Fulvestrant is an estrogen receptor antagonist used to treat HR+ breast cancer that may also be HER2-. Fulvestrant is a drug treatment of hormone receptor (HR)-positive metastatic breast cancer in post-menopausal women with disease progression following anti-estrogen therapy.
- Mechanism
- Curator reviewed
Fulvestrant competitively and reversibly binds to estrogen receptors present in cancer cells and achieves its anti-estrogen effects through two separate mechanisms. First, fulvestrant binds to the receptors and downregulates them so that estrogen is no longer able to bind to these receptors. Second, fulvestrant degrades the estrogen receptors to which it is bound. Both of these mechanisms inhibit the growth of tamoxifen-resistant as well as estrogen-sensitive human breast cancer cell lines.
- Primary indication
- For the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy, as monotherapy or in combination with other antineoplastic agents.Curator reviewed · 8 structured indications
- Formula / weight
- C32H47F5O3S · 606.78 g/mol (avg)
- First approval
- Canada, 2004 · United States, 2010 · European Union, 2016
- Code names
- ICI-182780 · ZD-9238
- Brand names
Resolves to
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Which drugs share a target with Fulvestrant, and which of those have an active Phase 3 trial?
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