Detailed description page of ThPDB2

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10651 details
Primary information
ID10651
Therapeutic IDTh1136
Protein NameGlucarpidase
Sequence>Th1136_Glucarpidase MRPSIHRTAIAAVLATAFVAGTALAQKRDNVLFQAATDEQPAVIKTLEKLVNIETGTGDAEGIAAAGNFLEAELKNLGFTVTRSKSAGLVVGDNIVGKIKGRGGKNLLLMSHMDTVYLKGILAKAPFRVEGDKAYGPGIADDKGGNAVILHTLKLLKEYGVRDYGTITVLFNTDEEKGSFGSRDLIQEEAKLADYVLSFEPTSAGDEKLSLGTSGIAYVQVNITGKASHAGAAPELGVNALVEASDLVLRTMNIDDKAKNLRFNWTIAKAGNVSNIIPASATLNADVRYARNEDFDAAMKTLEERAQQKKLPEADVKVIVTRGRPAFNAGEGGKKLVDKAVAYYKEAGGTLGVEERTGGGTDAAYAALSGKPVIESLGLPGFGYHSDKAEYVDISAIPRRLYMARRLIMDLGAGK
Molecular Weight83000
Chemical FormulaC3670H5926N10114O1140S12
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeElimination half-life of 5.6 hours
DescriptionRecombinant (E. Coli derived) form of the Pseudomonas sp. (strain RS-16) enzyme, carboxypeptidase G2. It inactivates methotrexate and other antifolates by hydrolyzing glutamate on the carboxyl terminal of these compounds. Since methotrexate is eliminated enzymatically and not by the kidneys, glucarpidase is indicated in patients on methotrexate treatment who have kidney dysfunction, and are experiencing an abnormally high plasma concentration of methotrexate (>1 micromole per liter).
Indication/DiseaseUsed in patients on methotrexate treatment who have kidney dysfunction, and are experiencing an abnormally high plasma concentration of methotrexate (> 1 micromole per liter).
PharmacodynamicsGlucarpidase acts as an antidote to toxic methotrexate levels by elminating methotrexate by a non-kidney route.
Mechanism of ActionGlucarpidase inactivates methotrexate, and other antifolates, by hydrolyzing glutamate on the carboxyl terminal of these compounds. For methotrexate specifically, it is hydrolyzed to the inactive metabolites glutamate and 4-deoxy-4-amino-N10-methylpteroic acid (DAMPA).
ToxicityMost common adverse reactions include hypotension, flushing, nausea, vomiting, headache, and paresthesia.
MetabolismMetabolism was not determined.
AbsorptionIn healthy patients not taking methotrexate, the average maximum concentration for glucarpidase was 3.3 µg/mL.
Glucarpidase is likely limited to the plasma volume since its volume of distribution is 3.6 L.
ClearanceIn healthy patients not taking methotrexate, glucarpidase has a clearance of 7.5 mL/min.
CategoriesEnzymes
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetMethotrexate
Brand NameVoraxaze
CompanyBTG International
Brand DescriptionBTG International
Prescribed Fortoxic plasma methotrexate concentrations
Chemical NameNA
FormulationEach vial contains 1,000 Units of glucarpidase, lactose monohydrate (10 mg), Tris-HCl (0.6 mg) and zinc acetate dihydrate (0.002 mg).
Physical Appearance VORAXAZE is supplied as a Sterile, preservative-free, white lyophilized powder in single-use vials
Route of AdministrationIntravenous Injection
Recommended Dosage50 Units per kg
ContraindicationNA
Side Effectsparaesthesias, flushing, nausea and/or vomiting, hypotension, and headache
Useful Link 1Link
Useful Link 2NA
RemarksNA