Estrone sulfamate

Estrone sulfamate

Estrone sulfamate (also known as EMATE) is a steroidal estrogen and a sulfamate ester. It is an estrogen sulfotransferase inhibitor and is used in hormone replacement therapy for menopausal symptoms. It is also used in the treatment of breast cancer and prostate cancer.

Chemistry

Estrone sulfamate is a synthetic, steroidal estrogen that is a sulfamate ester of estrone. It is a white, crystalline powder that is soluble in water and alcohol. The chemical formula of estrone sulfamate is C18H22O8S.

Pharmacology

Estrone sulfamate acts as an estrogen sulfotransferase inhibitor. This enzyme is responsible for the sulfation of estrogens, which is a major pathway for the inactivation of these hormones. By inhibiting this enzyme, estrone sulfamate increases the levels of active estrogens in the body.

Clinical use

Estrone sulfamate is used in hormone replacement therapy to treat symptoms of menopause such as hot flashes and vaginal dryness. It is also used in the treatment of breast cancer and prostate cancer. In breast cancer, it is used as a second-line treatment in postmenopausal women with estrogen receptor-positive tumors. In prostate cancer, it is used in combination with other drugs to suppress testosterone levels.

Side effects

The most common side effects of estrone sulfamate include nausea, vomiting, breast tenderness, and menstrual irregularities. Less common side effects include blood clots, stroke, and endometrial cancer.

See also

• Estrone
• Estrogen sulfotransferase
• Hormone replacement therapy
• Breast cancer
• Prostate cancer