Classifications: antineoplastic; hormone, antiestrogen; Therapeutic: antineoplastic; antiestrogen
Prototype: Tamoxifen citrate
Pregnancy Category: D
Fulvestrant is an estrogen receptor antagonist that selectively binds to the estrogen receptors (ER) of breast cancer cells.
It competes well with estradiol (estrogen) in binding to these receptor sites. Estrogen stimulates the tumor growth of estrogen-sensitive
breast tissue cancer cells in postmenopausal women.
In postmenopausal women, many breast cancers have estrogen receptors (ERs), and the growth of these tumors is stimulated by
estrogen. Therefore, fulvestrant decreases estrogen-sensitive breast tissue tumor growth.
Treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following
Hypersensitivity to fulvestrant; pregnancy (category D); lactation.
Moderate to severe liver impairment; biliary disease; coagulopathy; anticoagulant therapy. Safety and effectiveness in children
Route & Dosage
|Metastatic Breast Cancer
Adult: IM 250 mg once/mo
- Do not administer unless the possibility of pregnancy has been ruled out.
- Break the seal of the white plastic cover on the syringe luer connector to remove the cover with the attached rubber tip cap.
Twist to lock the needle to the luer connector. Remove excess gas from the syringe (a small gas bubble may remain).
- Administer slowly in the buttock.
- Immediately activate needle protection device upon withdrawal from patient by pushing lever arm completely forward until needle
tip is fully covered.
- Store in a refrigerator, 2°8° C (36°46° F) in original container.
Adverse Effects (≥1%)Body as a Whole: Asthenia, pain, injection site pain,
, fever, peripheral edema. CNS:
, anxiety. CV: Vasodilation. GI: Nausea, vomiting, constipation, diarrhea,
anorexia. Hematologic: Anemia
. Musculoskeletal: Bone pain, arthritis
. Respiratory: Pharyngitis, dyspnea, cough. Skin:
7 d. Duration:
1 mo. Distribution:
99% protein bound. Metabolism:
In liver via CYP3A4. Elimination:
90% in feces. Half-Life:
Assessment & Drug Effects
- Monitor for S&S of tumor progression.
- Lab tests: Monitor periodic CBC with differential.
Patient & Family Education
- Use two methods of contraception while taking this drug. Immediately notify physician if you think you are pregnant.
- Report vaginal bleeding to physician. Understand the possibility of drug-induced menstrual irregularities before starting