Pegloticase

Identification

Summary

Pegloticase is a recombinant uricase used for the treatment of chronic gout in adult patients refractory to conventional therapy.

Brand Names

Krystexxa

Generic Name

Pegloticase

DrugBank Accession Number

DB09208

Background

Pegloticase is a porcine recombinant PEGylated uricase indicated for the treatment of chronic gout in adult patients that do not respond to other types of therapies.⁵ Pegloticase has a similar activity to rasburicase, an enzyme that metabolizes uric acid to allantoin. In gout patients treated with pegloticase, the conversion of uric acid to allantoin leads to lower plasma uric acid concentrations.⁵

Pegloticase has a longer terminal elimination half-life thanks to the addition of a polyethylene glycol (PEG) group. Therefore therapeutic drug levels can be maintained with infrequent and relatively low pegloticase doses.³ The PEG group also gives pegloticase a lower potential to induce an immune response.³ However, cases of anaphylaxis and infusion reactions have been reported in patients treated with this drug.⁵ Pegloticase was approved by the FDA in 2014, and in 2022, the drug label included the co-administration of pegloticase and methotrexate.⁵

Type

Biotech

Groups

Approved, Investigational

Biologic Classification

Protein Based Therapies
Recombinant Enzymes

Protein Chemical Formula

C₁₅₄₉H₂₄₃₀N₄₀₈O₄₄₈S₈

Protein Average Weight

34192.8533 Da

Sequences

> Pegloticase
TYKKNDEVEFVRTGYGKDMIKVLHIQRDGKYHSIKEVATTVQLTLSSKKDYLHGDNSDVI
PTDTIKNTVNVLAKFKGIKSIETFAVTICEHFLSSFKHVIRAQVYVEEVPWKRFEKNGVK
HVHAFIYTPTGTHFCEVEQIRNGPPVIHSGIKDLKVLKTTQSGFEGFIKDQFTTLPEVKD
RCFATQVYCKWRYHQGRDVDFEATWDTVRSIVLQKFAGPYDKGEYSPSVQKTLYDIQVLT
LGQVPEIEDMEISLPNIHYLNIDMSKMGLINKEEVLLPLDNPYGKITGTVKRKLSSRL

References:

1. United States Adopted Name (USAN): Pegloticase statement on a non-propietary name adopted by the USAN Council [Link]

Download FASTA Format

Synonyms

• Pegloticase
• Puricase

Pharmacology

Indication

Pegloticase is a PEGylated uric acid specific enzyme indicated for the treatment of chronic gout in adult patients refractory to conventional therapy.⁵

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Associated Conditions

• Chronic, refractory Gout

Contraindications & Blackbox Warnings

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Pharmacodynamics

Pegloticase is a uricase enzyme conjugated with mPEG with an average degree of substitution of 40.8 moles of mPEG/mole of protein.⁶ In patients treated with 8 mg of pegloticase, mean plasma uric acid levels were 0.7 mg/dL approximately 24 hours after the first dose.⁵ In comparison, subjects in the placebo group had a mean plasma uric acid level of 8.2 mg/dL. The decrease in plasma uric acid was sustained for long periods. Patients treated with 8-12 mg of pegloticase had a uric acid concentration equal to or lower than 6 mg/dL for more than 300 h.⁵

Cases of anaphylaxis have been reported in patients treated with pegloticase. In most cases, anaphylaxis manifests within 2 hours of infusion; however, delayed hypersensitivity reactions may also occur. Anaphylaxis risk is higher in patients with uric acid levels above 6 mg/dL.⁵ In patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency, pegloticase may lead to life-threatening hemolytic reactions and methemoglobinemia. Patients treated with pegloticase may also experience infusion reactions, gout flares, and congestive heart failure.⁵

Mechanism of action

Gout is characterized by the presence of hyperuricemia, a biochemical abnormality where the concentration of serum urate is higher or equal to 6.8 mg/dl.¹ Pegloticase is a PEGylated recombinant modified mammalian urate oxidase (uricase) that converts uric acid into allantoin, an inert and highly water-soluble metabolite, with hydrogen peroxide and carbon dioxide as by-products of this reaction.^5,6,4 Allantoin is excreted by the kidneys, and this reduces the amount of uric acid in serum. The reduction in serum uric acid induces a concentration gradient that promotes the migration of urate from joints and tissues, making it readily available for allantoin conversion.^5,6

Target	Actions	Organism
AUric acid	substrate metabolizer	Humans

Absorption

In patients with symptomatic gout given single-dose intravenous infusions of pegloticase (0.5 to 12 mg), maximum serum concentrations of pegloticase increased in a dose proportional manner.⁵ The AUC increased linearly up to a dose of 8 mg.² Pegloticase administered intravenously has a T_max of 2.25 h (range from 1.92 to 4.25 h), a C_max of 2.17 µg/ml (range from 1.25 to 4.77 µg/ml), and an AUC_0-t of 445 h⋅µg/ml (range from 223 to 1040 h⋅µg/ml).⁶ Since pegloticase is administered intravenously, it is expected that it has a bioavailability close to 100%. The pharmacokinetic profile of pegloticase is not significantly influenced by age, sex, weight, and creatinine clearance; however, it is affected by body surface area and anti-pegloticase antibodies.⁵

Volume of distribution

The volume of distribution of pegloticase ranges from 5 to 10 L.²

Protein binding

This pharmacokinetic property has not been studied.

Metabolism

As a recombinant enzyme, pegloticase is expected to be metabolized by proteases throughout the body.

Route of elimination

Nonclinical studies suggest that pegloticase is renally excreted. Due to the PEG moiety pegloticase, urinary excretion is likely to be the primary route of elimination.⁶

Half-life

In patients with symptomatic gout given single-dose intravenous infusions of pegloticase (0.5 to 12 mg), half-life ranged from 6.4 to 13.8 days. The mean plasma half-life of pegloticase was 300 hr or 12.5 days.² In a second study where gout patients were given 4 to 12 mg of pegloticase intravenously every 2 or 4 weeks, the mean terminal elimination half-life of pegloticase in serum was approximately 2 weeks long, ranging from 170 to 1049 hours.³

Clearance

In gout patients given 4 to 12 mg of pegloticase intravenously every 2 or 4 weeks, clearance was ​​0.0615 L/month/kg.³

Adverse Effects

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Toxicity

No pegloticase overdose cases have been reported. The single maximum intravenous dose that has been administered is 12 mg as uricase protein.⁵ Patients experiencing an overdose are at an increased risk of severe adverse effects such as anaphylaxis, gout flares and congestive heart failure. The drug label recommends to monitor patients suspected of experiencing a pegloticase overdose, and initiate general supportive measures as no specific antidote has been identified.⁵

The carcinogenic and genotoxic potential of pegloticase has not been evaluated. At doses up to 40 mg/kg, pegloticase did not show evidence of fertility impairment in rats (dose equivalent to 50 times the maximum recommended human dose.⁵

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Interacting Gene/Enzyme	Allele name	Genotype(s)	Defining Change(s)	Type(s)	Description	Details
Glucose-6-phosphate 1-dehydrogenase	Villeurbanne	Not Available	1000_1002delACC	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Torun	Not Available	1006A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Sunderland	Not Available	105_107delCAT	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Iwatsuki	Not Available	1081G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Serres	Not Available	1082C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Tondela	Not Available	1084_1101delCTGAACGAGCGCAAGGCC	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Loma Linda	Not Available	1089C->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Aachen	Not Available	1089C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Tenri	Not Available	1096A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Montpellier	Not Available	1132G>A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Calvo Mackenna	Not Available	1138A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Riley	Not Available	1139T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Olomouc	Not Available	1141T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Tomah	Not Available	1153T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Lynwood	Not Available	1154G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Madrid	Not Available	1155C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Iowa, Walter Reed, Springfield	Not Available	1156A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Beverly Hills, Genova, Iwate, Niigata, Yamaguchi	Not Available	1160G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Hartford	Not Available	1162A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Praha	Not Available	1166A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Krakow	Not Available	1175T>C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Wisconsin	Not Available	1177C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Nashville, Anaheim, Portici	Not Available	1178G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Alhambra	Not Available	1180G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Bari	Not Available	1187C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Puerto Limon	Not Available	1192G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Covao do Lobo	Not Available	1205C>A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Clinic	Not Available	1215G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Utrecht	Not Available	1225C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Suwalki	Not Available	1226C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Riverside	Not Available	1228G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Japan, Shinagawa	Not Available	1229G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Kawasaki	Not Available	1229G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Munich	Not Available	1231A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Georgia	Not Available	1284C->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Sumare	Not Available	1292T->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Telti/Kobe	Not Available	1318C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Santiago de Cuba, Morioka	Not Available	1339G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Harima	Not Available	1358T->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Figuera da Foz	Not Available	1366G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Amiens	Not Available	1367A>T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Bangkok Noi	Not Available	1376G->T, 1502T->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Fukaya	Not Available	1462G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Campinas	Not Available	1463G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Buenos Aires	Not Available	1465C>T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Arakawa	Not Available	1466C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Brighton	Not Available	1488_1490delGAA	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Kozukata	Not Available	159G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Amsterdam	Not Available	180_182delTCT	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	No name	Not Available	202G->A, 376A->G, 1264C>G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Swansea	Not Available	224T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Urayasu	Not Available	281_283delAGA	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Vancouver	Not Available	317C->G544C->T592C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Mt Sinai	Not Available	376A->G, 1159C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Plymouth	Not Available	488G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Volendam	Not Available	514C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Shinshu	Not Available	527A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Chikugo	Not Available	535A->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Tsukui	Not Available	561_563delCTC	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Pedoplis-Ckaro	Not Available	573C>G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Santiago	Not Available	593G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Minnesota, Marion, Gastonia, LeJeune	Not Available	637G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Cincinnati	Not Available	637G->T, 1037A->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Harilaou	Not Available	648T->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	North Dallas	Not Available	683_685delACA	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Asahikawa	Not Available	695G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Durham	Not Available	713A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Stonybrook	Not Available	724_729delGGCACT	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Wayne	Not Available	769C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Aveiro	Not Available	806G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Cleveland Corum	Not Available	820G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Lille	Not Available	821A>T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Bangkok	Not Available	825G>C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Sugao	Not Available	826C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	La Jolla	Not Available	832T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Wexham	Not Available	833C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Piotrkow	Not Available	851T>C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	West Virginia	Not Available	910G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Omiya	Not Available	921G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Nara	Not Available	953_976delCCACCAAAGGGTACCTGGAC GACC	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Manhattan	Not Available	962G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Rehevot	Not Available	964T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Honiara	Not Available	99A->G / 1360C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Tokyo, Fukushima	Not Available	1246G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Chatham	Not Available	1003G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Fushan	Not Available	1004C->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Partenope	Not Available	1052G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Ierapetra	Not Available	1057C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Anadia	Not Available	1193A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Abeno	Not Available	1220A->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Surabaya	Not Available	1291G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Pawnee	Not Available	1316G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	S. Antioco	Not Available	1342A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Cassano	Not Available	1347G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Hermoupolis	Not Available	1347G->C / 1360C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Union,Maewo, Chinese-2, Kalo	Not Available	1360C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Andalus	Not Available	1361G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Cosenza	Not Available	1376G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Canton, Taiwan- Hakka, Gifu-like, Agrigento-like	Not Available	1376G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Flores	Not Available	1387C->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Kaiping, Anant, Dhon, Sapporo-like, Wosera	Not Available	1388G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Kamogawa	Not Available	169C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Costanzo	Not Available	179T>C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Amazonia	Not Available	185C->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Songklanagarind	Not Available	196T->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Hechi	Not Available	202G->A / 871G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Namouru	Not Available	208T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Bao Loc	Not Available	352T>C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Crispim	Not Available	375G->T, 379G->T383T->C384C>T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Acrokorinthos	Not Available	376A->G / 463C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Santa Maria	Not Available	376A->G / 542A->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Ananindeua	Not Available	376A->G / 871G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Vanua Lava	Not Available	383T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Valladolid	Not Available	406C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Belem	Not Available	409C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Liuzhou	Not Available	442G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Shenzen	Not Available	473G>A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Taipei “Chinese- 3”	Not Available	493A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Toledo	Not Available	496C>T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Naone	Not Available	497G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Nankang	Not Available	517T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Miaoli	Not Available	519C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Mediterranean, Dallas, Panama‚ Sassari, Cagliari, Birmingham	Not Available	563C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Coimbra Shunde	Not Available	592C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Nilgiri	Not Available	593G>A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Radlowo	Not Available	679C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Roubaix	Not Available	811G>C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Haikou	Not Available	835A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Chinese-1	Not Available	835A->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Mizushima	Not Available	848A>G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Osaka	Not Available	853C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Viangchan, Jammu	Not Available	871G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Seoul	Not Available	916G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Ludhiana	Not Available	929G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Farroupilha	Not Available	977C->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Chinese-5	Not Available	1024C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Rignano	Not Available	130G>A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Orissa	Not Available	131C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	G6PDNice	Not Available	1380G>C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Kamiube, Keelung	Not Available	1387C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Neapolis	Not Available	1400C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Aures	Not Available	143T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Split	Not Available	1442C->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Kambos	Not Available	148C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Palestrina	Not Available	170G>A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Metaponto	Not Available	172G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Musashino	Not Available	185C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Asahi	Not Available	202G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	A- (202), Ferrara I	Not Available	202G->A / 376A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Murcia Oristano	Not Available	209A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Ube Konan	Not Available	241C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Lagosanto	Not Available	242G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Guangzhou	Not Available	274C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Hammersmith	Not Available	323T->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Sinnai	Not Available	34G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	A- (680)	Not Available	376A->G / 680G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	A- (968), Betica,Selma, Guantanamo	Not Available	376A->G / 968T->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Salerno Pyrgos	Not Available	383T>G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Quing Yan	Not Available	392G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Lages	Not Available	40G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Ilesha	Not Available	466G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Mahidol	Not Available	487G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Malaga	Not Available	542A->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Sibari	Not Available	634A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Mexico City	Not Available	680G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Nanning	Not Available	703C->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Seattle, Lodi, Modena, Ferrara II, Athens-like	Not Available	844G->C	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Bajo Maumere	Not Available	844G->T	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Montalbano	Not Available	854G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Kalyan-Kerala, Jamnaga, Rohini	Not Available	949G->A	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details
Glucose-6-phosphate 1-dehydrogenase	Gaohe	Not Available	95A->G	ADR Inferred	Increased risk of potentially fatal hemolytic anemia and methemoglobinemia.	Details

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Allopurinol	The risk or severity of adverse effects can be increased when Allopurinol is combined with Pegloticase.
Antihemophilic factor (recombinant), PEGylated	The therapeutic efficacy of Antihemophilic factor (recombinant), PEGylated can be decreased when used in combination with Pegloticase.
Bendroflumethiazide	The therapeutic efficacy of Pegloticase can be decreased when used in combination with Bendroflumethiazide.
Benziodarone	The risk or severity of adverse effects can be increased when Benziodarone is combined with Pegloticase.
Benzthiazide	The therapeutic efficacy of Pegloticase can be decreased when used in combination with Benzthiazide.
Certolizumab pegol	The therapeutic efficacy of Pegloticase can be decreased when used in combination with Certolizumab pegol.
Chlorothiazide	The therapeutic efficacy of Pegloticase can be decreased when used in combination with Chlorothiazide.
Cyclopenthiazide	The therapeutic efficacy of Pegloticase can be decreased when used in combination with Cyclopenthiazide.
Cyclothiazide	The therapeutic efficacy of Pegloticase can be decreased when used in combination with Cyclothiazide.
Damoctocog alfa pegol	The therapeutic efficacy of Damoctocog alfa pegol can be decreased when used in combination with Pegloticase.

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Food Interactions

No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Krystexxa	Injection, solution	8 mg/1mL	Intravenous	Savient Pharmaceuticals	2010-09-14	Not applicable
Krystexxa	Injection, solution	8 mg/1mL	Intravenous	Horizon Pharma Inc.	2010-09-14	2018-12-31
Krystexxa	Injection, solution	8 mg/1mL	Intravenous	Horizon Therapeutics USA, Inc.	2010-09-14	Not applicable
Krystexxa	Injection, solution, concentrate	8 mg/ml	Intravenous	Crealta Pharmaceuticals Llc	2016-09-08	2016-07-22

Categories

ATC Codes

M04AX02 — Pegloticase

• M04AX — Other antigout preparations
• M04A — ANTIGOUT PREPARATIONS
• M04 — ANTIGOUT PREPARATIONS
• M — MUSCULO-SKELETAL SYSTEM

Drug Categories

• Antigout Preparations
• Compounds used in a research, industrial, or household setting
• Enzymes
• Enzymes and Coenzymes
• Musculo-Skeletal System
• Oxidoreductases
• Pegylated agents
• Recombinant Proteins
• Uric Acid-specific Enzyme

Chemical TaxonomyProvided by Classyfire

Description

Not Available

Kingdom

Organic Compounds

Super Class

Organic Acids

Class

Carboxylic Acids and Derivatives

Sub Class

Amino Acids, Peptides, and Analogues

Direct Parent

Peptides

Alternative Parents

Not Available

Substituents

Not Available

Molecular Framework

Not Available

External Descriptors

Not Available

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

R581OT55EA

CAS number

885051-90-1

References

Synthesis Reference

Hartman, J., et al. (2006). Variant form of urate oxidase and use thereof (U.S. Patent No. 8,293,228 B2). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/30/f1/72/f63e5683fed87b/US8293228.pdf

General References

1. Sattui SE, Gaffo AL: Treatment of hyperuricemia in gout: current therapeutic options, latest developments and clinical implications. Ther Adv Musculoskelet Dis. 2016 Aug;8(4):145-59. doi: 10.1177/1759720X16646703. Epub 2016 May 2. [Article]
2. Sundy JS, Ganson NJ, Kelly SJ, Scarlett EL, Rehrig CD, Huang W, Hershfield MS: Pharmacokinetics and pharmacodynamics of intravenous PEGylated recombinant mammalian urate oxidase in patients with refractory gout. Arthritis Rheum. 2007 Mar;56(3):1021-8. doi: 10.1002/art.22403. [Article]
3. Yue CS, Huang W, Alton M, Maroli AN, Waltrip RW, Wright D, Marco MD: Population pharmacokinetic and pharmacodynamic analysis of pegloticase in subjects with hyperuricemia and treatment-failure gout. J Clin Pharmacol. 2008 Jun;48(6):708-18. doi: 10.1177/0091270008317589. Epub 2008 Apr 16. [Article]
4. Shannon JA, Cole SW: Pegloticase: a novel agent for treatment-refractory gout. Ann Pharmacother. 2012 Mar;46(3):368-76. doi: 10.1345/aph.1Q593. Epub 2012 Mar 6. [Article]
5. FDA Approved Drug Products: KRYSTEXXA (pegloticase) injection for intravenous use [Link]
6. EMA Summary of Product Characteristics: KRYSTEXXA (pegloticase) injection for intravenous use [Link]

External Links

KEGG Drug

D09316

PubChem Substance

347910417

RxNav

1011650

ChEMBL

CHEMBL1237025

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

Wikipedia

Pegloticase

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Uncontrolled Gout	1
4	Completed	Treatment	Gouty Arthritis	2
4	Completed	Treatment	Kidney Transplantation / Uncontrolled Gout	1
4	Recruiting	Treatment	Chronic Uncontrolled Gout / Gouty Arthritis / Uncontrolled Gout	1
4	Recruiting	Treatment	Gout Chronic / Uncontrolled Gout	1
4	Recruiting	Treatment	Hematopoietic and Lymphoid System Neoplasm / Malignant Solid Neoplasms / Tumour lysis syndrome	1
3	Completed	Treatment	Chronic Gout Refractory to Conventional Therapy	1
3	Completed	Treatment	Gouty Arthritis	2
2	Completed	Other	Gouty Arthritis	1
2	Completed	Treatment	Gout Chronic	2

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, solution	Intravenous	8 mg/1mL
Injection, solution, concentrate	Intravenous	8 MG/ML

Prices

Not Available

Patents

Not Available

Properties

State

Solid

Experimental Properties

Not Available

Targets

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Details1. Uric acid

Kind

Small molecule

Organism

Humans

Pharmacological action

Yes

Actions

Substrate

Metabolizer

References

1. FDA Approved Drug Products: KRYSTEXXA (pegloticase) injection for intravenous use [Link]

×

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Drug created at October 20, 2015 19:34 / Updated at September 05, 2022 12:50