Glucarpidase
Glucarpidase Uses, Dosage, Side Effects, Food Interaction and all others data.
Glucarpidase is the recombinant form of the Pseudomonas sp. (strain RS-16) enzyme carboxypeptidase G2 that is produced in Escherichia coli. In patients, glucarpidase inactivates methotrexate, and other antifolates, by hydrolyzing glutamate on the carboxyl terminal of these compounds. Therefore since methotrexate is eliminated enzymatically and not by the kidneys, glucarpidase is indicated in patients on methotrexate treatment who have kidney dysfunction, and are experiencing an abnormally high plasma concentration of methotrexate (>1 micromole per liter). Glucarpidase is marketed under the brand name Voraxaze®.
Glucarpidase acts as an antidote to toxic methotrexate levels by elminating methotrexate by a non-kidney route.
| Trade Name | Glucarpidase |
| Availability | Prescription only |
| Generic | Glucarpidase |
| Glucarpidase Other Names | Carboxypeptidase G2, Folate hydrolase G2, Glucarpidase, Glutamate carboxypeptidase |
| Related Drugs | leucovorin, Voraxaze, levoleucovorin, Khapzory |
| Weight | 1000units, |
| Type | Intravenous Powder For Injection, Intravenous |
| Formula | C1950H3157N543O599S7 |
| Weight | 44016.6653 Da |
| Protein binding | Plasma protein binding was not quantified. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Glucarpidase is a carboxypeptidase enzyme used to treat toxic plasma methotrexate concentrations by providing an alternate elimination pathway for methotrexate in patients who have impaired renal function.
Used in patients on methotrexate treatment who have kidney dysfunction, and are experiencing an abnormally high plasma concentration of methotrexate (> 1 micromole per liter).
Glucarpidase is also used to associated treatment for these conditions: >1 micromole per liter toxic plasma methotrexate concentrations
How Glucarpidase works
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).
Toxicity
Most common adverse reactions include hypotension, flushing, nausea, vomiting, headache, and paresthesia.
Food Interaction
- Take with or without food.
Volume of Distribution
Glucarpidase is likely limited to the plasma volume since its volume of distribution is 3.6 L.
Elimination Route
In healthy patients not taking methotrexate, the average maximum concentration for glucarpidase was 3.3 μg/mL.
Half Life
In healthy patients not taking methotrexate, glucarpidase has an elimination half-life of 5.6 hours. In patients with severe renal impairment (creatinine clearance <30 mL/min), glucarpidase has an longer elimination half-life at 8.2 hours.
Clearance
In healthy patients not taking methotrexate, glucarpidase has a clearance of 7.5 mL/min.
Elimination Route
Route of elmination was not determined.
Innovators Monograph
You find simplified version here Glucarpidase
