Fulvestrant (Faslodex)

General information

Class/mechanism: Estrogen receptor antagonist; competitively binds to the estrogen receptor (ER) and downregulates estrogen receptor expression.
Route: IM
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

• ER/PR+ Breast cancer

Patient drug information

• Fulvestrant (Faslodex) package insert
• Fulvestrant (Faslodex) patient drug information (Chemocare)
• Fulvestrant (Faslodex) patient drug information (UpToDate)

History of changes in FDA indication

• 2002-04-25: Initial FDA approval for the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy. (Based on Trial 0021 & Trial 0020)
• 2010-09-10: Approved at a dose of 500 mg for hormone receptor positive metastatic breast cancer (full details missing). (Based on CONFIRM)
• 2016-03-02: Approved for the treatment of HR-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer in combination with palbociclib in women with disease progression after endocrine therapy. (Based on PALOMA-3)
• 2017-08-25: Approved for a new indication as monotherapy for the treatment of hormone receptor (HR) positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer in postmenopausal women not previously treated with endocrine therapy. (Based on FALCON)
• 2017-11-14: Approved for treatment of HR-positive, HER2-negative advanced or metastatic breast cancer in combination with abemaciclib in women with disease progression after endocrine therapy. (Based on MONALEESA-3)
• 2019-03-11: Approved for the treatment of HR-positive, HER2-negative advanced or metastatic breast cancer in postmenopausal women, in combination with ribociclib, as initial endocrine based therapy or following disease progression on endocrine therapy. (Based on MONARCH 2)

History of changes in EMA indication

• 2004-03-09: Initial authorization

History of changes in Health Canada indication

• 2004-02-17: Initial notice of compliance
• Uncertain date: Indicated for treatment of estrogen receptor-positive, human epidermal growth receptor 2 (HER2)negative locally advanced or metastatic breast cancer in postmenopausal women not previously treated with endocrine therapy.
• Uncertain date: Indicated as hormonal treatment of locally advanced or metastatic breast cancer in postmenopausal women, regardless of age, who have disease progression following prior anti-estrogen therapy.

History of changes in PMDA indication

• 2011-09-26: Initial approval for the treatment of postmenopausal breast cancer.
• 2017-09-27: Revised indication and a new dosage for the treatment of breast cancer.

Also known as

• Code names: ICI-182780, ZD-9238
• Brand names: Faslodex, Fasnorm, Fulvenat, Fulvidax, Fuvestrol