FULVESTRANT EVER PHARMA
EVER Pharama
Identification
- Active ingredient (INN)
- FLUVESTRANT
- Internal code
- 05 E 164
- Country of Origin
- Austria
- Pharmaceutical form
- IM Injectable Solution (Pre-filled Syringe)
- Prescription List
- Highly Regulated (List I)
- Packaging
- b/2 seringue pre-remplies de 5ml
DAWA Clinical Workbench v2.0
Information may not be accurate. Always consult a physician, pharmacist, or specialist before acting on any data shown here.
Description
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.
Indications
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.
Pharmacodynamics
Fulvestrant for intramuscular administration is an estrogen receptor antagonist without known agonist effects.
Metabolism
of fulvestrant appears to involve combinations of a number of possible biotransformation pathways analogous to those of endogenous steroids, including oxidation, aromatic hydroxylation, conjugation with glucuronic acid and/or sulphate at the and 17 positions of the steroid nucleus, and oxidation of the side chain sulphoxide.
Identified metabolites are either less active or exhibit similar activity to fulvestrant in antiestrogen models.
Studies using human liver preparations and recombinant human enzymes indicate that cytochrome P-450 3A4 (CYP 3A4) is the only P-450 isoenzyme involved in the oxidation of fulvestrant; however, the relative contribution of P-450 and non-P-450 routes in vivo is unknown.
Route of Elimination
Fulvestrant was rapidly cleared by the hepatobiliary route with excretion primarily via the feces (approximately 90%).
Renal elimination was negligible (less than 1%).
Adverse Effects
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Toxicity
There is no clinical experience with overdosage in humans.