1. Rasburicase Drugbank ID: DB00049
Protein chemical formula : C1521H2381N417O461S7
Protein average weight :
Half-life : 18 hours

2. Description Indication Pharmacodynamics
Rasburicase is a recombinant urate-oxidase enzyme produced by a genetically modified Saccharomyces cerevisiae strain. The cDNA coding for rasburicase was cloned from a strain of Aspergillus flavus .
Indication
For treatment of hyperuricemia, reduces elevated plasma uric acid levels (from chemotherapy)
Pharmacodynamics
Drugs used to treat lympohoid leukemia, non-Hodgkin's lymphoma and acute myelogenous leukemia often lead to the accumulation of toxic plasma levels of purine metabolites (i.e. uric acid). The injection of rasburicase reduces levels of uric acid and mitigates the toxic effects of chemotherapy induced tumor lysis.

3. Volume of Distribution
Mechanism Of Action
Rasburicase catalyzes enzymatic oxidation of uric acid into an inactive and soluble metabolite (allantoin).
Volume of Distribution
110 to 127 mL/kg [pediatric patients]
75.8 to 138 mL/kg [adult patients]
Categories
Gout Suppressants and Antihyperuricemic Agents
Affected Organism
Humans and other mammals
Patents
Country Patent Number Approved Expires
Canada
Canada

4. Sequence
SAVKAARYGKDNVRVYKVHKDEKTGVQTVYEMTVCVLLEGEIETSYTKADNSVIVATDSIKNTIYITAKQNPVTPPELFGSILGTHFIEKYNHIHAAHVNIVCHRWTRMDIDGKPHPHSFIRDSEEKRNVQVDVVEGKGIDIKSSLSGLTVLKSTNSQFWGFLRDEYTTLKETWDRILSTDVDATWQWKNFSGLQEVRSHVPKFDATWATAREVTLKTFAEDNSASVQATMYKMAEQILARQQLIETVEYSLPNKHYFEIDLSWHKGLQNTGKNAEVFAPQSDPNGLIKCTVGRSSLKSKL
Targets :
Uric acid

5. Brands : Elitek Company : Sanofi-Synthelabo Inc Description : Elitek (rasburicase) is a recombinant urate-oxidase produced by a genetically modified Saccharomyces cerevisiae strain. The cDNA coding for rasburicase was cloned from a strain of Aspergillus flavus. Rasburicase is a tetrameric protein with identical subunits. Each subunit is made up of a single 301 amino acid polypeptide chain with a molecular mass of about 34 kDa. Used For/Prescribed for : It is used for preventing high blood levels of uric acid from occurring in patients with certain types of cancer (eg, leukemia, lymphoma, solid malignant tumors) who are receiving cancer chemotherapy treatment. Formulation : Elitek (rasburicase) is supplied in 3 mL and 10 mL colorless, glass vials containing rasburicase at a concentration of 1.5 mg/mL after reconstitution. Elitek 1.5 mg presentation contains 1.5 mg rasburicase, 10.6 mg mannitol, 15.9 mg L-alanine, between 12.6 and 14.3 mg of dibasic sodium phosphate (lyophilized powder), and a diluent (1 mL Water for Injection, USP, and 1 mg Poloxamer 188). Elitek 7.5 mg presentation contains 7.5 mg of rasburicase, 53 mg mannitol, 79.5 mg L-alanine, and between 63 and 71.5 mg dibasic sodium phosphate (lyophilized powder) and a diluent (5 mL Water for Injection, USP, and 5 mg Poloxamer 188).

6. Form : sterile, white to off-white, lyophilized powder Route of administration : intravenous administration Dosage : The recommended dose of Elitek (rasburicase) is 0.2 mg/kg as a 30 minute intravenous infusion daily for up to 5 days. Dosing beyond 5 days or administration of more than one course is not recommended. Contraindication : in a pateint with history of anaphylaxic or severe hypersensitivity, individulas deficient in glucose -6-phosphate dehydrogenase. Side effects : SEVERE side effects occur: Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); blue or gray skin color; chest pain; chills; coughing up blood; dark urine; fever; irregular heartbeat; numbness or tingling of the skin; persistent sore throat; severe dizziness; shortness of breath, trouble breathing, or wheezing; swelling of the hands or feet; weakness; yellowing of the eyes and skin.

7. Drug Interaction : A total of 7 drugs (15 brand and generic names) are known to interact with Elitek (rasburicase). among which 6 major drug interactions (13 brand and generic names) and 1 moderate drug interactions (2 brand and generic names). Major Drug Interactions are :
amyl nitrite / sodium nitrite / sodium thiosulfate Citanest Forte (epinephrine / prilocaine) Citanest HCl Plain (prilocaine) Cyanide Antidote Kit (amyl nitrite / sodium nitrite / sodium thiosulfate) Emla (lidocaine / prilocaine topical) Emla Anesthetic Disc (lidocaine / prilocaine topical) epinephrine / prilocaine lidocaine / prilocaine topical Nithiodote (sodium nitrite / sodium thiosulfate) Oraqix (lidocaine / prilocaine topical) prilocaine sodium nitrite sodium nitrite / sodium thiosulfate Minor Drug Interaction ;
idelalisib Zydelig (idelalisib)

8. Brands : Fasturtec Description : Fasturtec is a medicine that contains the active substance rasburicase. It is a recombinant urate-oxidase enzyme produced by genetically modified Saccharomyces cerevisiae strain. Rasburicase is a tetrameric protein with identical subunits of a molecular mass of about 34 kDa. Used For/Prescribed for : Fasturtec is used to treat and prevent high levels of uric acid in the blood in order to prevent kidney failure. It is used in adults and children with blood cancers who are at risk of a sudden rise in uric acid levels when they start to receive chemotherapy (medicines to treat cancer) . Form : powder and solvent that are made upto make solution. Route of administration : intravenous administartion Dosage : The recommended dose is 0.2 mg per kilogram body weight in both children and adults, given as a daily infusion for up to seven days. The duration of treatment is adjusted depending on the patient’s blood levels of uric acid and the doctor’s judgment. The infusion should last 30 minutes. Contraindication : SEVERE side effects occur: Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); blue or gray skin color; chest pain; chills; coughing up blood; dark urine; fever; irregular heartbeat; numbness or tingling of the skin; persistent sore throat; severe dizziness; shortness of breath, trouble breathing, or wheezing; swelling of the hands or feet; weakness; yellowing of the eyes and skin.

9. Genral References
# Giraldez M: A single, fixed dose of Rasburicase (6 mg maximum) for Treatment of Tumor Lysis Syndrome in Adults. Eur J Haematol Apr 12. "Pubmed":
# Collings I, Watier Y, Giffard M, Dagogo S, Kahn R, Bonnete F, Wright JP, Fitch AN, Margiolaki I: Polymorphism of microcrystalline urate oxidase from Aspergillus flavus. Acta Crystallogr D Biol Crystallogr May;66(Pt 5): Epub 2010 Apr 21. "Pubmed":

10. Refrence http://www.elitek.us/ http://www.drugs.com/cdi/elitek.html