| Revision as of 12:36, 6 December 2011 editBeetstra (talk | contribs)Edit filter managers, Administrators172,031 edits Saving copy of the {{drugbox}} taken from revid 463304597 of page Rasburicase for the Chem/Drugbox validation project (updated: 'DrugBank', 'ChEMBL'). |
Latest revision as of 07:20, 21 November 2024 edit Boghog (talk | contribs)Autopatrolled, Extended confirmed users, IP block exemptions, New page reviewers, Pending changes reviewers, Rollbackers, Template editors137,536 edits consistent citation formatting |
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{{Short description|Pharmaceutical drug}} |
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{{ambox | text = This page contains a copy of the infobox ({{tl|drugbox}}) taken from revid of page ] with values updated to verified values.}} |
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{{Use dmy dates|date=August 2024}} |
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{{cs1 config|name-list-style=vanc|display-authors=6}} |
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{{Drugbox |
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{{Drugbox |
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| Verifiedfields = changed |
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| Verifiedfields = changed |
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| verifiedrevid = 458438338 |
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| verifiedrevid = 464380284 |
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| IUPAC_name = Aspergillus urate oxidase |
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| image = Rasburicase.png |
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| image = Rasburicase.png |
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| width = 191 |
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| width = 191 |
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| alt = |
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<!--Clinical data--> |
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<!-- Clinical data --> |
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| tradename = |
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| pronounce = |
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| tradename = Elitek, Fasturtec |
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| Drugs.com = {{drugs.com|monograph|rasburicase}} |
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| Drugs.com = {{drugs.com|monograph|rasburicase}} |
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| MedlinePlus = |
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| pregnancy_category = |
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| DailyMedID = Rasburicase |
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| legal_status = RX/POM |
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| pregnancy_AU = B2 |
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| routes_of_administration = Intravenous |
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| pregnancy_AU_comment = |
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| pregnancy_category= |
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| routes_of_administration = ] |
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| ATC_prefix = V03 |
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| ATC_suffix = AF07 |
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| legal_AU = S4 |
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<!--Pharmacokinetic data--> |
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| legal_US = Rx-only |
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| legal_EU = Rx-only |
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| legal_EU_comment = <ref>{{cite web | title=Fasturtec EPAR | website=European Medicines Agency (EMA) | date=23 February 2001 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/fasturtec | access-date=14 August 2024}}</ref> |
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| legal_status = Rx-only |
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<!-- Pharmacokinetic data --> |
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| bioavailability = N/A |
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| bioavailability = N/A |
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| protein_bound = |
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| protein_bound = |
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| metabolism = |
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| metabolism = |
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| elimination_half-life = 18 hrs |
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| elimination_half-life = 18 hrs |
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| excretion = |
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| excretion = |
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<!--Identifiers--> |
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<!-- Identifiers --> |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID = NA |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 134774-45-1 |
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| CAS_number = 134774-45-1 |
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| ATC_prefix = V03 |
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| ATC_suffix = AF07 |
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| PubChem = |
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| PubChem = |
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| IUPHAR_ligand = 7467 |
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| DrugBank_Ref = {{drugbankcite|changed|drugbank}} |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = DB00049 |
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| DrugBank = DB00049 |
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| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} |
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| ChemSpiderID = none |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = 08GY9K1EUO |
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| UNII = 08GY9K1EUO |
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| KEGG = D05704 |
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| ChEMBL_Ref = {{ebicite|changed|EBI}} |
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| ChEMBL_Ref = {{ebicite|changed|EBI}} |
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| ChEMBL = <!-- blanked - oldvalue: 1201594 --> |
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| ChEMBL = 1201594 |
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| C=1521 | H=2381 | N=417 | O=461 | S=7 |
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<!-- Chemical data --> |
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| molecular_weight = 34109.5 |
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| IUPAC_name = Aspergillus urate oxidase |
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| C=1521 | H=2381 | N=417 | O=461 | S=7 |
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}} |
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}} |
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'''Rasburicase''', sold under the brand name '''Elitek''' in the US and '''Fasturtec''' in the EU, is a ] that helps to clear ] from the ]. It is a ] version of ], an ] that metabolizes uric acid to ]. Urate oxidase is known to be present in many mammals but does not naturally occur in humans.<ref name="Wilson2012"/> Rasburicase is produced by a genetically modified '']'' strain. The ] (cDNA) coding for rasburicase was cloned from a strain of '']''.<ref name="Wilson2012">{{cite journal | vauthors = Wilson FP, Berns JS | title = Onco-nephrology: tumor lysis syndrome | journal = Clinical Journal of the American Society of Nephrology | volume = 7 | issue = 10 | pages = 1730–1739 | date = October 2012 | pmid = 22879434 | doi = 10.2215/CJN.03150312 | doi-access = free }}</ref> |
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Rasburicase ({{UniProt|Q00511}}) is a ] with identical subunits. Each subunit is made up of a single 301 ] polypeptide chain with a molecular mass of about 34 ]. The drug product is a sterile, white to off-white, lyophilized powder intended for intravenous administration following reconstitution with a diluent. 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.<ref name="Elitek rasburicase">{{cite web|title=Elitek (rasburicase)|url=http://www.rxlist.com/elitek-drug/clinical-pharmacology.htm|publisher=Rxlist}}</ref> |
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It is on the ].<ref name="WHO22nd">{{cite book | vauthors = ((World Health Organization)) | title = World Health Organization model list of essential medicines: 22nd list (2021) | year = 2021 | hdl = 10665/345533 | author-link = World Health Organization | publisher = World Health Organization | location = Geneva | id = WHO/MHP/HPS/EML/2021.02 | hdl-access=free }}</ref> |
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==Medical uses== |
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Rasburicase is approved for use by the ] (and European counterparts) for the prevention and treatment of ] (TLS)<ref name="pmid18632493">{{cite journal | vauthors = Ho VQ, Wetzstein GA, Patterson SG, Bradbury R | title = Abbreviated rasburicase dosing for the prevention and treatment of hyperuricemia in adults at risk for tumor lysis syndrome | journal = Supportive Cancer Therapy | volume = 3 | issue = 3 | pages = 178–182 | date = April 2006 | pmid = 18632493 | doi = 10.3816/SCT.2006.n.016 }}</ref> in people receiving ] for ] such as ]s and ]s. However, it is not clear if it results in important benefits such as decreased kidney problems or decreased risk of death as of 2017.<ref>{{cite journal | vauthors = Cheuk DK, Chiang AK, Chan GC, Ha SY | title = Urate oxidase for the prevention and treatment of tumour lysis syndrome in children with cancer | journal = The Cochrane Database of Systematic Reviews | volume = 2017 | issue = 3 | pages = CD006945 | date = March 2017 | pmid = 28272834 | pmc = 6464610 | doi = 10.1002/14651858.CD006945.pub4 }}</ref> |
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It is being investigated for treating severely ] from other sources. For example, it has been used for hyperuricemia in ],<ref name="pmid17396159">{{cite journal | vauthors = Cammalleri L, Malaguarnera M | title = Rasburicase represents a new tool for hyperuricemia in tumor lysis syndrome and in gout | journal = International Journal of Medical Sciences | volume = 4 | issue = 2 | pages = 83–93 | date = March 2007 | pmid = 17396159 | pmc = 1838823 | doi = 10.7150/ijms.4.83 }}</ref> in other ] conditions, and in ] with ].<ref name="pmid_21572370">{{cite journal | vauthors = Lin PY, Lin CC, Liu HC, Lee MD, Lee HC, Ho CS, Chiu NC, Peng CC, Huang FY, Tsai JD | title = Rasburicase improves hyperuricemia in patients with acute kidney injury secondary to rhabdomyolysis caused by ecstasy intoxication and exertional heat stroke | journal = Pediatric Critical Care Medicine | volume = 12 | issue = 6 | pages = e424–e427 | date = November 2011 | pmid = 21572370 | doi = 10.1097/PCC.0b013e3182192c8d | s2cid = 23910863 }}</ref> |
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=== Contraindication === |
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Rasburicase use is contraindicated in patients with a G6PDH deficiency as it may cause sudden, severe hemolysis. The blood smear revealed numerous abnormal red blood cells (RBCs) with membranous defects (bite cells) and submembranous blister-like structures (blister cells). These cell types are characteristic of Heinz body hemolytic anemia (HBHA). While Heinz bodies are not visible on a Giemsa-stained smear, they can be detected with supravital staining, appearing as 1- to 3-μm inclusions in RBCs (inset).<ref>{{cite book | vauthors = Dean L, Kane M | chapter = Rasburicase Therapy and G6PD and CYB5R Genotype | veditors = Pratt VM, Scott SA, Pirmohamed M, etal | title = Medical Genetics Summaries | date = 29 September 2020 | publisher = National Center for Biotechnology Information (US) | pmid = 32997466 | chapter-url = https://www.ncbi.nlm.nih.gov/books/NBK562585/ }}</ref><ref>{{cite journal | vauthors = Hrisinko MA, Chen YH | title = Rasburicase-induced Heinz body hemolytic anemia in a patient with chronic lymphocytic leukemia | journal = Blood | volume = 126 | issue = 6 | pages = 826 | date = August 2015 | pmid = 26473196 | doi = 10.1182/blood-2015-06-648576 }}</ref> |
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==Side effects== |
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Rasburicase administration can cause ] (incidence unknown); ] may occur in susceptible individuals such as those with ] due to the production of hydrogen peroxide in the urate oxidase reaction.<ref name="Wilson2012"/> Testing patients for G6PDH deficiency prior to starting a course of rasburicase has been recommended.<ref name="Wilson2012"/> |
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==Pharmacology== |
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=== Mechanism of Action === |
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In humans, ] is the final step in the catabolic pathway of purines. Rasburicase catalyzes enzymatic oxidation of poorly soluble uric acid into an inactive and more soluble metabolite allantoin with ] and ] as byproducts in the chemical reaction.<ref name="Wilson2012"/> |
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=== Pharmacodynamics === |
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The measurement of plasma uric acid was used to evaluate the effectiveness of rasburicase in clinical studies. Following administration of either 0.15 or 0.20 mg/kg rasburicase daily for up to 5 days, plasma uric acid levels decreased within 4 hours and were maintained below 7.5 mg/dL in 98% of adult and 90% of pediatric patients for at least 7 days. There was no evidence of a dose response effect on uric acid control for doses between 0.15 and 0.20 mg/kg rasburicase.<ref name="Elitek rasburicase"/> |
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=== Pharmacokinetics === |
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The pharmacokinetics of rasburicase were evaluated in both pediatric and adult patients with ], ] or other hematological malignancies. Rasburicase exposure, as measured by AUC0-24 hr and Cmax, tended to increase with a dose range from 0.15 to 0.2 mg/kg. The mean terminal half-life was similar between pediatric and adult patients and ranged from 15.7 to 22.5 hours. The mean volume of distribution of rasburicase ranged from 110 to 127 mL/kg in pediatric patients and from 75.8 to 138 mL/kg in adult patients, respectively. Minimal accumulation of rasburicase ( < 1.3 fold) was observed between days 1 and 5 of dosing. In adults, age, gender, baseline liver enzymes and creatinine clearance did not impact the pharmacokinetics of rasburicase. A cross-study comparison revealed that after administration of rasburicase at 0.15 or 0.20 mg/kg, the geometric mean values of body-weight normalized clearance were approximately 40% lower in Japanese (n=20) than that in Caucasians (n=22).<ref name="Elitek rasburicase"/> |
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== Society and culture == |
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=== Economics === |
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Rasburicase is much more expensive than the conventional uric acid lowering treatment for ].<ref name="pmid15708917">{{cite journal | vauthors = Reinders MK, van Roon EN, Brouwers JR, Jansen TL | title = A costly therapeutic dilemma in tophaceous gout: is etanercept or rasburicase preferable? | journal = Annals of the Rheumatic Diseases | volume = 64 | issue = 3 | pages = 516; author reply 516 | date = March 2005 | pmid = 15708917 | pmc = 1755382 | doi = 10.1136/ard.2003.017087corr1 }}</ref> |
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== References == |
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{{reflist}} |
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{{Detoxifying agents for antineoplastic treatment}} |
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{{Portal bar | Medicine}} |
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