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Identification
NameAsparaginase
Accession NumberDB00023  (BTD00011, BIOD00011)
TypeBiotech
GroupsApproved
DescriptionL-asparagine amidohydrolase from E. coli
Protein structureDb00023
Related Articles
Protein chemical formulaC1377H2208N382O442S17
Protein average weight31731.9 Da
Sequences
> Elspar Sequence
QMSLQQELRYIEALSAIVETGQKMLEAGESALDVVTEAVRLLEECPLFNAGIGAVFTRDE
THELDACVMDGNTLKAGAVAGVSHLRNPVLAARLVMEQSPHVMMIGEGAENFAFARGMER
VSPEIFSTSLRYEQLLAARKEGATVLDHSGAPLDEKQKMGTVGAVALDLDGNLAAATSTG
GMTNKLPGRVGDSPLVGAGCYANNASVAVSCTGTGEVFIRALAAYDIAALMDYGGLSLAE
ACERVVMEKLPTLGGSGGLIAIDHEGNVALPFNTEGMYRAWGYAGDTPTTGIYREKGDTV
ATQ
>sp|P00805|ASPG2_ECOLI L-asparaginase 2 OS=Escherichia coli (strain K12) GN=ansB PE=1 SV=2
MEFFKKTALAALVMGFSGAALALPNITILATGGTIAGGGDSATKSNYTVGKVGVENLVNA
VPQLKDIANVKGEQVVNIGSQDMNDNVWLTLAKKINTDCDKTDGFVITHGTDTMEETAYF
LDLTVKCDKPVVMVGAMRPSTSMSADGPFNLYNAVVTAADKASANRGVLVVMNDTVLDGR
DVTKTNTTDVATFKSVNYGPLGYIHNGKIDYQRTPARKHTSDTPFDVSKLNELPKVGIVY
NYANASDLPAKALVDAGYDGIVSAGVGNGNLYKSVFDTLATAAKTGTAVVRSSRVPTGAT
TQDAEVDDAKYGFVASGTLNPQKARVLLQLALTQTKDPQQIQQIFNQY
Download FASTA Format
Synonyms
Asparaginase (E. coli)
L-asparagine amidohydrolase
Putative L-asparaginase precursor
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ErwinasePowder, for solution10000 unitIntramuscular; Intravenous; SubcutaneousJazz Pharmaceuticals France Sas2009-07-01Not applicableCanada
KidrolasePowder, for solution10000 unitIntramuscular; IntravenousJazz Pharmaceuticals France Sas1974-12-31Not applicableCanada
SpectrilaInjection, powder, for solution10000 UIntravenousMedac Gesellschaft Fuer Klinische Spezialpraeparate Mb H2016-01-14Not applicableEu
SpectrilaInjection, powder, for solution10000 UIntravenousMedac Gesellschaft Fuer Klinische Spezialpraeparate Mb H2016-01-14Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ElsparMerck & Co. Inc
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIG4FQ3CKY5R
CAS number9015-68-3
Pharmacology
IndicationFor treatment of acute lympocytic leukemia and non-Hodgkins lymphoma
Structured Indications
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. 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 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
L-asparagineSmall moleculeyes
other/unknown
Humannot applicabledetails
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life8-30 hrs
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Asparaginase.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Asparaginase.Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of Asparaginase.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Asparaginase.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Asparaginase.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Asparaginase.Approved
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Asparaginase.Approved, Investigational, Vet Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Asparaginase.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Asparaginase.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Asparaginase.Approved, Investigational
OuabainOuabain may decrease the cardiotoxic activities of Asparaginase.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Asparaginase.Approved, Vet Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Asparaginase.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Masao Nambu, “Process for producing immobilized L-asparaginase preparations for the therapy of leukemia.” U.S. Patent US4617271, issued January, 1977.

US4617271
General References
  1. Appel IM, van Kessel-Bakvis C, Stigter R, Pieters R: Influence of two different regimens of concomitant treatment with asparaginase and dexamethasone on hemostasis in childhood acute lymphoblastic leukemia. Leukemia. 2007 Nov;21(11):2377-80. Epub 2007 Jun 7. [PubMed:17554375 ]
  2. Link [Link]
External Links
ATC CodesL01XX02
AHFS Codes
  • 10:00.00
PDB Entries
FDA labelDownload (880 KB)
MSDSNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionIntramuscular; Intravenous; Subcutaneous10000 unit
Powder, for solutionIntramuscular; Intravenous10000 unit
Injection, powder, for solutionIntravenous10000 U
Prices
Unit descriptionCostUnit
Elspar 10000 unit vial74.6USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
hydrophobicity0.059Not Available
isoelectric point4.67Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

1. L-asparagine
Kind
Small molecule
Organism
Human
Pharmacological action
yes
Actions
other/unknown
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Wetzler M, Sanford BL, Kurtzberg J, DeOliveira D, Frankel SR, Powell BL, Kolitz JE, Bloomfield CD, Larson RA: Effective asparagine depletion with pegylated asparaginase results in improved outcomes in adult acute lymphoblastic leukemia: Cancer and Leukemia Group B Study 9511. Blood. 2007 May 15;109(10):4164-7. Epub 2007 Jan 30. [PubMed:17264295 ]
  4. Wenner KA, Vieira Pinheiro JP, Escherich G, Wessalowski R, Jorch N, Wolff J, Stehn M, Kohlschutter A, Boos J, Janka-Schaub GE: Asparagine concentration in plasma after 2,500 IU/m(2) PEG-asparaginase i.v. in children with acute lymphoblastic leukemia. Klin Padiatr. 2005 Nov-Dec;217(6):321-6. [PubMed:16307417 ]
  5. Appel IM, Pinheiro JP, den Boer ML, Lanvers C, Reniers NC, Boos J, Pieters R: Lack of asparagine depletion in the cerebrospinal fluid after one intravenous dose of PEG-asparaginase: a window study at initial diagnosis of childhood ALL. Leukemia. 2003 Nov;17(11):2254-6. [PubMed:14523472 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23