Concept

Fosfestrol

Summary
Fosfestrol, sold under the brand name Honvan and also known as diethylstilbestrol diphosphate (DESDP), is an estrogen medication which is used in the treatment of prostate cancer in men. It is given by slow intravenous infusion once per day to once per week or by mouth once per day. Side effects of fosfestrol include nausea and vomiting, cardiovascular complications, blood clots, edema, and genital skin reactions, among others. Fosfestrol is an estrogen, and hence is an agonist of the estrogen receptor, the biological target of estrogens like estradiol. It acts as a prodrug of diethylstilbestrol. Fosfestrol was patented in 1941 and was introduced for medical use in 1955. It was previously marketed widely throughout the world, but now remains available in only a few countries. Fosfestrol is used as a form of high-dose estrogen therapy in the treatment of castration-resistant prostate cancer. It is added once progression of metastases has occurred following therapy with other interventions such orchiectomy, gonadotropin-releasing hormone modulators, and nonsteroidal antiandrogens. Fosfestrol has also been used to prevent the testosterone flare at the start of gonadotropin-releasing hormone agonist therapy in men with prostate cancer. Fosfestrol sodium is given at a dosage of 600 to 1200 mg/day by slow intravenous infusion over a period of 1 hour for a treatment duration of 5 to 10 days in men with prostate cancer. Following this, it is given at a dose of 300 mg/day for 10 to 20 days. Maintenance doses of fosfestrol sodium of 300 to 600 mg may be given four times per week. This may be gradually reduced to one 300 to 600-mg dose per week over a period of several months. Fosfestrol sodium is also used to a lesser extent by oral administration initially at a dosage of 360 to 480 mg three times per day in the treatment of prostate cancer. Maintenance doses of 120 to 240 mg three times per day may be used and can be gradually reduced to 240 mg/day. Fosfestrol is available in the form of solutions for intravenous administration and tablets for oral administration.
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