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Trials

Economics

Properties

Spectra

Taxonomy

Asparaginase

Targets (1)

Identification

Name

Asparaginase

Accession Number

DB00023 (BTD00011, BIOD00011)

Type

Biotech

Groups

Approved

Description

L-asparagine amidohydrolase from E. coli

Protein structure

Protein chemical formula

C₁₃₇₇H₂₂₀₈N₃₈₂O₄₄₂S₁₇

Protein average weight

31731.9 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)
Escherichia coli L-asparaginase
L-asparaginase
L-asparagine amidohydrolase

External IDs

Not Available

Product Ingredients

Not Available

Approved Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Erwinase	Powder, for solution	10000 unit	Intramuscular; Intravenous; Subcutaneous	Jazz Pharmaceuticals France Sas	2009-07-01	Not applicable
Kidrolase	Powder, for solution	10000 unit	Intramuscular; Intravenous	Jazz Pharmaceuticals France Sas	1974-12-31	Not applicable
Spectrila	Injection, powder, for solution	10000 U	Intravenous	Medac Gesellschaft Fuer Klinische Spezialpraeparate Mb H	2016-01-14	Not applicable
Spectrila	Injection, powder, for solution	10000 U	Intravenous	Medac Gesellschaft Fuer Klinische Spezialpraeparate Mb H	2016-01-14	Not applicable

Approved Generic Prescription Products

Not Available

Approved Over the Counter Products

Not Available

Unapproved/Other Products

Not Available

International/Other Brands

Elspar (Merck & Co. Inc)

Brand mixtures

Not Available

Categories

UNII

G4FQ3CKY5R

CAS number

9015-68-3

Pharmacology

Indication

For treatment of acute lympocytic leukemia and non-Hodgkins lymphoma

Structured Indications

Acute Lymphoblastic Leukaemias (ALL)

Pharmacodynamics

In 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 action

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.

Target	Actions	Organism
AL-asparagine	other/unknown	Human

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Not Available

Half life

8-30 hrs

Clearance

Not Available

Toxicity

Not Available

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction	Drug group
Acetyldigitoxin	Acetyldigitoxin may decrease the cardiotoxic activities of Asparaginase.	Approved
Bevacizumab	Bevacizumab may increase the cardiotoxic activities of Asparaginase.	Approved, Investigational
Cabazitaxel	The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Asparaginase.	Approved
Cyclophosphamide	Cyclophosphamide may increase the cardiotoxic activities of Asparaginase.	Approved, Investigational
Deslanoside	Deslanoside may decrease the cardiotoxic activities of Asparaginase.	Approved
Dexamethasone	The serum concentration of Dexamethasone can be increased when it is combined with Asparaginase.	Approved, Investigational, Vet Approved
Digitoxin	Digitoxin may decrease the cardiotoxic activities of Asparaginase.	Approved
Digoxin	Digoxin may decrease the cardiotoxic activities of Asparaginase.	Approved
Docetaxel	The risk or severity of adverse effects can be increased when Docetaxel is combined with Asparaginase.	Approved, Investigational
Oleandrin	Anvirzel may decrease the cardiotoxic activities of Asparaginase.	Experimental
Ouabain	Ouabain may decrease the cardiotoxic activities of Asparaginase.	Approved
Paclitaxel	The risk or severity of adverse effects can be increased when Paclitaxel is combined with Asparaginase.	Approved, Vet Approved
Trastuzumab	Trastuzumab may increase the cardiotoxic activities of Asparaginase.	Approved, Investigational

Food Interactions

Not 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

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 ]
Link [Link]

External Links

UniProt: P37595
Genbank: U00096
ChEMBL: CHEMBL2108989
PharmGKB: PA448492
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Asparaginase

ATC Codes

L01XX02 — Asparaginase

AHFS Codes

10:00.00

PDB Entries

1NNS

FDA label

Download (880 KB)

MSDS

Not Available

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
1	Active Not Recruiting	Other	Acute Myeloid Leukaemias (AML)	1
1	Completed	Supportive Care	Acute Lymphoblastic Leukaemias (ALL) / Non Hodgkins Lymphoma	1
1	Completed	Treatment	Acute Lymphoid Leukemia Relapse / Acute Lymphoid Leukemia Relapse After Bone Marrow Transplant	1
1	Completed	Treatment	Leukemias	1
1	Completed	Treatment	Leukemias / Myelodysplastic Syndromes	1
1	Terminated	Treatment	Acute Lymphoblastic Leukaemia Recurrent / Allergy to Native e.Coli Asparaginase / Allergy to PEG e.Coli Asparaginase	1
1, 2	Active Not Recruiting	Treatment	Recurrent Childhood Acute Lymphoblastic Leukemia	1
1, 2	Completed	Treatment	Acute 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 Leukemia	1
1, 2	Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL)	1
2	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL)	1
2	Completed	Treatment	Acute Lymphocytic Leukemia (ALL)	1
2	Completed	Treatment	B-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 Leukemia	1
2	Completed	Treatment	Leukemias	10
2	Completed	Treatment	Leukemias / Malignant Lymphomas	2
2	Completed	Treatment	Leukemias / Neutropenias / Thrombocytopenias	1
2	Completed	Treatment	Malignant Lymphomas	1
2	Completed	Treatment	Non-Hodgkin's Lymphoma (NHL)	1
2	Not Yet Recruiting	Treatment	Acute B-Cell Lymphoblastic Leukaemia	1
2	Not Yet Recruiting	Treatment	B 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 Lymphoma	1
2	Not Yet Recruiting	Treatment	Malignancies, Hematologic	1
2	Recruiting	Treatment	Extranodal NK-T-CELL LYMPHOMA / NK/T Cell Lymphoma	1
2	Recruiting	Treatment	Lymphoma, Extranodal NK-T-Cell	1
2	Terminated	Treatment	Acute Lymphocytic Leukemia (ALL) / Acute Myeloid Leukaemias (AML) / Mixed Lineage Acute Leukemia	1
2	Terminated	Treatment	Lymphoma, Lymphoblastic	1
2	Terminated	Treatment	Recurrent Adult Acute Lymphoblastic Leukemia	1
2	Unknown Status	Treatment	Leukemias	2
2	Unknown Status	Treatment	Lymphoblastic Leukemia, Acute	1
2	Withdrawn	Treatment	Acute Lymphoblastic Leukemia (ALL)/Lymphoblastic Lymphoma (LBL)	1
2, 3	Completed	Treatment	Acute Lymphoblastic Leukemia, in Relapse	1
2, 3	Completed	Treatment	Adult 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 Leukemia	1
2, 3	Unknown Status	Treatment	Leukemias	1
3	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL) / Adult 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 Leukemia	1
3	Active Not Recruiting	Treatment	Acute Myeloid Leukaemias (AML) / Granulocytic Sarcoma / Leukaemia cutis / Myeloid Neoplasm / Untreated Adult Acute Myeloid Leukemia / Untreated Childhood Myeloid Neoplasm	1
3	Active Not Recruiting	Treatment	Acute Undifferentiated Leukemia (AUL) / T-cell Childhood Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia	1
3	Active Not Recruiting	Treatment	B-cell Childhood Acute Lymphoblastic Leukemia / Intermediate Risk Recurrent Childhood Acute Lymphoblastic Leukemia / L1 Childhood Acute Lymphoblastic Leukemia / L2 Childhood Acute Lymphoblastic Leukemia	1
3	Active Not Recruiting	Treatment	Childhood 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 Malignancies	1
3	Active Not Recruiting	Treatment	Drug/Agent Toxicity by Tissue/Organ / Leukemias	1
3	Active Not Recruiting	Treatment	Leukemias	1
3	Active Not Recruiting	Treatment	Malignant Lymphomas	1
3	Completed	Supportive Care	Cardiac Toxicity / Leukemias / Malignant Lymphomas	1
3	Completed	Treatment	Acute Lymphoblastic Leukaemias (ALL)	2
3	Completed	Treatment	Childhood 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 Malignancies	1
3	Completed	Treatment	Childhood Acute Lymphoblastic Leukemia in Remission / Recurrent Childhood Acute Lymphoblastic Leukemia	1
3	Completed	Treatment	Leukemias	9
3	Completed	Treatment	Leukemias / Malignant Lymphomas	1
3	Completed	Treatment	Leukemias / Myelodysplastic Syndromes	1
3	Completed	Treatment	Leukemias / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Neoplasms	1
3	Recruiting	Treatment	Acute Lymphoblastic Leukemia, Pediatric	1
3	Recruiting	Treatment	B Acute Lymphoblastic Leukemia / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia	1
3	Recruiting	Treatment	Childhood Acute Myeloid Leukemia / Childhood Myelodysplastic Syndrome / Cytopenias / Down Syndrome (DS) / Myeloid Leukemia Associated With Down Syndrome / Myeloproliferative Neoplasms	1
3	Terminated	Treatment	Acute Lymphoblastic Leukaemias (ALL)	1
3	Terminated	Treatment	Malignant Lymphomas	1
3	Unknown Status	Treatment	Leukemias	2
3	Unknown Status	Treatment	Leukemias / Malignant Lymphomas	1
3	Unknown Status	Treatment	Lymphoblastic Leukemia, Acute	1
3	Unknown Status	Treatment	Malignant Lymphomas	2
3	Withdrawn	Treatment	Leukemias	1
4	Completed	Treatment	Acute Lymphoblastic Leukaemias (ALL)	5
4	Completed	Treatment	Adult Acute Lymphocytic Leukemia	3
4	Completed	Treatment	Lymphoma, Lymphoblastic	1
4	Recruiting	Treatment	Acute Lymphobkastic Leukemia	1
4	Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL)	1
4	Recruiting	Treatment	Peripheral T Cell Lymphoma (PTCL)	1
4	Unknown Status	Treatment	Adult Acute Lymphocytic Leukemia	2
Not Available	Active Not Recruiting	Treatment	Adult Acute Lymphoblastic Leukemia / Childhood Acute Lymphoblastic Leukemia	1
Not Available	Active Not Recruiting	Treatment	Leukemias	1
Not Available	Completed	Treatment	L1 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 Leukemia	1
Not Available	Completed	Treatment	Leukemia, Lymphocytic, Acute	1
Not Available	Completed	Treatment	Leukemias	1
Not Available	Completed	Treatment	Lymphoma, Lymphoblastic	1
Not Available	Completed	Treatment	T-cell Childhood Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia	1
Not Available	No Longer Available	Not Available	Acute Lymphoblastic Leukaemias (ALL) / Acute Lymphocytic Leukemia (ALL)	1
Not Available	Unknown Status	Treatment	Leukemias	2
Not Available	Unknown Status	Treatment	Ph-negative Adult Acute Lymphoblastic Leukemia	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Dosage forms

Form	Route	Strength
Powder, for solution	Intramuscular; Intravenous; Subcutaneous	10000 unit
Powder, for solution	Intramuscular; Intravenous	10000 unit
Injection, powder, for solution	Intravenous	10000 U

Prices

Unit description	Cost	Unit
Elspar 10000 unit vial	74.6USD	vial

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Not Available

Properties

State

Liquid

Experimental Properties

Property	Value	Source
hydrophobicity	0.059	Not Available
isoelectric point	4.67	Not Available

Taxonomy

Description: Not Available
Kingdom: Organic Compounds
Super Class: Organic Acids
Class: Carboxylic Acids and Derivatives
Sub Class: Amino Acids, Peptides, and Analogues
Direct Parent: Peptides
Alternative Parents: Not Available
Substituents: Not Available
Molecular Framework: Not Available
External Descriptors: Not Available

Targets

1. L-asparagine

Kind

Small molecule

Organism

Human

Pharmacological action

Yes

Actions

Other/unknown

References

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 ]
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 ]
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 ]
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 ]
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 ]

Drug created on June 13, 2005 07:24 / Updated on June 08, 2017 10:01