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    Glucarpidase

    ACTIVE PHARMA INGREDIENTS

    DEVELOPMENTS

    FINISHED DOSAGE FORMULATIONS

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    2D Structure
    Also known as: 9074-87-7, Q5572303
    Molecular Formula
    Zn4+8
    Molecular Weight
    261.5  g/mol
    InChI Key
    LZQXMCNBQHANEY-UHFFFAOYSA-N
    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.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    zinc(2+)
    2.1.2 InChI
    InChI=1S/4Zn/q4*+2
    2.1.3 InChI Key
    LZQXMCNBQHANEY-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    [Zn+2].[Zn+2].[Zn+2].[Zn+2]
    2.2 Synonyms
    2.2.1 MeSH Synonyms

    1. Voraxaze

    2.2.2 Depositor-Supplied Synonyms

    1. 9074-87-7

    2. Q5572303

    2.3 Create Date
    2007-12-05
    3 Chemical and Physical Properties
    Molecular Weight 261.5 g/mol
    Molecular Formula Zn4+8
    Hydrogen Bond Donor Count0
    Hydrogen Bond Acceptor Count0
    Rotatable Bond Count0
    Exact Mass261.70916 g/mol
    Monoisotopic Mass255.71657 g/mol
    Topological Polar Surface Area0 Ų
    Heavy Atom Count4
    Formal Charge8
    Complexity0
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count4
    4 Drug and Medication Information
    4.1 Drug Indication

    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.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Glucarpidase acts as an antidote to toxic methotrexate levels by elminating methotrexate by a non-kidney route.

    5.2 FDA Pharmacological Classification
    5.2.1 Pharmacological Classes
    Carboxypeptidases [CS]; Carboxypeptidase [EPC]
    5.3 ATC Code

    V03AF09

    V - Various

    V03 - All other therapeutic products

    V03A - All other therapeutic products

    V03AF - Detoxifying agents for antineoplastic treatment

    V03AF09 - Glucarpidase

    5.4 Absorption, Distribution and Excretion

    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.

    5.5 Metabolism/Metabolites

    Metabolism was not determined.

    5.6 Biological 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.

    5.7 Mechanism of Action

    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).