In this article, we will discuss Glucarpidase (Mechanism of Action). So, let’s get started.
Mechanism of Action
Glucarpidase is a recombinant bacterial enzyme that hydrolyzes the carboxyl-terminal glutamate residue from folic acid and classical antifolates such as methotrexate. Glucarpidase converts methotrexate to its inactive metabolites 4-deoxy-4-amino-N10-methylpteroic acid (DAMPA) and glutamate. Glucarpidase provides an alternate non-renal pathway for methotrexate elimination in patients with renal dysfunction during high-dose methotrexate treatment.
Plasma methotrexate concentrations within 48 hours following administration of Glucarpidase can only be reliably measured by a chromatographic method because DAMPA interferes with the immunoassays. Following administration of Glucarpidase 50 Units/kg to patients in Study 1, methotrexate concentration measured by a chromatographic method was reduced by ≥ 97% within 15 minutes in all 22 treatment-evaluable patients, and was maintained at a > 95% reduction up to 8 days in 20 of the 22 patients.