Products
Glucarpidase is commercially available in the United States as an injectable (Voraxaze). The drug has not yet been approved in many countries.
Structure and properties
Glucarpidase is a carboxypeptidase biotechnologically derived from genetically modified. It is protein composed of 390 amino acids and exists as a homodimer with a molecular weight of 83 kDa. Glucarpidase was originally isolated from.
Effects
Glucarpidase (ATC V03AF09) inactivates methotrexate. It is an enzyme that cleaves the glutamate portion of the molecule, converting the drug to the inactive metabolites DAMPA (2,4-diamino-N10-methylpteroic acid) and glutamate. These are excreted mainly through the liver.
Indications
For the treatment of toxic methotrexate plasma concentrations (>1 µmol per liter) in patients with delayed methotrexate clearance due to impaired renal function.
Dosage
According to the SmPC. The drug is injected intravenously.
Contraindications
Glucarpidase is contraindicated in case of hypersensitivity. Full precautions can be found in the drug label.
Interactions
The enzyme may also inactivate structurally related folates. Leucovorin should not be administered concomitantly because it is also a substrate of glucarpidase.
Adverse effects
Possible adverse effects include hypersensitivity reactions, paresthesias, flushing, nausea, vomiting, low blood pressure, and headache.
