Asparaginase Drugbank ID : DB00023 Protein chemical formula : C1377H2208N382O442S17 Protein average weight : 31731.9000 Half life : 8-30 hrs

Description : Indication : Pharmacodynamics : L-asparagine amidohydrolase from E. coli Indication : For treatment of acute lympocytic leukemia and non-Hodgkins lymphoma 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 : Drug Interaction: Targets : Affected organisms : 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. Drug Interaction: Trastuzumab : Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. Targets : L-asparagine Affected organisms : Humans and other mammals

Categories : Sequence : Antineoplastic Agents QMSLQQELRYIEALSAIVETGQKMLEAGESALDVVTEAVRLLEECPLFNAGIGAVFTRDETHELDACVMDGNTLKAGAVAGVSHLRNPVLAARLVMEQSPHVMMIGEGAENFAFARGMERVSPEIFSTSLRYEQLLAARKEGATVLDHSGAPLDEKQKMGTVGAVALDLDGNLAAATSTGGMTNKLPGRVGDSPLVGAGCYANNASVAVSCTGTGEVFIRALAAYDIAALMDYGGLSLAEACERVVMEKLPTLGGSGGLIAIDHEGNVALPFNTEGMYRAWGYAGDTPTTGIYREKGDTVATQ

Brands : Elspar Company : Merck & Co. Inc Description : Elspar (asparaginase) 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 Unit of asparaginase is defined as that amount of enzyme required to generate 1 μmol of ammonia per minute at pH 7.3 and 37°C. The specific activity of Elspar is at least 225 International Units per milligram of protein. Used for/Prescribed for : Treating acute lymphocytic leukemia (ALL). It is used along with other cancer medicines. Elspar is an antineoplastic agent. It works by decreasing the amount of asparagine in the body, which kills certain leukemia cells. Formulation : Each vial contains 10,000 International Units of asparaginase and 80 mg of mannitol. Form : lyophilized plug or powder Route of administration : intravenous or intramuscular. Intravenous method dose has higher risk of allergic reaction, so often a test dose is given first.

Dosage : The recommended dose of Elspar is 6,000 International Units/m² intramuscularly (IM) or intravenously (IV) three times a week. Contraindication : allergic Side effects : Fever, chills (see flu like symptoms) Nausea and vomiting Allergic reaction, (sudden onset of wheezing, itching, rash, face swelling, agitation, low blood pressure). Drug interaction : A total of 155 drugs (461 brand and generic names) are known to interact with Elspar (asparaginase escherichia coli). In which 30 major drug interactions (74 brand and generic names) and 125 moderate drug interactions (387 brand and generic names) .

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 Jun 7;. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17554375 # http://www.google.com/patents/EP2046369A2

References : http://www. rxlist. com/elspar-drug. htm http://www