==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

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1337 details
Primary information
ThPP IDTh1048
Therapeutic Peptide/Protein NamePegaspargase
SequenceMEFFKKTALAALVMGFSGAALALPNITILATGGTIAGGGDSATKSNYTVG view full sequnce in fasta
Functional ClassificationIc
Molecular Weight31731.9
Chemical FormulaC1377H2208N382O442S17
Isoelectric Point4.67
Hydrophobicity0.059
Melting Point (℃)N.A.
Half LifeN.A.
DescriptionPegylated L-asparagine amidohydrolase from E. coli. Pegylation substantially (by a factor of 4) extends the protein half life.
Indication/DiseaseFor treatment of acute lymphoblastic leukemia.
PharmacodynamicsIn a significant number of patients with acute leukemia, the malignant cells are dependent on an exogenous source of asparagine for survival. Normal cells, however, are able to synthesize asparagine and thus are affected less by the rapid depletion produced by treatment with the enzyme asparaginase. Oncaspar exploits a metabolic defect in asparagine synthesis of some malignant cells.
Mechanism of ActionPegaspargase, more effective than asparaginase, converts asparagine to aspartic acid and ammonia. It facilitates production of oxaloacetate which is needed for general cellular metabolism. Some malignant cells lose the ability to produce asparagine and so the loss of exogenous sources of asparagine leads to cell death.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesAntineoplastic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
TargetL-asparagine
Information of corresponding available drug in the market
Brand NameOncaspar
CompanyEnzon Inc
Brand DiscriptionOncaspar (pegaspargase) is L-asparaginase (L-asparagine amidohydrolase) that is covalently conjugated to monomethoxypolyethylene glycol (mPEG). L-asparaginase is a tetrameric enzyme that is produced endogenously by E. coli and consists of identical 34.5 k
Prescribed forOncaspar is indicated as a component of a multi-agent chemotherapeutic regimen for the first line treatment of patients with Acute Lymphoblastic Leukemia (ALL).
Chemical NameN.A.
FormulationOncaspar is supplied as a clear, colorless, preservative-free, isotonic sterile solution in phosphate-buffered saline, pH 7.3. Each milliliter contains 750 ± 150 International Units of pegaspargase, dibasic sodium phosphate, USP (5.58 mg), monobasic sodiu
Physcial AppearnceSolution
Route of AdministrationIntravenous or intramuSubcutaneousular administrat
Recommended DosageThe recommended dose of Oncaspar is 2,500 International Units/m_ intramuscularly or intravenously. Oncaspar should be administered no more frequently than every 14 days. When Oncaspar is administered intramuscularly, the volume at a single injection site should be limited to 2ml.
ContraindicationHistory of serious allergic reactions to Oncaspar. History of serious thrombosis with prior L-asparaginase therapy. History of pancreatitis with prior L-asparaginase therapy. History of serious hemorrhagic events with prior L-asparaginase therapy.
Side EffectsHypersensitivity reactions, coagulopathy, hyperglycemia, elevated serum transaminase concentrations, hyperbilirubinemia, pancreatitis, CNS thrombosis.No apparent difference in adverse effects following IV versus IM administration.
Useful Linkhttp://www.fda.gov/AboutFDA/CentersOffices/OfficeofMedicalProductsandTobacco/CDER/ucm095609.htm
PubMed ID14499708, 23794007
3-D StructureTh1048 (View) or (Download)