fulvestrant (Rx)

Brand and Other Names:Faslodex
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution

  • 250mg/5mL

Breast Cancer

Also see Administration

Monotherapy

  • Indicated for hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer in postmenopausal women not previously treated with endocrine therapy, OR HR-positive advanced breast cancer 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 combination with palbociclib or abemaciclib 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 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

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

and fulvestrant

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    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

            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%)
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            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

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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

            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.

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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

            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

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

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            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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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.