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Asparaginase
Systematic (IUPAC) name
E. coli L-asparagine amidohydrolase
Identifiers
CAS number 9015-68-3
ATC code L01XX02
PubChem  ?
DrugBank BTD00011
Chemical data
Formula C 1377H2208N382O442S17  
Mol. mass 31731.9 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 8-30 hrs
Excretion  ?
Therapeutic considerations
Pregnancy cat. C(US)
Legal status
Routes  ?

Asparaginase (EC 3.5.1.1) is an enzyme that catalyzes the hydrolysis of asparagine to aspartic acid. It is marketed under the brand name Elspar, to treat acute lymphoblastic leukemia (ALL) and is also used in some mast cell tumor protocols. [1] Unlike other chemotherapy agents, it can be given as an intramuscular, subcutaneous, or intravenous injection without fear of tissue irritation.

Contents

Mechanism of action

The rationale behind asparaginase is that it takes advantage of the fact that ALL leukemic cells are unable to synthesize the non-essential amino acid asparagine, whereas normal cells are able to make their own asparagine; thus leukemic cells require high amount of asparagine. These leukemic cells depend on circulating asparagine. Asparaginase, however, catalyzes the conversion of L-asparagine to aspartic acid and ammonia. This deprives the leukemic cell of circulating asparagine.

Side effects

The main side-effect is an allergic or hypersensitivity reaction. Asparaginase has also been associated with pancreatitis. Additionally, it can also be associated with a coagulopathy as it decreases protein synthesis, including synthesis of coagulation factors (eg progressive isolated decrease of fibrinogen) and anticoagulant factor (generally antithrombin III; sometimes protein C & S as well), leading to bleeding or thrombotic events such as stroke.

References

  1. ^ Appel IM, van Kessel-Bakvis C, Stigter R, Pieters R (2007). "Influence of two different regimens of concomitant treatment with asparaginase and dexamethasone on hemostasis in childhood acute lymphoblastic leukemia". Leukemia 21: 2377. doi:10.1038/sj.leu.2404793. PMID 17554375.  

External links

  • MeSH Asparaginase
  • [1] THE PET PHARMACY By Wendy C. Brooks, DVM, DipABVP; Educational Director, VeterinaryPartner.com







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