosis and growth factor secretion.

Recommended dosage

Toremifene is taken orally, and the recommended dose is usually 40 to 60 milligrams once a day, although larger doses are sometimes prescribed. If a dose is missed, patients should not double the next dosage. Instead, they should return to their regular schedule and contact their doctor. Toremifene can interfere with the anticoagulant drug warfarin, resulting in severe consequences and death. If these two drugs are used together, patients will be monitored closely. Oral contraceptives and estrogen supplements can also interfere with the action of toremifene.

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