Glucarpidase is a recombinant carboxypeptidase enzyme produced using recombinant DNA technology in genetically modified Escherichia coli. It is a 390-amino-acid homodimer with an approximate molecular weight of 83 kDa. Glucarpidase provides an alternative, non-renal pathway for the elimination of methotrexate by enzymatically converting methotrexate into inactive metabolites.
Glucarpidase is a specialized biological enzyme used in the management of toxic methotrexate concentrations, particularly when methotrexate elimination is delayed. It hydrolyzes the carboxyl-terminal glutamate residue from methotrexate and other classical antifolates. The resulting methotrexate metabolites include 4-deoxy-4-amino-N10-methylpteroic acid (DAMPA) and glutamate.
Glucarpidase is manufactured by recombinant DNA technology using genetically modified Escherichia coli cells. The finished medicinal product is supplied as a sterile, preservative-free, white lyophilized powder for intravenous administration.
Commercial glucarpidase injection is supplied as 1,000 Units per single-dose vial. After reconstitution with 1 mL of sterile 0.9% sodium chloride solution, the nominal concentration is 1,000 Units/mL.
Glucarpidase rapidly hydrolyzes circulating methotrexate through a non-renal elimination pathway. This enzymatic conversion reduces plasma methotrexate concentrations and is particularly relevant in patients experiencing delayed methotrexate elimination.
Glucarpidase is supplied as a white to off-white lyophilized powder. The vial is reconstituted with 1 mL of sterile 0.9% sodium chloride solution. The reconstituted solution should be clear, colorless and free from visible particulate matter.
The unopened product is stored under refrigeration at 2°C to 8°C and should not be frozen. The U.S. prescribing information specifies that reconstituted product may be stored at 2°C to 8°C for up to 4 hours if not used immediately; the UK/EU product information gives different validated in-use stability conditions, so the applicable regional product specification should be followed.
Glucarpidase medicinal product is supplied in a single-dose Type I glass vial. The commercial presentation contains 1,000 Units per vial.
Glucarpidase is used as a specialized rescue therapy to reduce toxic plasma methotrexate concentrations in patients with delayed methotrexate elimination. Its clinical use is associated with high-dose methotrexate treatment and impaired or delayed methotrexate clearance.
We offer pharmaceutical and biotechnology industry support for Glucarpidase API and recombinant biological products, including technical documentation, product specifications, quality information and supply requirements. Product availability, batch specifications, regulatory documentation and commercial terms can be discussed according to customer requirements.
Glucarpidase is a recombinant biological product and requires biological-product appropriate quality controls. Depending on the intended application and applicable regulatory requirements, documentation may include Certificate of Analysis (CoA), Certificate of Origin, technical data, batch information, storage requirements and other quality/regulatory documentation.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 5.5 – 6.5 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 2.0% |