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 Search 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. 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 Search 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 Search 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 Search 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 Search 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 ‹ › PHARMACOECONOMICS Manufacturers Not Available Packagers Not Available Dosage forms Search 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 About About DrugBank DrugBank Blog Wishart Research Group Terms of Use Privacy Policy