Summary of Clinical Use

Approved to treat cancer patients with impaired kidney function receiving methotrexate [1]. These patients experience elevated levels of methotrexate as kidney function impairment renders them unable to metabolise the drug to inactive products and reduce levels effectively after the drug has been given. This enzyme drug has had orphan drug designation in the EU since 2003.

Mechanism Of Action and Pharmacodynamic Effects

Glucarpidase enzymatically inactivates methotrexate by hydrolyzing methotrexate's carboxyl terminal glutamate moiety [2], generating glutamate and 2,4-diamino-N(10)-methylpteroic acid [1]. This effects the required reduction in plasma levels of methotrexate in the indicated patient group and prevents methotrexate overdose.

External links

For extended ADME data see the following: Drugs.com