Details of the Drug
General Information of Drug (ID: DM4F29C)
| Drug Name | Crizotinib | ||||||||||||||||||||||
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| Synonyms | Xalkori (TN); novel ALK inhibitors | ||||||||||||||||||||||
| Indication | 
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| Affected Organisms | Humans and other mammals | ||||||||||||||||||||||
| ATC Code | |||||||||||||||||||||||
| Drug Type | Small molecular drug | ||||||||||||||||||||||
| Structure |  | ||||||||||||||||||||||
| 3D MOL | 2D MOL | ||||||||||||||||||||||
| #Ro5 Violations (Lipinski): 0 | Molecular Weight (mw) | 450.3 | |||||||||||||||||||||
| Logarithm of the Partition Coefficient (xlogp) | 3.7 | ||||||||||||||||||||||
| Rotatable Bond Count (rotbonds) | 5 | ||||||||||||||||||||||
| Hydrogen Bond Donor Count (hbonddonor) | 2 | ||||||||||||||||||||||
| Hydrogen Bond Acceptor Count (hbondacc) | 6 | ||||||||||||||||||||||
| ADMET Property | 
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| Chemical Identifiers | 
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| Cross-matching ID | |||||||||||||||||||||||
| Combinatorial Drugs (CBD) | Click to Jump to the Detailed CBD Information of This Drug | ||||||||||||||||||||||
Molecular Interaction Atlas of This Drug
|  Drug Therapeutic Target (DTT) | 
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|  Drug Transporter (DTP) | 
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|  Drug-Metabolizing Enzyme (DME) | 
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|  Drug Off-Target (DOT) | 
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| Molecular Interaction Atlas (MIA) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Molecular Expression Atlas of This Drug
| The Studied Disease | Non-small-cell lung cancer | |||||||||||||||||||||||||||||||||||||||||||||||||||||
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| ICD Disease Classification | 2C25.Y | |||||||||||||||||||||||||||||||||||||||||||||||||||||
| 
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| Molecular Expression Atlas (MEA) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||
Experimental Cancer Drug Sensitivity Information
Drug-Drug Interaction (DDI) Information of This Drug
| Coadministration of a Drug Treating the Same Disease as Crizotinib 
 Coadministration of a Drug Treating the Disease Different from Crizotinib (Comorbidity) 
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug
| DIG | 
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| Pharmaceutical Formulation | 
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References
| 1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4903). | ||||
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| 2 | BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs | ||||
| 3 | Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds | ||||
| 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| 5 | Met tyrosine kinase inhibitor, PF-2341066, suppresses growth and invasion of nasopharyngeal carcinoma.Drug Des Devel Ther. 2015 Aug 26;9:4897-907. | ||||
| 6 | Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66. | ||||
| 7 | Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar. Int J Cancer. 2014 Mar 15;134(6):1484-94. | ||||
| 8 | Crizotinib for the treatment of non-small-cell lung cancer. Am J Health Syst Pharm. 2013 Jun 1;70(11):943-7. | ||||
| 9 | Multi-parameter in vitro toxicity testing of crizotinib, sunitinib, erlotinib, and nilotinib in human cardiomyocytes. Toxicol Appl Pharmacol. 2013 Oct 1;272(1):245-55. | ||||
| 10 | Cytotoxicity of 34 FDA approved small-molecule kinase inhibitors in primary rat and human hepatocytes. Toxicol Lett. 2018 Jul;291:138-148. doi: 10.1016/j.toxlet.2018.04.010. Epub 2018 Apr 12. | ||||
| 11 | Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers. Sci Transl Med. 2012 Feb 8;4(120):120ra17. doi: 10.1126/scitranslmed.3003316. Epub 2012 Jan 25. | ||||
| 12 | Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon. Toxicol Sci. 2017 Jun 1;157(2):500-509. doi: 10.1093/toxsci/kfx063. | ||||
| 13 | Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification. Mol Cancer Ther. 2012 Jul;11(7):1557-64. doi: 10.1158/1535-7163.MCT-11-0934. Epub 2012 Jun 22. | ||||
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