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
Glucarpidase
Glucarpidase

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

*** Taking medicines without doctor's advice can cause long-term problems.
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