Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 250mg/5mL
Advanced Breast Cancer
Also see Administration
Monotherapy
- Indicated for hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative in postmenopausal women not previously treated with endocrine therapy
- Indicated for HR-positive in postmenopausal women with disease progression following endocrine therapy
- 500 mg IM on days 1, 15, 29, then once monthly thereafter
Combination therapy with palbociclib or abemaciclib
- Indicated HR-positive, HER2-negative advanced or metastatic breast cancer in women with disease progression after endocrine therapy
- Fulvestrant 500 mg IM on days 1, 15, 29, and once monthly thereafter AND
- Palbociclib 125 mg PO qDay for days 1-21 of each 28-day cycle OR
- Abemaciclib 150 mg PO BID
- Continue until disease progression or unacceptable toxicity
- Pre/perimenopausal women treated with the palbociclib/abemaciclib combination should be treated with luteinizing hormone-releasing hormone (LHRH) agonists according to current clinical practice standards
Combination with ribociclib
- Indicated HR-positive, HER2-negative advanced or metastatic breast cancer in postmenopausal women in combination with ribociclib
- Administer as initial endocrine based therapy or following disease progression on endocrine therapy
- Fulvestrant 500 mg IM on days 1, 15, 29, and once monthly thereafter AND
- Ribociclib 600 mg for days 1-21 of each 28-day cycle
- Continue until disease progression or unacceptable toxicity
- Pre/perimenopausal women treated with the ribociclib combination should be treated with luteinizing hormone-releasing hormone (LHRH) agonists according to current clinical practice standards
Dosage Modifications
Hepatic impairment
- Mild (Child-Pugh A): No dosage adjustment required
- Moderate (Child-Pugh B): 250 mg IM on days 1, 15, 29, then once monthly thereafter
- Severe (Child-Pugh C): Not studied
Renal impairment
- Negligible amounts of fulvestrant are eliminated in urine
- In clinical trials, fulvestrant concentrations in women with eCrCl ≥30 mL/min were similar to women with normal creatinine
Dosage Forms & Strengths
injectable solution
- 50mg/mL
Precocious Puberty (Off-label)
Indicated in females for progressive precocious puberty associated with McCune-Albright syndrome
Hepatic Impairment
- Dose adjustment may be required, although no specific recommendations defined for children with hepatic impairment (in adults with Child-Pugh class B, the dose is decreased by 50%)
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (1)
- siponimod
siponimod and fulvestrant both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
Minor (2)
- maitake
maitake increases effects of fulvestrant by pharmacodynamic synergism. Minor/Significance Unknown. Maitake mushroom has anti-tumor effects (animal/in vitro research).
- taurine
fulvestrant decreases levels of taurine by unspecified interaction mechanism. Minor/Significance Unknown.
Adverse Effects
>10%
Nausea (26%)
Asthenia (23%)
Pain (19%)
Vasodilatation (18%)
Pharyngitis (16%)
HA (15%)
Back pain (14%)
Constipation (13%)
Vomiting (13%)
Abd pain (12%)
Diarrhea (12%)
Inj site pain (11%)
1-10%
Cough (10%)
Anorexia (9%)
Peripheral edema (9%)
Chest pain (7%)
Flu-like syndrome (7%)
Rash (7%)
Depression (6%)
Fever (6%)
UTI (6%)
Anemia (5%)
<1%
Angioedema
Leukopenia
Myalgia
Thrombosis
Osteoporosis
Postmarketing Reports
Injection site reaction
Thromboembolic phenomena
Myalgia
Vertigo
Leukopenia
Hypersensitivity reactions including angioedema and urticaria
Vaginal bleeding (mainly during the first 6 weeks after changing from existing hormonal therapy)
Elevated bilirubin, gamma GT, hepatitis, and liver failure
Combination Therapy with Palbociclib
Frequency Not Defined
- Neutropenia
- Leukopenia
- Infections
- Fatigue
- Nausea
- Anemia
- Stomatitis
- Diarrhea
- Thrombocytopenia
- Vomiting
- Alopecia
- Rash
- Decreased appetite
- Pyrexia
<10%
- Asthenia (7.5%)
- Aspartate aminotransferase increased (7.5%)
- Dysgeusia (6.7%)
- Epistaxis (6.7%)
- Lacrimation increased (6.4%)
- Dry skin (6.1%)
- Alanine aminotransferase increased (5.8%)
- Vision blurred (5.8%)
- Dry eye (3.8%)
- Febrile neutropenia (0.9%)
Warnings
Contraindications
Hypersensitivity to fulvestrant or any component of formulation
Cautions
Caution in bleeding diathesis, thrombocytopenia, therapeutic anticoagulation
Systemic exposure was increased in patients with moderate hepatic impairment (see Dosage Modifications)
Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception; see Pregnancy section
Therapy can interfere with estradiol measurement by immunoassay, resulting in falsely elevated estradiol levels
Injection site related events including sciatica, neuralgia, neuropathic pain, and peripheral neuropathy reported; caution should be taken while administering therapy at dorsogluteal injection site due to proximity of underlying sciatic nerve
Pregnancy & Lactation
Pregnancy
Based on findings from animal studies and its mechanism of action, fulvestrant can cause fetal harm when administered to a pregnant woman
In animal reproduction studies, administration of fulvestrant to pregnant rats and rabbits during organogenesis resulted in embryo-fetal toxicity at daily doses that are significantly less than the maximum recommended human dose
Advise pregnant women of the potential risk to a fetus
Advise females of reproductive potential to use effective contraception during treatment and for 1 year after the last dose
Pregnancy testing is recommended for females of reproductive potential within 7 days prior to initiating fulvestrant
Lactation
Excretion in human milk unknown
Detected in rat milk
Because of the potential for serious adverse reactions in breastfed infants, advise lactating women not to breastfeed during treatment and for 1 year after the final dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Breast cancer: Competitively binds to estrogen receptors on tumors and other tissue targets, producing nuclear complex that decreases DNA synthesis and inhibits estrogen effects; no estrogen-receptor agonist activity; downregulates estrogen receptors and inhibits breast tumor growth
Precocious puberty (off-label): Estrogen receptor antagonist
Absorption
Peak Plasma Time: 7 days
Duration: Plasma levels detected for 1 month
Distribution
Protein Bound: 99%
Vd: 3-5 L/kg
Metabolism
Via multiple hepatic pathways
Excretion
Half-Life: 40 days
Excretion: Feces >90%; urine <1%
Administration
IM Administration
Also see Dosage Modifications
Administer IM in buttocks slowly over 1-2 minutes; not to exceed 250 mg/5 mL per IM injection site
Discard the empty single use syringe into an approved sharps collector in accordance with applicable regulations and institutional policy
Storage
Store in refrigerator at 2-8°C (36-46°F)
Protect from light, store in the original carton until time of use
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| fulvestrant intramuscular - | 250 mg/5 mL solution |  | |
| fulvestrant intramuscular - | 250 mg/5 mL solution |  | |
| fulvestrant intramuscular - | 250 mg/5 mL solution |  | |
| fulvestrant intramuscular - | 250 mg/5 mL solution |  | |
| Faslodex intramuscular - | 250 mg/5 mL solution |  |
Copyright © 2010 First DataBank, Inc.
Formulary
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