Glucarpidase inactivates methotrexate, and other antifolates, by hydrolyzing glutamate on the carboxyl terminal of these compounds. For methotrexate specifically, it is hydrolyzed to the inactive metabolites glutamate and 4-deoxy-4-amino-N10-methylpteroic acid (DAMPA).
Glucarpidase acts as an antidote to toxic methotrexate levels by elminating methotrexate by a non-kidney route.
Metabolism was not determined.
Most common adverse reactions include hypotension, flushing, nausea, vomiting, headache, and paresthesia.