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fulvestrant (Rx)Brand and Other Names:Faslodex

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution

  • 50mg/mL
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Breast Cancer

Monotherapy

  • Indicated for hormone receptor (HR) positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy
  • 500 mg IM on days 1, 15, 29, then once monthly thereafter

Combination with palbociclib

  • Indicated for HR-positive, (HER2)-negative advanced or metastatic breast cancer in combination with palbociclib in women (regardless of menopausal status) with disease progression after endocrine therapy
  • Fulvestrant 500 mg IM on days 1, 15, 29, and once monthly thereafter
  • Palbociclib starting dose: 125 mg PO qDay with food x21 days followed by 7 days off therapy to comprise a complete cycle of 28 days
  • Pre/perimenopausal women treated with the palbociclib combination should be treated with luteinizing hormone-releasing hormone (LHRH) agonists according to current clinical practice standards

Dosage Modifications

Hepatic impairment

  • Moderate hepatic impairment (Child-Pugh class B): 250 mg IM on days 1, 15, 29, then once monthly thereafter
  • Severe impairment: Not studied

Dosage Forms & Strengths

injectable solution

  • 50mg/mL
more...

Precocious Puberty (Off-label)

Indicated in females for progressive precocious puberty associated with McCune-Albright syndrome

4 mg/kg IM qMonth 

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%)
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Interactions

Interaction Checker

fulvestrant and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            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

            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

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            Warnings

            Contraindications

            Hypersensitivity to fulvestrant or any component of formulation

            Cautions

            Caution in bleeding diathesis, thrombocytopenia, therapeutic anticoagulation

            Hepatic impairment; decrease dose to 250 mg dose with moderate hepatic impairment (Child-Pugh class B)

            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

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            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

            Lactation

            Excretion in human milk unknown; do not breastfeed

            Pregnancy Category: D

            Lactation: excretion in milk unknown; contraindicated

            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.

            more...
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            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%

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            Administration

            IM Administration

            Administer IM in buttocks slowly (over 1-2 minutes per injection) as two 5-mL (250 mg) injections, on in each buttock (or one 5-mL IM injection for moderate hepatic impairment)

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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