| Primary information |
|---|
| ID | 1845 |
| ThPP ID | Th1233 |
| Therapeutic Peptide/Protein Name | Pegloticase |
| Sequence | TYKKNDEVEFVRTGYGKDMIKVLHIQRDGKYHSIKEVATTVQLTLSSKKD view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 34192.8533 |
| Chemical Formula | C1549H2430N408O448S8 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting Point (℃) | NA |
| Half Life | Median: ~14 days |
| 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. |
| Indication/Disease | For the treatment of chronic gout in adult patients refractory to conventional therapy. |
| Pharmacodynamics | NA |
| Mechanism of Action | Pegloticase is a recombinant uricase that catalyzes the metabolism of uric acid to allantoin. |
| 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. |
| Metabolism | NA |
| 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 | NA |
| Clearance | NA |
| Categories | Enzymes |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | The risk or severity of adverse effects can be increased while combining Pegloticase with Allopurinol, Certolizumab pegol, Febuxostat, Pegademase bovine, Pegaptanib, Pegaspargase, Pegfilgrastim, Peginterferon alfa-2a, Peginterferon alfa-2b, Pegvisomant etc |
| Target | Uric acid |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Pegloticase (Krystexxa) |
| Company | NA |
| Brand Discription | Pegloticase is a uric acid-specific enzyme (uricase). It works by allowing uric acid to be more easily removed from the body by the kidneys. |
| Prescribed for | Treating chronic gout in certain patients |
| Chemical Name | NA |
| Formulation | NA |
| Physcial Appearance | Solid |
| Route of Administration | Intravenous |
| Recommended Dosage | Gout: IV: 8 mg every 2 weeks |
| Contraindication | Hypersensitivity to the active substance |
| Side Effects | Chest pain or discomfort, cough, difficult or labored breathing, difficulty with swallowing, dizziness, facial swelling, fast heartbeat, fever or chills, flushing or redness of the skin, gout flare, headache, hives or welts, itching, or skin rash, nausea or vomiting, puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue, redness of the skin, tightness in the chest, unusual tiredness or weakness, unusually warm skin |
| Useful Link | http://www.rxlist.com/krystexxa-drug.htm , https://www.drugs.com/cdi/pegloticase.html , https://en.wikipedia.org/wiki/Pegloticase |
| PubMed ID | 27493693 |
| 3-D Structure | N.A. |