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Identification
Name Pegaspargase
Accession Number DB00059 (BIOD00079, BTD00079)
Type biotech
Groups approved
Description

Pegylated L-asparagine amidohydrolase from E. coli. Pegylation substantially (by a factor of 4) extends the protein half life.
Protein structure Db00059
Display: 3D Structure
Protein chemical formula C1377H2208N382O442S17
Protein average weight 31731.9000
Sequences 
>DB00059 sequence
QMSLQQELRYIEALSAIVETGQKMLEAGESALDVVTEAVRLLEECPLFNAGIGAVFTRDE
THELDACVMDGNTLKAGAVAGVSHLRNPVLAARLVMEQSPHVMMIGEGAENFAFARGMER
VSPEIFSTSLRYEQLLAARKEGATVLDHSGAPLDEKQKMGTVGAVALDLDGNLAAATSTG
GMTNKLPGRVGDSPLVGAGCYANNASVAVSCTGTGEVFIRALAAYDIAALMDYGGLSLAE
ACERVVMEKLPALGGSGGLIAIDHEGNVALPFNTEGMYRAWGYAGDTPTTGIYREKGDTV
ATQ

FASTA
Synonyms
  • L-asparagine amidohydrolase
  • Putative L-asparaginase precursor
Synonyms
L-asparagine amidohydrolase
Putative L-asparaginase precursor
Salts Not Available
Brand names
Name Company
Oncaspar (Enzon Inc)
Brand mixtures Not Available
Categories
  • Antineoplastic Agents
CAS number 130167-69-0
Taxonomy
Kingdom Not Available
Classes Not Available
Substructures Not Available
Pharmacology
Indication For treatment of acute lymphoblastic leukemia
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. Oncaspar exploits a metabolic defect in asparagine synthesis of some malignant cells.
Mechanism of action Pegaspargase, 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.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers Not Available
Packagers
Dosage forms
Form Route Strength
Injection, solution Intramuscular
Injection, solution Intravenous
Prices
Unit description Cost Unit
Oncaspar 750 unit/ml vial 656.0 USD ml
Patents Not Available
Properties
State liquid
Melting point Not Available
Experimental Properties
Property Value Source
hydrophobicity 0.059 PhysProp
isoelectric point 4.67 Various sources
References
Synthesis Reference Not Available
General Reference
  1. Graham ML: Pegaspargase: a review of clinical studies. Adv Drug Deliv Rev. 2003 Sep 26;55(10):1293-302. Pubmed
External Links
Resource Link
UniProt P37595 Link_out
Genbank U00096 Link_out
PharmGKB PA450833 Link_out
Drug Product Database 2236849 Link_out
RxList http://www.rxlist.com/cgi/generic2/pegaspargase.htm Link_out
Drugs.com http://www.drugs.com/cdi/pegaspargase.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Pegaspargase Link_out
ATC Codes
  • L01XX24
AHFS Codes Not Available
PDB Entries
FDA label show (400 KB)
MSDS Not Available
Interactions
Drug Interactions
Drug Interaction
Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Food Interactions Not Available
Targets

1. Asparagine

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
  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
  3. Douer D, Yampolsky H, Cohen LJ, Watkins K, Levine AM, Periclou AP, Avramis VI: Pharmacodynamics and safety of intravenous pegaspargase during remission induction in adults aged 55 years or younger with newly diagnosed acute lymphoblastic leukemia. Blood. 2007 Apr 1;109(7):2744-50. Pubmed
  4. 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
  5. Dinndorf PA, Gootenberg J, Cohen MH, Keegan P, Pazdur R: FDA drug approval summary: pegaspargase (oncaspar) for the first-line treatment of children with acute lymphoblastic leukemia (ALL). Oncologist. 2007 Aug;12(8):991-8. Pubmed
Comments
Drug created on June 13, 2005 07:24 / Updated on September 03, 2010 13:03