Glucarpidase — Drug Monograph

Brand names: Voraxaze

Drug class: Supportive Care Agent

Mechanism of Action

Recombinant bacterial carboxypeptidase G2 enzyme that cleaves the C-terminal glutamate residue from methotrexate, converting it into inactive DAMPA (4-deoxy-4-amino-N10-methylpteroic acid) and glutamate. This provides a rapid, non-renal pathway for clearing toxic extracellular methotrexate from plasma when renal excretion has failed.

FDA Indications

• Treatment of toxic plasma methotrexate concentrations (>1 micromol/L) in patients with delayed methotrexate clearance due to impaired renal function

Common Side Effects

• Paresthesia
• Flushing
• Nausea
• Headache

Clinical Pearl

Recombinant carboxypeptidase G2 that hydrolyzes toxic extracellular methotrexate into inactive metabolites (DAMPA and glutamate) during acute renal failure or delayed clearance. CRITICAL TIMING: give as soon as toxic MTX levels with renal impairment are recognized (ideally within 48–60 hours of MTX initiation) to prevent irreversible end-organ toxicity. DO NOT give leucovorin within 2 hours before or after glucarpidase, as leucovorin is a substrate for the enzyme. After administration,…

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