Fulvestrant

Fulvestrant Uses, Dosage, Side Effects, Food Interaction and all others data.

Fulvestrant is a drug treatment of hormone receptor (HR)-positive metastatic breast cancer in post-menopausal women with disease progression following anti-estrogen therapy. It is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor. While it is used as monotherapy for the treatment of breast cancers, it is also used in combination with alpelisib for the treatment of HR-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer

Fulvestrant for intramuscular administration is an estrogen receptor antagonist without known agonist effects.

Trade Name Fulvestrant
Availability Prescription only
Generic Fulvestrant
Fulvestrant Other Names Fulvestrant
Related Drugs Arimidex, Ibrance, Femara, Aromasin, Faslodex, Verzenio, Afinitor, Xeloda, Herceptin, Lynparza
Weight 50mg/ml,
Type Injection, Intramuscular Solution, Intramuscular
Formula C32H47F5O3S
Weight Average: 606.78
Monoisotopic: 606.316607362
Protein binding

99% (mainly VLDL, LDL, and HDL)

Groups Approved, Investigational
Therapeutic Class
Manufacturer Glenmark Pharmaceuticals Europe Ltd
Available Country United Kingdom, United States
Last Updated: September 19, 2023 at 7:00 am
Fulvestrant
Fulvestrant

Uses

Fulvestrant is an estrogen receptor antagonist used to treat HR+ breast cancer that may also be HER2-.

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.

Fulvestrant is also used to associated treatment for these conditions: Advanced or Metastatic Breast Cancer, Refractory, advanced Breast cancer, Refractory, metastatic Breast cancer

How Fulvestrant works

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.

Toxicity

There is no clinical experience with overdosage in humans.

Food Interaction

No interactions found.

Fulvestrant Disease Interaction

Major: hepatic dysfunctionModerate: bleeding

Volume of Distribution

  • 3 to 5 L/kg

Half Life

40 days

Elimination Route

Fulvestrant was rapidly cleared by the hepatobiliary route with excretion primarily via the feces (approximately 90%). Renal elimination was negligible (less than 1%).

Innovators Monograph

You find simplified version here Fulvestrant

*** Taking medicines without doctor's advice can cause long-term problems.
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