Pegloticase
| Clinical data | |
|---|---|
| Trade names | Krystexxa |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a611015 |
| Licence data | US FDA:link |
| Pregnancy cat. | C (US) |
| Legal status | ℞-only (US) |
| Routes | Intravenous |
| Pharmacokinetic data | |
| Bioavailability | N/A |
| Half-life | 10–12 days |
| Identifiers | |
| CAS number | 885051-90-1  |
| ATC code | M04AX02 |
| UNII | R581OT55EA  |
| KEGG | D09316 |
| ChEMBL | CHEMBL1237025 |
| Chemical data | |
| Formula | C1549H2430N408O448S8 (peptide monomer) |
| Mol. mass | 497 kDa (polymer-modified tetramer) |
| (what is this?) (verify) | |
Pegloticase (trade name Krystexxa, formerly Puricase)[1] is a drug for the treatment of severe, treatment-refractory, chronic gout, developed by Savient Pharmaceuticals.[2][3] In September 2010, the FDA approved pegloticase for marketing in the United States after two clinical trials demonstrated the drug lowered uric acid levels and reduced deposits of uric acid crystals in joints and soft tissue. The European Medicines Agency (EMA) granted marketing authorization in January 2013 for treatment of disabling tophaceous gout. Pegloticase is the first and only drug approved for this indication.
The drug is administered intravenously.
Mechanism of action
Pegloticase is a recombinant porcine-like uricase. Similarly to rasburicase, it metabolises uric acid to allantoin. This reduces the risk of precipitates, 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.[4]
Side effects
Pegloticase may show immunogenicity.[5]
Chemistry
Pegloticase is a tetrameric peptide composed of four identical chains of about 300 amino acids each. Approximately nine of the 30 lysine residues in each chain are pegylated. These side chains consist of about 225 ethylene glycol units each.[2]
See also
References
- ↑ Savient to Present Multiple Abstracts At the European League Against Rheumatism (EULAR) 2009 Annual Congress
- ↑ 2.0 2.1 Statement on a nonproprietary name adopted by the USAN Council
- ↑ Savient Pharmaceuticals: Uricase
- ↑ Biggers, K; Scheinfeldt, N (2008). Current Opinion in Investigational Drugs 9 (4): 422–429.
- ↑ Abraham J. Domb, Neeraj Kumar (2 August 2011). Biodegradable Polymers in Clinical Use and Clinical Development. John Wiley & Sons.
External links
- Krystexxa (pegloticase) Injection, for intravenous infusion: Full prescribing information
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