Fulvestrant was developed by AstraZeneca. It was approved as a prescription drug in the U.S. in 2002, and is sold under the Faslodex brand name. The drug is indicated for the treatment of estrogen receptor positive breast cancer with disease progression following traditional anti-estrogen therapy (such as tamoxifen). AstraZeneca has since expanded the market for Faslodex to include over one dozen countries, including Argentina, Belgium, Brazil, Denmark, Finland, France, Germany, Greece, Ireland, Israel, Italy, Netherlands, Norway, Poland, Portugal, Spain, Sweden, Switzerland, United Kingdom, and Venezuela.
How is Fulvestrant supplied
Faslodex (fulvestrant) is supplied in pre-filled syringes containing 50-mg/mL fulvestrant, either as a single 5 mL or two 2.5 mL injections. The product must be refrigerated for storage.
Structural Characteristics of Fulvestrant
Fulvestrant is an estrogen receptor antagonist. It has the chemical designation 7-alpha-[9- (4,4,5,5,5-penta fluoropentylsulphinyl)nonyl]estra-1,3,5-(10)- triene-3,17- beta-diol.
Fulvestrant Side Effects
The most common side effects associated with fulvestrant include gastrointestinal disturbances such as nausea, vomiting, constipation, abdominal pain, and diarrhea. Other common adverse effects include headache, back pain, hot flashes, and sore throat. Less common side effects include rash, loss of strength, urinary-tract infections, venous thromboembolism, liver enzyme elevations, vaginal bleeding, muscle pain, and low white blood cell count. Injection side reactions may also occur. Anti-estrogens can harm the development of an unborn fetus, and should never be taken during pregnancy. When taken by men (as an off-label use) to reduce estrogenicity during prolonged periods of steroid treatment, a pure estrogen antagonist may increase cardiovascular disease (CVD) risk by retarding some beneficial properties of estrogen on cholesterol values. This may include a suppression of HDL (good) cholesterol values greater than that induced by steroid therapy alone.
Fulvestrant is FDA approved for the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. The recommended dose is 250 mg administered intramuscularly (buttock) per month, as either a single 5 mL injection or two 2.5 mL injections.
When used (off-label) to mitigate the estrogenic side effects of anabolic/androgenic steroid use, male athletes and bodybuilders may find a similar dose to be beneficial.
Fulvestrant is available in more than one dozen countries. At the present time, all fulvestrant in circulation is likely to be of the Faslodex brand name. The drug itself is exceedingly expensive, and as a result is not widely traded on the black market.
Wlliam Llewellyn (2011) - Anabolics