Mechanism of Action
FASLODEX is an estrogen receptor antagonist with no known agonist activity7
Watch this video to learn more about how FASLODEX works. Please note: symbols in the video are for visual representation only and do not accurately depict the appearance of molecules.
FASLODEX: ER antagonist without known agonist effects
FASLODEX blocks estrogen binding at the receptor level and inhibits estrogen-stimulated cell division7-9
- Binding competitively at the ER, creating a conformational change7,8,10,11
- Blocking the binding of estrogen to the ER7,9
- Accelerating degradation of the ER and inhibiting both receptor dimerization and translocation to the nucleus, resulting in inhibition of estrogen-stimulated cell division7-9
Tumors exposed to FASLODEX continue to express ER and may remain hormone responsive.12,13
FASLODEX is indicated for the treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease
progression following antiestrogen therapy.
IMPORTANT SAFETY INFORMATION:
Click Here for Additional Safety Information
FASLODEX is contraindicated in patients with known hypersensitivity to the drug or to
any of its components. Hypersensitivity reactions, including urticaria and angioedema have been reported in association with FASLODEX.
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