pegloticase (Rx)

Brand and Other Names:Krystexxa
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution

  • 8mg/mL

Gout

Indicated for treatment of chronic gout in adults refractory to conventional treatment

8 mg IV infusion q2wk coadministered with methotrexate 15 mg PO qWeek

If coadministering with methotrexate, initiate weekly methotrexate and folic acid or folinic acid supplementation at least 4 weeks before to initiating, and throughout pegloticase treatment

Pegloticase alone may be used in patients for whom methotrexate is contraindicated or not clinically appropriate

Dosage Modifications

Renal impairment

  • No dosage adjustment required

Hepatic impairment

  • Not studied

Dosing Considerations

Limitations of use

  • Not recommended for asymptomatic hyperuricemia

Precautions before initiating

  • Discontinue oral urate-lowering medications
  • Do NOT initiate oral urate-lowering agents while taking pegloticase

Monitoring

  • Risk of infusion reactions, including anaphylaxis, is higher in patients who have lost therapeutic response
  • Monitor serum uric acid levels before each infusion and discontinue treatment if levels increase to >6 mg/dL, particularly when 2 consecutive levels >6 mg/dL are observed

<18 years: Safety and efficacy not established

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Interactions

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            Adverse Effects

            >10%

            Gout flares (77%)

            Infusion reactions (26%)

            Nausea (12%)

            Urticaria (10.6%)

            1-10%

            Chest discomfort (9.5%)

            Chest pain (9.5%)

            Erythema (9.5%)

            Pruritus (9.5%)

            Nasopharyngitis (7%)

            Anaphylaxis (5%)

            Postmarketing Reports

            Hemolysis and methemoglobinemia in patients with G6PD deficiency

            Congestive heart failure

            Asthenia

            Malaise

            Peripheral swelling

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            Warnings

            Black Box Warnings

            Anaphylaxis and infusion reactions have been reported; these reactions may occur with any infusion, including the first, and typically manifest within 2 h of infusion (although delayed-type hypersensitivity has also been reported)

            Only administer in a healthcare setting, and monitor for appropriate period following infusion

            Premedicate with antihistamines and corticosteroids

            Risk for anaphylaxis is higher if serum uric acid level >6 mg/dL, monitor serum uric acid levels before infusion and consider discontinuing if levels increase to >6 mg/dL (particularly if 2 consecutive levels of >6 mg/dL are observed)

            Do not administer to patients with history of G6PD Deficiency; Screen patients at risk for G6PD Deficiency prior to initiating therapy; Life threatening hemolytic reactions and methemoglobinemia have been reported in these patients

            Contraindications

            History of serious hypersensitivity, including anaphylaxis, to pegloticase or its components

            G6PD-deficiency (increased risk of hemolysis and methemoglobinemia)

            Cautions

            Life threatening hemolytic reactions and methemoglobinemia reported with G6PD deficiency; screen patients at risk for G6PD deficiency before initiating (eg, patients of African, Mediterranean [including Southern European and Middle Eastern], and Southern Asian ancestry); do not administer to patients with G6PD deficiency

            Gout flares may occur after initiating owing to changing serum uric acid levels resulting in mobilization of urate from tissue deposits; gout flare prophylaxis with an NSAID or colchicine is recommended starting at least 1 week before starting and during pegloticase treatment and for at least 6 months, unless medically contraindicated or not tolerated

            Exacerbation of pre-existing CHF reported; exercise caution when using this drug in patients who have congestive heart failure and monitor patients closely following infusion

            No controlled trial data are available regarding safety and efficacy of retreatment with pegloticase after stopping treatment for >4 weeks; owing to immunogenicity of pegloticase, patients receiving retreatment may be at increased risk of anaphylaxis and infusion reactions

            Anaphylaxis

            • Anaphylaxis reported; pretreat with antihistamines and corticosteroids before each infusion; risk increased with uric acid level >6 mg/dL (especially when 2 consecutive level >6 mg/dL observed); monitor serum uric acid levels prior to infusions and discontinue treatment if levels increase to above 6 mg/dL
            • Therapy should be administered in a healthcare setting by healthcare providers prepared to manage anaphylaxis; patients should be pre-treated with antihistamines and corticosteroids
            • Anaphylaxis may occur with any infusion, including a first infusion, and generally manifests within 2 hr of the infusion; however, delayed-type hypersensitivity reactions have also been reported
            • Patients should be closely monitored for appropriate period of time for anaphylaxis after administration of the drug; patients should be informed of the symptoms and signs of anaphylaxis and instructed to seek immediate medical care should anaphylaxis occur after discharge from the healthcare setting

            Infusion reactions

            • Infusion reactions may occur; manifestations include urticaria, dyspnea, chest discomfort, chest pain, erythema, and pruritus (symptoms overlap with anaphylaxis); risk of infusion reactions increased with uric acid level >6 mg/dL; monitor serum uric acid levels prior to infusions and discontinue treatment if levels increase to above 6 mg/dL
            • Because of the possibility that concomitant use of oral urate-lowering therapy and this medication may potentially blunt the rise of serum uric acid levels, it is recommended that before starting therapy patients discontinue oral urate-lowering medications and not institute therapy with oral urate-lowering agents while taking this medication
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            Pregnancy & Lactation

            Pregnancy

            There are no adequate and well-controlled studies in pregnant women

            Animal data

            • No structural abnormalities were observed on animal reproduction studies, when pegloticase administered by subcutaneous injection to pregnant rats and rabbits during period of organogenesis at doses up to 50 and 75 times, respectively, the maximum recommended human dose (MRHD); decreases in mean fetal and pup body weights were observed at approximately 50 and 75 times MRHD, respectively

            Lactation

            Not known whether drug is excreted in human milk; drug should not be used when breastfeeding unless clear benefit to mother can overcome unknown risk to newborn/infant.

            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

            Recombinant, pegylated uric acid specific enzyme; achieves its therapeutic effect by catalyzing oxidation of uric acid to allantoin, thereby lowering serum uric acid levels

            Pharmacokinetics

            Onset of action: 24 hr

            Duration: 12.5 days

            Half-life: 14 days

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            Administration

            IV Compatibilities

            Solution: 0.9% NaCl, 0.45% NaCl

            IV Preparation

            IV infusion

            • Withdraw 1 mL from vial (discard any unused portion) and add to a single 250 mL bag of 0.9% or 0.45% NaCl
            • Invert infusion bag a number of times to ensure thorough mixing
            • DO NOT SHAKE
            • Stable for 4 hr at room temperature (20-25ºC [68-77ºF]); however, recommended to store refrigerated and use within 4 hr

            IV Administration

            Do NOT administer as IV push or bolus

            Premedicate with antihistamines and corticosteroids

            Administer IV infusion over at least 2 hr via gravity feed or volumetric infusion pump

            If an infusion reaction occurs, may slow, or stop and restart infusion at slower rate, at the discretion of the physician

            Infusion reactions can occur after completion; observe patient ~1 hr post-infusion

            Storage

            Protect from light

            Do not shake

            Unopened vials

            • Refrigerate at 2-8ºC (36-46ºF) in original carton

            Admixture

            • Recommended to refrigerate at 2-8ºC (36-46ºF)
            • May store at room temperature (20-25ºC [68-77ºF])
            • Use within 4 hr
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            Patient Handout

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            Formulary

            FormularyPatient Discounts

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            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.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
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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.