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Glucarpidase (Voraxaze) is a single emergency injection that chops up methotrexate in the blood when a patient's kidneys have failed to clear a high dose, preventing potentially fatal toxicity.
Glucarpidase was approved by the FDA in January 2012 to reduce toxic plasma methotrexate concentrations (above 1 micromole per litre) in adults and children with delayed methotrexate clearance due to impaired renal function, on pooled single-arm studies in which a single 50 units/kg dose lowered methotrexate by more than 95% within 15 minutes in almost all patients. It does not replace leucovorin, which must continue (given at least two hours apart because glucarpidase also cleaves leucovorin), and it is not for patients with expected clearance. In the EU it is available through named-patient supply rather than a central authorisation. Marketed by BTG, now SERB.
Backbone ribbon from PDB 1CG2. RCSB PDB 1CG2. The ribbon widens where the chain is folded into a regular pattern and narrows where it is a loose loop.
Carboxypeptidase G2 from Pseudomonas that cleaves the terminal glutamate from methotrexate, converting it within minutes to inactive DAMPA and glutamate, independent of renal function.
1.Glucarpidase binds its target.
| Region | Year | Indication |
|---|---|---|
| US | 2012 | Toxic plasma methotrexate concentrations with delayed clearance due to impaired renal function |
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Query for this drug: (TITLE:"Glucarpidase" OR ABSTRACT:"Glucarpidase" OR TITLE:"Voraxaze" OR ABSTRACT:"Voraxaze" OR TITLE:"Carboxypeptidase G2" OR ABSTRACT:"Carboxypeptidase G2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Glucarpidase, not a curated reading list.
Shares SERB Pharmaceuticals and the tag supportive.
Shares SERB Pharmaceuticals and the tag supportive.