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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 IDs Not Available
Product Ingredients 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
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
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Asparaginase.Approved
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
OleandrinAnvirzel may decrease the cardiotoxic activities of Asparaginase.Experimental
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
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingOtherAcute Myeloid Leukaemias (AML)1
1CompletedSupportive CareAcute Lymphoblastic Leukaemias (ALL) / Non Hodgkins Lymphoma1
1CompletedTreatmentAcute Lymphoid Leukemia Relapse / Acute Lymphoid Leukemia Relapse After Bone Marrow Transplant1
1CompletedTreatmentLeukemias1
1CompletedTreatmentLeukemias / Myelodysplastic Syndromes1
1TerminatedTreatmentAllergy to Native e.Coli Asparaginase / Allergy to PEG e.Coli Asparaginase / Relapsed Acute Lymphoblastic Leukemia1
1, 2Active Not RecruitingTreatmentRecurrent Childhood Acute Lymphoblastic Leukemia1
1, 2CompletedTreatmentAcute Undifferentiated Leukemia (AUL) / B-cell Adult Acute Lymphoblastic Leukemia / B-cell Childhood Acute Lymphoblastic Leukemia / L1 Adult Acute Lymphoblastic Leukemia / L1 Childhood Acute Lymphoblastic Leukemia / L2 Adult Acute Lymphoblastic Leukemia / L2 Childhood Acute Lymphoblastic Leukemia / Philadelphia Chromosome Negative Adult Precursor Acute Lymphoblastic Leukemia / Philadelphia Chromosome Positive Adult Precursor Acute Lymphoblastic Leukemia / Philadelphia Chromosome Positive Childhood Precursor Acute Lymphoblastic Leukemia / T-cell Adult Acute Lymphoblastic Leukemia / T-cell Childhood Acute Lymphoblastic Leukemia / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
1, 2RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
2Active Not RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
2CompletedTreatmentB-cell Adult Acute Lymphoblastic Leukemia / B-cell Childhood Acute Lymphoblastic Leukemia / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Lymphoblastic Lymphoma / Recurrent Childhood Acute Lymphoblastic Leukemia / Recurrent Childhood Lymphoblastic Lymphoma / T-cell Adult Acute Lymphoblastic Leukemia / T-cell Childhood Acute Lymphoblastic Leukemia1
2CompletedTreatmentLeukemias10
2CompletedTreatmentLeukemias / Lymphoma NOS2
2CompletedTreatmentLeukemias / Neutropenias / Thrombocytopenias1
2CompletedTreatmentLymphoma NOS1
2CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
2Not Yet RecruitingTreatmentB Acute Lymphoblastic Leukemia / B Lymphoblastic Lymphoma / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent B Lymphoblastic Lymphoma / Recurrent T Lymphoblastic Leukemia/Lymphoma / Refractory B Lymphoblastic Lymphoma / Refractory T Lymphoblastic Lymphoma / T Acute Lymphoblastic Leukemia / T Lymphoblastic Lymphoma1
2Not Yet RecruitingTreatmentMalignancies, Hematologic1
2RecruitingTreatmentLymphoma, Extranodal NK-T-Cell1
2TerminatedTreatmentAcute Lymphoid Leukemia (ALL) / Acute Myeloid Leukaemias (AML) / Mixed Lineage Acute Leukemia1
2TerminatedTreatmentLymphoma, Lymphoblastic1
2TerminatedTreatmentRecurrent Adult Acute Lymphoblastic Leukemia1
2Unknown StatusTreatmentLeukemias2
2WithdrawnTreatmentAcute Lymphoblastic Leukemia (ALL)/Lymphoblastic Lymphoma (LBL)1
2, 3CompletedTreatmentAcute Lymphoblastic Leukemia, in Relapse1
2, 3CompletedTreatmentAdult B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 / Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
2, 3Unknown StatusTreatmentLeukemias1
3Active Not RecruitingTreatmentAcute Undifferentiated Leukemia (AUL) / T-cell Childhood Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
3Active Not RecruitingTreatmentAdult T Acute Lymphoblastic Leukemia / Childhood T Acute Lymphoblastic Leukemia / Stage II Adult T-Cell Leukemia/Lymphoma / Stage II Childhood Lymphoblastic Lymphoma / Stage II Contiguous Adult Lymphoblastic Lymphoma / Stage II Non-Contiguous Adult Lymphoblastic Lymphoma / Stage III Adult Lymphoblastic Lymphoma / Stage III Adult T-Cell Leukemia/Lymphoma / Stage III Childhood Lymphoblastic Lymphoma / Stage IV Adult Lymphoblastic Lymphoma / Stage IV Adult T-Cell Leukemia/Lymphoma / Stage IV Childhood Lymphoblastic Lymphoma / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
3Active Not RecruitingTreatmentB-cell Childhood Acute Lymphoblastic Leukemia / Intermediate Risk Recurrent Childhood Acute Lymphoblastic Leukemia / L1 Childhood Acute Lymphoblastic Leukemia / L2 Childhood Acute Lymphoblastic Leukemia1
3Active Not RecruitingTreatmentChildhood Acute Basophilic Leukemia / Childhood Acute Eosinophilic Leukemia / Childhood Acute Erythroleukemia (M6) / Childhood Acute Megakaryocytic Leukemia (M7) / Childhood Acute Minimally Differentiated Myeloid Leukemia (M0) / Childhood Acute Monoblastic Leukemia (M5a) / Childhood Acute Monocytic Leukemia (M5b) / Childhood Acute Myeloblastic Leukemia With Maturation (M2) / Childhood Acute Myeloblastic Leukemia Without Maturation (M1) / Childhood Acute Myelomonocytic Leukemia (M4) / Childhood Myelodysplastic Syndromes / De Novo Myelodysplastic Syndromes / Secondary Acute Myeloid Leukemia / Secondary Myelodysplastic Syndromes / Untreated Childhood Acute Myeloid Leukemia and Other Myeloid Malignancies1
3Active Not RecruitingTreatmentDrug/Agent Toxicity by Tissue/Organ / Leukemias1
3Active Not RecruitingTreatmentLeukemias1
3Active Not RecruitingTreatmentLymphoma NOS1
3CompletedSupportive CareCardiac Toxicity / Leukemias / Lymphoma NOS1
3CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL)2
3CompletedTreatmentChildhood Acute Erythroleukemia (M6) / Childhood Acute Megakaryocytic Leukemia (M7) / Childhood Acute Monoblastic Leukemia (M5a) / Childhood Acute Monocytic Leukemia (M5b) / Childhood Acute Myeloblastic Leukemia With Maturation (M2) / Childhood Acute Myeloblastic Leukemia Without Maturation (M1) / Childhood Acute Myelomonocytic Leukemia (M4) / Childhood Myelodysplastic Syndromes / Chronic Myelomonocytic Leukemia / De Novo Myelodysplastic Syndromes / Refractory Anemia / Refractory Anemia With Excess Blasts / Refractory Anemia With Excess Blasts in Transformation / Refractory Anemia With Ringed Sideroblasts / Secondary Myelodysplastic Syndromes / Untreated Childhood Acute Myeloid Leukemia and Other Myeloid Malignancies1
3CompletedTreatmentChildhood Acute Lymphoblastic Leukemia in Remission / Recurrent Childhood Acute Lymphoblastic Leukemia1
3CompletedTreatmentLeukemias9
3CompletedTreatmentLeukemias / Lymphoma NOS1
3CompletedTreatmentLeukemias / Myelodysplastic Syndromes1
3CompletedTreatmentLeukemias / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Neoplasms1
3Not Yet RecruitingTreatmentAcute Lymphoblastic Leukemia, Pediatric1
3RecruitingTreatmentB Acute Lymphoblastic Leukemia / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia1
3RecruitingTreatmentChildhood Acute Myeloid Leukemia / Childhood Myelodysplastic Syndrome / Cytopenias / Down Syndrome (DS) / Myeloid Leukemia Associated With Down Syndrome / Myeloproliferative Neoplasms1
3RecruitingTreatmentLeukaemia cutis / Sarcoma, Myeloid / Untreated Adult Acute Myeloid Leukemia / Untreated Childhood Myeloid Neoplasm1
3TerminatedTreatmentAcute Lymphoblastic Leukaemias (ALL)1
3TerminatedTreatmentLymphoma NOS1
3Unknown StatusTreatmentLeukemias2
3Unknown StatusTreatmentLeukemias / Lymphoma NOS1
3Unknown StatusTreatmentLymphoma NOS2
3WithdrawnTreatmentLeukemias1
4CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL)1
4CompletedTreatmentAdult Acute Lymphocytic Leukemia3
4CompletedTreatmentLymphoma, Lymphoblastic1
4Unknown StatusTreatmentAdult Acute Lymphocytic Leukemia2
Not AvailableActive Not RecruitingTreatmentAdult Acute Lymphoblastic Leukemia / Childhood Acute Lymphoblastic Leukemia1
Not AvailableActive Not RecruitingTreatmentLeukemias1
Not AvailableCompletedTreatmentL1 Childhood Acute Lymphoblastic Leukemia / L2 Childhood Acute Lymphoblastic Leukemia / Non-T, Non-B Childhood Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia / T-cell Childhood Acute Lymphoblastic Leukemia1
Not AvailableCompletedTreatmentLeukemia, Lymphocytic, Acute1
Not AvailableCompletedTreatmentLeukemias1
Not AvailableCompletedTreatmentLymphoma, Lymphoblastic1
Not AvailableCompletedTreatmentT-cell Childhood Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
Not AvailableNo Longer AvailableNot AvailableAcute Lymphoblastic Leukaemias (ALL) / Acute Lymphoid Leukemia (ALL)1
Not AvailableUnknown StatusTreatmentLeukemias2
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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23