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1. Voraxaze
1. 9074-87-7
2. Q5572303
| Molecular Weight | 261.5 g/mol |
|---|---|
| Molecular Formula | Zn4+8 |
| Hydrogen Bond Donor Count | 0 |
| Hydrogen Bond Acceptor Count | 0 |
| Rotatable Bond Count | 0 |
| Exact Mass | 261.70916 g/mol |
| Monoisotopic Mass | 255.71657 g/mol |
| Topological Polar Surface Area | 0 Ų |
| Heavy Atom Count | 4 |
| Formal Charge | 8 |
| Complexity | 0 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 4 |
Used in patients on methotrexate treatment who have kidney dysfunction, and are experiencing an abnormally high plasma concentration of methotrexate (> 1 micromole per liter).
FDA Label
Treatment of methotrexate toxicity
Voraxaze is indicated to reduce toxic plasma methotrexate concentration in adults and children (aged 28 days and older) with delayed methotrexate elimination or at risk of methotrexate toxicity.
Glucarpidase acts as an antidote to toxic methotrexate levels by elminating methotrexate by a non-kidney route.
V03AF09
V - Various
V03 - All other therapeutic products
V03A - All other therapeutic products
V03AF - Detoxifying agents for antineoplastic treatment
V03AF09 - Glucarpidase
Absorption
In healthy patients not taking methotrexate, the average maximum concentration for glucarpidase was 3.3 g/mL.
Route of Elimination
Route of elmination was not determined.
Volume of Distribution
Glucarpidase is likely limited to the plasma volume since its volume of distribution is 3.6 L.
Clearance
In healthy patients not taking methotrexate, glucarpidase has a clearance of 7.5 mL/min.
Metabolism was not determined.
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.
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).
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