About: Crizotinib     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type
http://linked.open...gbank/description
  • Crizotinib an inhibitor of receptor tyrosine kinase for the treatment of non-small cell lung cancer (NSCLC). Verification of the presence of ALK fusion gene is done by Abbott Molecular's Vysis ALK Break Apart FISH Probe Kit. This verification is used to select for patients suitable for treatment. FDA approved in August 26, 2011. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # FDA label # Timm A, Kolesar JM: Crizotinib for the treatment of non-small-cell lung cancer. Am J Health Syst Pharm. 2013 Jun 1;70(11):943-7. doi: 10.2146/ajhp120261. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23686600 # Forde PM, Rudin CM: Crizotinib in the treatment of non-small-cell lung cancer. Expert Opin Pharmacother. 2012 Jun;13(8):1195-201. doi: 10.1517/14656566.2012.688029. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22594847 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Plasma terminal half-life, patients = 42 hours (en)
http://linked.open...ugbank/indication
  • Crizotinib is used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) that is anaplastic-lymphoma kinase (ALK)-positive as detected by a FDA-approved test. (en)
sameAs
Title
  • Crizotinib (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Crizotinib is a tyrosine kinase receptor inhibitor. More specifically, it inhibits anaplastic lymphoma kinase (ALK), hepatocyte growth factor receptor (HGFR, c-MET), and Recepteur d'Origine Nantais (RON). Abnormalities in the ALK gene caused by mutations or translocations may lead to expression of oncogenic fusion proteins. In patients with NSCLC, they have the EML4-ALK gene. Crizotinib inhibits ALK tyrosine kinase which ultimately results in decreased proliferation of cells that carry the genetic mutation and tumour survivability. (en)
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Following the administration of a single 250 mg radiolabeled crizotinib dose to healthy subjects, 63% and 22% of the administered dose was recovered in feces and urine, respectively. Unchanged crizotinib represented approximately 53% and 2.3% of the administered dose in feces and urine, respectively. (en)
http://linked.open.../drugbank/synonym
  • C-Met/Hepatocyte Growth Factor Receptor Tyrosine Kinase Inhibitor PF-02341066 (en)
  • (R)-Crizotinib (en)
  • C-Met/HGFR Tyrosine Kinase Inhibitor PF-02341066 (en)
  • Crizotinibum (en)
  • MET Tyrosine Kinase Inhibitor PF-02341066 (en)
  • PF 2341066 (en)
  • PF-2341066 (en)
http://linked.open...umeOfDistribution
  • Mean volume of distribution (Vss) is 1772 L following intravenous administration of a 50 mg dose. This high volume of distribution suggest extensive distribution into tissue from plasma. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • When given with a high-fat meal, AUC and Cmax were reduced by 14%. Despite this, crizotinib may be given with or without food. (en)
http://linked.open...nk/proteinBinding
  • Crizotinib is 91% bound to plasma protein. This is not affected by drug concentration. (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...l/drug/hasATCCode
http://linked.open...nd-Acceptor-Count
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http://linked.open...urface-Area--PSA-
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http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • The peak serum concentration was reached in 4 to 6 hours following an oral single-dose administration. Steady state was reached within 15 days when a dose of 250 mg twice daily was administered. The mean absolute bioavailability was 43% (range of 32% to 66%) following a single 250 mg oral dose. When taken with high-fat meal, AUC and Cmax were reduced. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 877399-52-5 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • The mean apparent clearance (CL/F) of crizotinib was lower at steady state (60 L/hr) after 250 mg twice daily than that after a single 250 mg oral dose (100 L/hr), which was likely due to autoinhibition of CYP3A by crizotinib after multiple dosing. (en)
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...-strongest-basic-
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