Pegloticase - Drugbank

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8/14/2018 Pegloticase - DrugBank

Pegloticase

Targets (1) Biointeractions (1)

IDENTIFICATION

Name Pegloticase

Accession Number DB09208

Type Biotech

Groups Approved, Investigational

Biologic Classiﬁcation Protein Based Therapies Recombinant Enzymes

Description Pegloticase is a recombinant procine-like uricase drug indicated for the treatment of severe, treatment-refractory, chronic gout. Similarly to rasburicase, pegloticase metabolises the conversion of uric acid to allantoin. This reduces the risk of precipitate formation and development of gout, since allantoin is ﬁve to ten times more soluble than uric acid. In contrast to rasburicase, pegloticase is pegylated to increase its elimination half-life from about eight hours to ten or twelve days, and to decrease the immunogenicity of the foreign uricase protein. This modiﬁcation allows for an application just once every two to four weeks, making this drug suitable for long-term treatment.

Protein chemical formula

C1549H2430N408O448S8

Protein average weight 34192.8533 Da

Sequences

> Pegloticase TYKKNDEVEFVRTGYGKDMIKVLHIQRDGKYHSIKEVATTVQLTLSSKKDYLHGDNSDVI PTDTIKNTVNVLAKFKGIKSIETFAVTICEHFLSSFKHVIRAQVYVEEVPWKRFEKNGVK HVHAFIYTPTGTHFCEVEQIRNGPPVIHSGIKDLKVLKTTQSGFEGFIKDQFTTLPEVKD RCFATQVYCKWRYHQGRDVDFEATWDTVRSIVLQKFAGPYDKGEYSPSVQKTLYDIQVLT LGQVPEIEDMEISLPNIHYLNIDMSKMGLINKEEVLLPLDNPYGKITGTVKRKLSSRL

https://www.drugbank.ca/drugs/DB09208 1/9 8/14/2018 Pegloticase - DrugBank

Download FASTA Format

Synonyms

Puricase

Prescription Products

MARKETING MARKETING NAME ↑↓ DOSAGE ↑↓ STRENGTH ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓

Krystexxa Injection, 8 mg/mL Intravenous Savient 2010-09-14 Not applicable solution Pharmaceuticals

Krystexxa Injection, 8 mg/mL Intravenous Horizon Pharma, 2010-09-14 Not applicable solution Inc.

Showing 1 to 3 of 3 entries ‹ ›

Unapproved/Other Products

MARKETING MARKETING NAME ↑↓ INGREDIENTS DOSAGE ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓

Krystexxa Pegloticase (8 Injection, Intravenous Crealta 2013-01-08 2016-07-22 mg/ml) solution, Pharmaceuticals concentrate Llc

Showing 1 to 1 of 1 entries ‹ ›

Categories

Alcohols

Antigout Preparations

Biomedical and Dental Materials

Enzymes

Enzymes and Coenzymes

Enzymes, Immobilized

Ethylene Glycols

Glycols

Macromolecular Substances

Musculo-Skeletal System

Oxidoreductases

Polymers

Uric Acid-speciﬁc Enzyme https://www.drugbank.ca/drugs/DB09208 2/9 8/14/2018 Pegloticase - DrugBank

UNII R581OT55EA

CAS number 885051-90-1

PHARMACOLOGY

Indication For the treatment of chronic gout in adult patients refractory to conventional therapy.

Associated Conditions

Chronic, refractory Gout

Pharmacodynamics Not Available

Mechanism of action Pegloticase is a recombinant uricase that catalyzes the metabolism of uric acid to allantoin.

A Uric acid

metabolizer

Human

Absorption Approximately 24 hours following the ﬁrst dose, mean plasma uric acid levels were 0.7 mg/dL. The duration of suppression of plasma uric acid appeared to be positively associated with pegloticase dose. Sustained decrease in plasma uric acid below the solubility concentration of 6 mg/dL for more than 300 hours was observed with doses of 8 mg and 12 mg.

Volume of distribution Not Available

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Not Available

Half life

Not Available

Clearance

Not Available https://www.drugbank.ca/drugs/DB09208 3/9 8/14/2018 Pegloticase - DrugBank Toxicity Conditions that should be monitored for when starting treatment with pegloticase include anaphylaxis, infusion reactions, an increase in gout ﬂares, and/or an exacerbation of pre-existing congestive heart failure.

Aﬀected organisms Not Available

Pathways Not Available

Pharmacogenomic Eﬀects/ADRs

INTERACTING ALLELE GENE/ENZYME ↑↓ NAME ↑↓ GENOTYPE(S) ↑↓ DEFINING CHANGE(S) ↑↓ TYPE(S) DESCRIPTION ↑↓ DETAILS

Glucose-6- Villeurbanne Not Available 1000_1002delACC ADR Increased risk of Details phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

Glucose-6- Torun Not Available 1006A->G ADR Increased risk of Details phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

Glucose-6- Sunderland Not Available 105_107delCAT ADR Increased risk of Details phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

Glucose-6- Iwatsuki Not Available 1081G->A ADR Increased risk of Details phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

Glucose-6- Serres Not Available 1082C->T ADR Increased risk of Details phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

Glucose-6- Tondela Not Available 1084_1101delCTGAACGAGCGCAAGGCC ADR Increased risk of Details phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

Glucose-6- Loma Linda Not Available 1089C->A ADR Increased risk of Details phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

https://www.drugbank.ca/drugs/DB09208 4/9 8/14/2018 Pegloticase - DrugBank

INTERACTING ALLELE Glucose-6- Aachen Not Available 1089C->G ADR Increased risk of Details GENE/ENZYME ↑↓ NAME ↑↓ GENOTYPE(S) ↑↓ DEFINING CHANGE(S) ↑↓ TYPE(S) DESCRIPTION ↑↓ DETAILS phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

Glucose-6- Tenri Not Available 1096A->G ADR Increased risk of Details phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

Glucose-6- Montpellier Not Available 1132G>A ADR Increased risk of Details phosphate 1- Inferred potentially fatal dehydrogenase hemolytic anemia and methemoglobinemia.

Showing 1 to 10 of 171 entries ‹ ›

INTERACTIONS

Drug Interactions

DRUG ↑↓ INTERACTION ↑↓ DRUG GROUP ↑↓ Allopurinol The risk or severity of adverse eﬀects can be increased when Allopurinol is combined Approved with Pegloticase.

Certolizumab The therapeutic eﬃcacy of Certolizumab pegol can be decreased when used in Approved pegol combination with Pegloticase.

Febuxostat The risk or severity of adverse eﬀects can be increased when Febuxostat is combined Approved with Pegloticase.

Pegademase The therapeutic eﬃcacy of Pegademase bovine can be decreased when used in Approved bovine combination with Pegloticase.

Pegaptanib The therapeutic eﬃcacy of Pegaptanib can be decreased when used in combination Approved, with Pegloticase. Investigational

Pegaspargase The therapeutic eﬃcacy of Pegaspargase can be decreased when used in combination Approved, with Pegloticase. Investigational

Pegfilgrastim The therapeutic efficacy of Pegfilgrastim can be decreased when used in combination Approved with Pegloticase.

Peginterferon alfa- The therapeutic eﬃcacy of Peginterferon alfa-2a can be decreased when used in Approved, 2a combination with Pegloticase. Investigational

Peginterferon alfa- The therapeutic eﬃcacy of Peginterferon alfa-2b can be decreased when used in Approved 2b combination with Pegloticase.

Pegvisomant The therapeutic eﬃcacy of Pegvisomant can be decreased when used in combination Approved with Pegloticase.

Showing 1 to 10 of 11 entries ‹ ›

Food Interactions

Not Available

https://www.drugbank.ca/drugs/DB09208 5/9 8/14/2018 Pegloticase - DrugBank

REFERENCES

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. [PubMed:27493693]

External Links KEGG Drug D09316

PubChem Substance 347910417

ChEMBL CHEMBL1237025

RxList RxList Drug Page

Drugs.com Drugs.com Drug Page

Wikipedia Pegloticase

ATC Codes M04AX02 — Pegloticase M04AX — Other antigout preparations M04A — ANTIGOUT PREPARATIONS M04 — ANTIGOUT PREPARATIONS M — MUSCULO-SKELETAL SYSTEM

FDA label Download (373 KB)

CLINICAL TRIALS

Clinical Trials

PHASE ↑↓ STATUS ↑↓ PURPOSE ↑↓ CONDITIONS ↑↓ COUNT ↑↓ 1 Completed Not Available Hemodialysis-dependent chronic kidney disease 1

2 Completed Treatment Acute Gouty Arthritis 2

2 Recruiting Other Acute Gouty Arthritis 1

2 Recruiting Treatment Gout Chronic 1

3 Completed Treatment Acute Gouty Arthritis 2

3 Completed Treatment Chronic Gout Refractory to Conventional Therapy 1

Not Available Completed Not Available Gout Chronic 1

Showing 1 to 7 of 7 entries https://www.drugbank.ca/drugs/DB09208 6/9 8/14/2018 Pegloticase - DrugBank

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PHARMACOECONOMICS

Manufacturers

Not Available

Packagers

Not Available

Dosage forms

FORM ↑↓ ROUTE ↑↓ STRENGTH ↑↓ Injection, solution Intravenous 8 mg/mL

Injection, solution, concentrate Intravenous 8 mg/ml

Showing 1 to 2 of 2 entries ‹ ›

Prices Not Available

Patents Not Available

PROPERTIES

State Solid

Experimental Properties Not Available

TAXONOMY

Description

Not Available

Kingdom

Organic Compounds

Super Class

Organic Acids

Class

Carboxylic Acids and Derivatives

Sub Class https://www.drugbank.ca/drugs/DB09208 7/9 8/14/2018 Pegloticase - DrugBank

Amino Acids, Peptides, and Analogues

Direct Parent Peptides

Alternative Parents Not Available

Substituents Not Available

Molecular Framework Not Available

External Descriptors Not Available

TARGETS

1. Uric acid

Kind Small molecule Organism Human Pharmacological action Yes

Actions Metabolizer

Drug created on October 20, 2015 13:34 / Updated on August 02, 2018 06:15

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https://www.drugbank.ca/drugs/DB09208 8/9 8/14/2018 Pegloticase - DrugBank Commercial Products API Pricing API Docs Data Licenses Support

This project is supported by the Canadian Institutes of Health Research (award #111062), Alberta Innovates - Health Solutions, and by The Metabolomics Innovation Centre (TMIC), a nationally-funded research and core facility that supports a wide range of cutting-edge metabolomic studies. TMIC is funded by Genome Alberta, Genome British Columbia, and Genome Canada, a not-for-proﬁt organization that is leading Canada's national genomics strategy with funding from the federal government. Maintenance, support, and commercial licensing is provided by OMx Personal Health Analytics, Inc. Designed by Educe Design & Innovation Inc.

https://www.drugbank.ca/drugs/DB09208 9/9