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 |
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
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
