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Th1233 details
Primary information
ID10873
Therapeutic IDTh1233
Protein NamePegloticase
Sequence>Th1233_Pegloticase TYKKNDEVEFVRTGYGKDMIKVLHIQRDGKYHSIKEVATTVQLTLSSKKDYLHGDNSDVIPTDTIKNTVNVLAKFKGIKSIETFAVTICEHFLSSFKHVIRAQVYVEEVPWKRFEKNGVKHVHAFIYTPTGTHFCEVEQIRNGPPVIHSGIKDLKVLKTTQSGFEGFIKDQFTTLPEVKDRCFATQVYCKWRYHQGRDVDFEATWDTVRSIVLQKFAGPYDKGEYSPSVQKTLYDIQVLTLGQVPEIEDMEISLPNIHYLNIDMSKMGLINKEEVLLPLDNPYGKITGTVKRKLSSRL
Molecular Weight34192.85
Chemical FormulaC1549H2430N408O448S8
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeMedian: ~14 days
DescriptionPegloticase 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/DiseaseFor the treatment of chronic gout in adult patients refractory to conventional therapy.
PharmacodynamicsNA
Mechanism of ActionPegloticase is a recombinant uricase that catalyzes the metabolism of uric acid to allantoin.
ToxicityConditions 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.
MetabolismNA
AbsorptionApproximately 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.
NA
ClearanceNA
CategoriesEnzymes
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionThe 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
TargetUric acid
Brand NamePegloticase (Krystexxa)
CompanyNA
Brand DescriptionNA
Prescribed ForTreating chronic gout in certain patients
Chemical NameNA
FormulationNA
Physical Appearance Solid
Route of AdministrationIntravenous
Recommended DosageGout: IV: 8 mg every 2 weeks
ContraindicationHypersensitivity to the active substance
Side EffectsChest 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 1Link
Useful Link 2NA
RemarksNA