Pegloticase
- Atc Codes:M04AX02
- CAS Codes:885051-90-1
- PHARMGKB ID:885051-90-1
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Krystexxa.
Drug combinations
Chemistry
Pegloticase: C~1549~H~2430~N~408~O~448~S~8~ (peptide monomer). Mw: 540. (1) Oxidase, urate (synthetic Sus scrofa variant pigKS-ΔN subunit), homotetramer, amide with α-carboxy-ω-methoxypoly(oxy-1,2-ethanediyl); (2) des-(1-6)-[7-threonine,46-threonine,291-lysine,301-serine]uricase (EC 1.7.3.3, urate oxydase) Sus scrofa (pig) tetramer, non acetylated, carbamates with α-carboxy-ω-methoxypoly(oxyethylene). CAS-885051-90-1.
Peptide monomer
Pharmacologic Category
Antigout Agents; Enzyme. (ATC-Code: M04AX02).
Mechanism of action
Pegloticase is a PEGylated uric acid-specific enzyme which is a recombinant uricase, and achieves its therapeutic effect by catalyzing the oxidation of uric acid to allantoin, thereby lowering serum uric acid. Allantoin is an inert and water-soluble purine metabolite. It is readily eliminated, primarily by renal excretion.
Therapeutic use
Treatment of chronic gout in adult patients refractory to conventional therapy. Not recommended for the treatment of asymptomatic hyperuricemia.
Pregnancy and lactiation implications
Should be used during pregnancy only if clearly needed. Not recommended during lactation.
Unlabeled use
Contraindications
Patients at higher risk for glucose-6-phosphate dehydrogenase (G6PD) deficiency (e.g. those of African and Mediterranean ancestry) should be screened due to the risk of hemolysis and methemoglobinemia.
Warnings and precautions
Anaphylaxis and infusion reactions have been reported to occur during and after administration of pegloticase (should be administered in healthcare settings and by healthcare providers prepared to manage anaphylaxis and infusion reactions; patients should be pre-medicated with antihistamines and corticosteroids and closely monitored for an appropriate period of time for anaphylaxis after administration). Monitor serum uric acid levels prior to infusions and consider discontinuing treatment if levels increase to above 6 mg/dL, particularly when 2 consecutive levels above 6 mg/dL are observed. An increase in gout flares is frequently observed upon initiation of anti-hyperuricemic therapy (need not be discontinued). Caution in patients who have congestive heart failure (monitor patients closely following infusion). Due to immunogenicity, patients receiving re-treatment may be at increased risk of anaphylaxis and infusion reactions (monitor carefully).