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Anticancer Drugs Glucarpidase Medicine Oncology Pharmacology Physiotherapy

Glucarpidase (Mechanism of Action)

In this article we will discuss Glucarpidase (Mechanism of Action)

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.

Pharmacodynamics

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.

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