ChemicalProperties White Powder
UsageA novel steroidal estrogen antagonist reported to lack any partial agonistactivity. Antineoplastic (hormonal).
BiologicalActivity A high affinity estrogen receptor antagonist (IC 50 = 0.29nM), devoid of any partial agonism both in vitro and in vivo . Also highaffinity agonist at the membrane estrogen receptor GPR30.
ProductCategories: Intermediates & Fine Chemicals;Pharmaceuticals;NuclearReceptors;Chiral Reagents;Steroids;Sulfur & SeleniumCompounds;FASLODEX;Anti-cancer&immunity
Fulvestrant Acetate (trade name Faslodex, by AstraZeneca) is a drug treatment of hormone receptor-positive metastatic breastcancer in postmenopausal women with disease progression following anti-estrogentherapy. It is a completeestrogen receptor antagonist with no agonisteffects, which in addition, accelerates the proteasomal degradation of theestrogen receptor. The drug has poor oral bioavailability, and is administeredmonthly via intramuscular injection.
Fulvestrant Acetate is a selective estrogen receptor degrader (SERD).It is indicated for the treatment of hormone receptor positivemetastatic breast cancer in postmenopausal women with diseaseprogression following anti-estrogen therapy. Fulvestrant Acetate provides effective second-line therapy in metastaticor locally advanced breast cancer for postmenopausal women who relapse orprogress after previous endocrine therapy. Four clinical trials in this setting showed similar efficacy to the otherhormonal agents (aromatase inhibitors and tamoxifen) with good tolerabilityprofile. Fulvestrant had a lower incidence of joint disorders. A Phase 2 clinical trial, sponsored by Atossa Genetics, is beingconducted by Dr. Sheldon Feldman, President of the The American Society ofBreast Surgeons, at Columbia University Breast Center in New York City on theuse of Fulvestrant Acetate administered through the microcatheterinto the lactiferous duct as neoadjuvant treatment forductal carcinoma in situand invasive breast cancer.