Drug intelligence / Profile preview

glucarpidase

Development stage
Approved
Lead developer
BTG International
Modality
Replacement Enzymes → Therapeutic Enzymes → Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

Glucarpidase is a recombinant bacterial enzyme (carboxypeptidase G2) used as an antidote to reduce toxic plasma methotrexate concentrations in patients with delayed methotrexate clearance due to impaired renal function. It is produced by genetically modified Escherichia coli and consists of a 390-amino acid homodimer protein. Glucarpidase works by hydrolyzing the carboxyl-terminal glutamate residue from folic acid and classical antifolates such as methotrexate, converting methotrexate into its inactive metabolites 4-deoxy-4-amino-N10-methylpteroic acid (DAMPA) and glutamate. This provides an alternative non-renal route for methotrexate elimination, rapidly reducing plasma levels of the drug and mitigating toxicity risks in both adult and pediatric cancer patients[1][2][3][6][8].

Brand names
Voraxaze
Other names
carboxypeptidase G2
02

Targets

DHFR (Dihydrofolate reductase)

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