==== 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.====

Detailed description page of THPdb

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1142 details
Primary information
ThPP IDTh1020
Therapeutic Peptide/Protein NameAsparaginase
SequenceElspar Sequence: QMSLQQELRYIEALSAIVETGQKMLEAGESALD view full sequnce in fasta
Functional ClassificationIc
Molecular Weight31731.9
Chemical FormulaC1377H2208N382O442S17
Isoelectric Point4.67
Hydrophobicity0.059
Melting Point (℃)N.A.
Half Life8-30 hours
DescriptionL-asparagine amidohydrolase from E. coli
Indication/DiseaseTo treat acute lympocytic leukemia and non-Hodgkins lymphoma
PharmacodynamicsIn most 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. Elspar exploits a metabolic defect in asparagine synthesis of some malignant cells.
Mechanism of ActionAsparaginase converts asparagine to aspartic acid and ammonia. It facilitates production of oxalo-acetate which is needed for general cellular metabolism. Some malignant cells lose the ability to produce asparagine and thus 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 NameElspar
CompanyMerck & Co. Inc
Brand DiscriptionElspar contains the enzyme L-asparagine amidohydrolase, type EC-2, derived from Escherichia coli. Elspar activity is expressed in terms of International Units according to the recommendation of the International Union of Biochemistry. One International Un
Prescribed forTo treat acute lymphocytic leukemia. It is used along with other cancer medicines. Elspar is an antineoplastic agent that works by decreasing the amount of asparagine in the body, which kills certain leukemia cells
Chemical NameN.A.
FormulationEach vial contains 10,000 International Units of asparaginase and 80 mg of mannitol.
Physcial AppearnceLyophilized plug or powder
Route of AdministrationIntravenous or intramuSubcutaneousular. Intravenou
Recommended DosageThe recommended dose of Elspar is 6,000 International Units/m_ intramuscularly (IM) or intravenously (IV) three times a week.
ContraindicationAllergic
Side EffectsFever, chills (see flu like symptoms), Nausea and vomiting, Allergic reaction, (sudden onset of wheezing, itching, rash, face swelling, agitation, low blood pressure). You will be monitored closely for this reaction, Poor appetite, Stomach cramping
Useful Linkhttp://www.rxlist.com/elspar-drug.htm
PubMed ID17554375, 14499708, 25098829, 24436152, 23794007, 22499236, 20824725
3-D StructureTh1020 (View) or (Download)