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

Interaction Checker

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            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (10)

                • certolizumab pegol

                  pegloticase will decrease the level or effect of certolizumab pegol by Other (see comment). Use Caution/Monitor. According to the manufacturer, potential for anti-PEG antibody development that may bind to other pegylated drugs; clinical significance unknown

                • pegademase

                  pegloticase will decrease the level or effect of pegademase by Other (see comment). Use Caution/Monitor. According to the manufacturer, potential for anti-PEG antibody development that may bind to other pegylated drugs; clinical significance unknown

                • pegaptanib

                  pegloticase will decrease the level or effect of pegaptanib by Other (see comment). Use Caution/Monitor. According to the manufacturer, potential for anti-PEG antibody development that may bind to other pegylated drugs; clinical significance unknown

                • pegaspargase

                  pegloticase will decrease the level or effect of pegaspargase by Other (see comment). Use Caution/Monitor. According to the manufacturer, potential for anti-PEG antibody development that may bind to other pegylated drugs; clinical significance unknown

                • pegfilgrastim

                  pegloticase will decrease the level or effect of pegfilgrastim by Other (see comment). Use Caution/Monitor. According to the manufacturer, potential for anti-PEG antibody development that may bind to other pegylated drugs; clinical significance unknown

                • peginterferon alfa 2a

                  pegloticase will decrease the level or effect of peginterferon alfa 2a by Other (see comment). Use Caution/Monitor. According to the manufacturer, potential for anti-PEG antibody development that may bind to other pegylated drugs; clinical significance unknown

                • peginterferon alfa 2b

                  pegloticase will decrease the level or effect of peginterferon alfa 2b by Other (see comment). Use Caution/Monitor. According to the manufacturer, potential for anti-PEG antibody development that may bind to other pegylated drugs; clinical significance unknown

                • pegvaliase

                  pegvaliase, pegloticase. Other (see comment). Use Caution/Monitor. Comment: The majority of patients treated with pegvaliase develop anti-polyethylene glycol (PEG) IgM and IgG antibodies. Risk of coadministration with different PEGylated products is unknown. There is a case report of anaphylaxis following a medroxyprogesterone acetate injectable suspension that contained PEG 3350. Carefully read all drug labels, including OTC drugs to check contents for PEG. Note: Unable to include an exhaustive product list for this interaction.

                • pegvisomant

                  pegloticase will decrease the level or effect of pegvisomant by Other (see comment). Use Caution/Monitor. According to the manufacturer, potential for anti-PEG antibody development that may bind to other pegylated drugs; clinical significance unknown

                • siponimod

                  siponimod and pegloticase 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 (0)

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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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                  Images

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                  Patient Handout

                  Patient Education
                  pegloticase intravenous

                  PEGLOTICASE - INJECTION

                  (peg-LOE-ti-kase)

                  COMMON BRAND NAME(S): Krystexxa

                  WARNING: Pegloticase may rarely cause a serious allergic reaction. This may occur during or after the infusion of the medication. Your doctor will check your blood before each treatment and monitor you closely during and after infusion. Your doctor should prescribe other medications (such as antihistamines, corticosteroids) to help prevent an allergic reaction. However, serious allergic reactions may still occur in a few patients. Get medical help right away if you develop any signs of an allergic reaction, such as rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing, chest discomfort/pain.Do not use this medication if you have a certain metabolic disorder called glucose-6-phosphate dehydrogenase (G6PD) deficiency because it can severely damage your red blood cells leading to anemia (hemolysis). If you are of African, Mediterranean, or Southern Asian descent, you may be at higher risk for G6PD deficiency and should be tested to see if you have this condition before starting this medication.

                  USES: Pegloticase is used to treat gout which has not responded to the usual treatments. It works by lowering high levels of uric acid in your body. Increased uric acid in your body can cause gout.

                  HOW TO USE: Read the Medication Guide provided by your pharmacist before you start using pegloticase and each time you get a refill. If you have any questions, ask your doctor or pharmacist.If you are taking other medications (such as allopurinol, febuxostat) by mouth to lower the level of uric acid in your body, your doctor will direct you to stop the medication before starting and during treatment with pegloticase. Taking these drugs with pegloticase may lessen how well it works.This medication is given by injection into a vein (over at least 2 hours) by a healthcare professional. It is usually given every 2 weeks.Use this medication regularly in order to get the most benefit from it. Remember to receive it every 2 weeks. It may help to mark your calendar with a reminder.You may experience more gout attacks for several months after starting this medicine while your body removes extra uric acid. Your doctor may prescribe additional medication (such as colchicine, nonsteroidal anti-inflammatory drugs-NSAIDs) to help prevent and treat these gout attacks.Tell your doctor if your condition lasts or gets worse.

                  SIDE EFFECTS: See also Warning section.Nausea, vomiting, sore throat, or runny nose may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

                  PRECAUTIONS: See also Warning section.Before receiving pegloticase, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: a certain metabolic disorder (G6PD deficiency), favism, heart failure.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.

                  DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Do not take other medications (such as allopurinol, febuxostat) taken by mouth to lower the level of uric acid in your body before and during treatment with pegloticase. (See also How to Use section.)

                  OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

                  NOTES: Laboratory and/or medical tests (such as uric acid levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

                  MISSED DOSE: It is important to get each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule.

                  STORAGE: Not applicable. This medication is given in a hospital or clinic and will not be stored at home.

                  Information last revised February 2022. Copyright(c) 2022 First Databank, Inc.

                  IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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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.
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                  NC NOT COVERED – Drugs that are not covered by the plan.
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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.