Details of the Drug

General Information of Drug (ID: DM4F29C)

Drug Name
Crizotinib
Synonyms Xalkori (TN); novel ALK inhibitors
Indication
Disease Entry ICD 11 Status REF
Non-small-cell lung cancer 2C25.Y Approved [1], [2]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 450.3
Topological Polar Surface Area (xlogp) 3.7
Rotatable Bond Count (rotbonds) 5
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 6
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Clearance
The drug present in the plasma can be removed from the body at the rate of 9.75 mL/min/kg [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 42 hours [4]
Metabolism
The drug is metabolized via the CYP3A4 and CYP3A5 in which these enzymes mediates the O-dealkylation of the drug [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.09% [4]
Vd
The volume of distribution (Vd) of drug is 1772 L [6]
Chemical Identifiers
Formula
C21H22Cl2FN5O
IUPAC Name
3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
Canonical SMILES
C[C@H](C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N
InChI
InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m1/s1
InChIKey
KTEIFNKAUNYNJU-GFCCVEGCSA-N
Cross-matching ID
PubChem CID
11626560
ChEBI ID
CHEBI:64310
CAS Number
877399-52-5
DrugBank ID
DB08865
TTD ID
D03ZBT
VARIDT ID
DR00523
INTEDE ID
DR0387
ACDINA ID
D00154

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
ALK tyrosine kinase receptor (ALK) TTPMQSO ALK_HUMAN Modulator [7]
HGF/Met signaling pathway (HGF/Met pathway) TTKA5LP NOUNIPROTAC Inhibitor [8]
Proto-oncogene c-Met (MET) TTNDSF4 MET_HUMAN Modulator [7]
Proto-oncogene c-Ros (ROS1) TTSZ6Y3 ROS1_HUMAN Modulator [7]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [9]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [9]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [10]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [11]
Cytochrome P450 3A5 (CYP3A5)
Main DME 		DEIBDNY CP3A5_HUMAN Substrate [11]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Non-small-cell lung cancer
ICD Disease Classification 2C25.Y
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Proto-oncogene c-Met (MET) DTT MET 1.08E-03 -0.24 -0.4
P-glycoprotein 1 (ABCB1) DTP P-GP 9.39E-02 1.07E-01 2.80E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 9.69E-01 1.16E-03 3.56E-03
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 8.15E-01 6.20E-03 5.61E-02
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 9.96E-01 -3.17E-03 -1.84E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.04E-02 6.29E-02 3.54E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Crizotinib
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Ceritinib DMB920Z Major Decreased metabolism of Crizotinib caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [71]
Lurbinectedin DMEFRTZ Major Decreased metabolism of Crizotinib caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [72]
PF-06463922 DMKM7EW Moderate Increased metabolism of Crizotinib caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [73]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Crizotinib and Osimertinib. Lung cancer [2C25] [74]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Crizotinib caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [75]
Capmatinib DMYCXKL Moderate Decreased metabolism of Crizotinib caused by Capmatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [76]
Selpercatinib DMZR15V Major Decreased metabolism of Crizotinib caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [77]
⏷ Show the Full List of 7 DDI Information of This Drug
Coadministration of a Drug Treating the Disease Different from Crizotinib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Crizotinib and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [71]
Metreleptin DM1NOEK Moderate Increased metabolism of Crizotinib caused by Metreleptin mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [73]
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Crizotinib and Ivosidenib. Acute myeloid leukaemia [2A60] [78]
Arn-509 DMT81LZ Major Increased metabolism of Crizotinib caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [71]
Gilteritinib DMWQ4MZ Major Increased risk of prolong QT interval by the combination of Crizotinib and Gilteritinib. Acute myeloid leukaemia [2A60] [74]
Oliceridine DM6MDCF Major Decreased metabolism of Crizotinib caused by Oliceridine mediated inhibition of CYP450 enzyme. Acute pain [MG31] [79]
Ivabradine DM0L594 Major Decreased metabolism of Crizotinib caused by Ivabradine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [80]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Crizotinib and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [81]
Levalbuterol DM5YBO1 Moderate Increased risk of ventricular arrhythmias by the combination of Crizotinib and Levalbuterol. Asthma [CA23] [82]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Crizotinib and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [83]
Eribulin DM1DX4Q Major Increased risk of prolong QT interval by the combination of Crizotinib and Eribulin. Breast cancer [2C60-2C6Y] [74]
Talazoparib DM1KS78 Moderate Decreased clearance of Crizotinib due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [84]
HKI-272 DM6QOVN Major Decreased metabolism of Crizotinib caused by HKI-272 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [85]
LY2835219 DM93VBZ Moderate Decreased metabolism of Crizotinib caused by LY2835219 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [86]
Tucatinib DMBESUA Major Decreased metabolism of Crizotinib caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [71]
Palbociclib DMD7L94 Moderate Decreased metabolism of Crizotinib caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [77]
Macitentan DMP79A1 Moderate Decreased metabolism of Crizotinib caused by Macitentan mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [87]
PF-04449913 DMSB068 Major Increased risk of prolong QT interval by the combination of Crizotinib and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [74]
Olodaterol DM62B78 Moderate Increased risk of ventricular arrhythmias by the combination of Crizotinib and Olodaterol. Chronic obstructive pulmonary disease [CA22] [88]
Vilanterol DMF5EK1 Moderate Increased risk of prolong QT interval by the combination of Crizotinib and Vilanterol. Chronic obstructive pulmonary disease [CA22] [82]
Intedanib DMSTA36 Moderate Decreased clearance of Crizotinib due to the transporter inhibition by Intedanib. Colorectal cancer [2B91] [89]
Osilodrostat DMIJC9X Major Increased risk of prolong QT interval by the combination of Crizotinib and Osilodrostat. Cushing syndrome [5A70] [74]
MK-8228 DMOB58Q Moderate Decreased metabolism of Crizotinib caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [74]
OPC-34712 DMHG57U Major Decreased metabolism of Crizotinib caused by OPC-34712 mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [90]
Deutetrabenazine DMUPFLI Major Increased risk of prolong QT interval by the combination of Crizotinib and Deutetrabenazine. Dystonic disorder [8A02] [74]
Ingrezza DMVPLNC Major Increased risk of prolong QT interval by the combination of Crizotinib and Ingrezza. Dystonic disorder [8A02] [74]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Crizotinib caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [73]
Cannabidiol DM0659E Minor Decreased metabolism of Crizotinib caused by Cannabidiol mediated inhibition of CYP450 enzyme. Epileptic encephalopathy [8A62] [77]
Bay 80-6946 DMLOS5R Moderate Decreased metabolism of Crizotinib caused by Bay 80-6946 mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [91]
Tazemetostat DMWP1BH Major Decreased metabolism of Crizotinib caused by Tazemetostat mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [92]
Mirabegron DMS1GYT Minor Decreased metabolism of Crizotinib caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [93]
Ripretinib DM958QB Moderate Decreased metabolism of Crizotinib caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [71]
Avapritinib DMK2GZX Major Decreased metabolism of Crizotinib caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [77]
Boceprevir DMBSHMF Major Decreased metabolism of Crizotinib caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [71]
MK-1439 DM215WE Minor Decreased metabolism of Crizotinib caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [94]
Fostemsavir DM50ILT Major Increased risk of prolong QT interval by the combination of Crizotinib and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [74]
Cobicistat DM6L4H2 Major Decreased metabolism of Crizotinib caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [71]
Dolutegravir DMCZGRE Minor Decreased metabolism of Crizotinib caused by Dolutegravir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [95]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Crizotinib and Teriflunomide. Hyper-lipoproteinaemia [5C80] [96]
Aliskiren DM1BV7W Moderate Decreased clearance of Crizotinib due to the transporter inhibition by Aliskiren. Hypertension [BA00-BA04] [96]
Lesinurad DMUR64T Moderate Increased metabolism of Crizotinib caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [73]
Berotralstat DMWA2DZ Major Decreased clearance of Crizotinib due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [97]
Suvorexant DM0E6S3 Major Decreased metabolism of Crizotinib caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [98]
Tasimelteon DMLOQ1V Moderate Decreased metabolism of Crizotinib caused by Tasimelteon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [99]
Polyethylene glycol DM4I1JP Moderate Increased risk of ventricular arrhythmias by the combination of Crizotinib and Polyethylene glycol. Irritable bowel syndrome [DD91] [77]
Naloxegol DML0B41 Major Decreased metabolism of Crizotinib caused by Naloxegol mediated inhibition of CYP450 enzyme. Large intestine motility disorder [DB32] [77]
Pemigatinib DM819JF Major Decreased metabolism of Crizotinib caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [77]
Glycerol phenylbutyrate DMDGRQO Moderate Increased metabolism of Crizotinib caused by Glycerol phenylbutyrate mediated induction of CYP450 enzyme. Liver disease [DB90-DB9Z] [73]
Artesunate DMR27C8 Moderate Decreased clearance of Crizotinib due to the transporter inhibition by Artesunate. Malaria [1F40-1F45] [71]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Crizotinib and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [100]
Idelalisib DM602WT Major Decreased metabolism of Crizotinib caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [71]
GDC-0199 DMH0QKA Major Decreased metabolism of Crizotinib caused by GDC-0199 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [71]
IPI-145 DMWA24P Moderate Decreased metabolism of Crizotinib caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [101]
Acalabrutinib DM7GCVW Major Decreased metabolism of Crizotinib caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [102]
Ibrutinib DMHZCPO Major Decreased metabolism of Crizotinib caused by Ibrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [103]
Ponatinib DMYGJQO Moderate Decreased metabolism of Crizotinib caused by Ponatinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [104]
Arry-162 DM1P6FR Moderate Decreased clearance of Crizotinib due to the transporter inhibition by Arry-162. Melanoma [2C30] [71]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Crizotinib and Vemurafenib. Melanoma [2C30] [96]
Selumetinib DMC7W6R Major Decreased metabolism of Crizotinib caused by Selumetinib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [105]
LGX818 DMNQXV8 Major Decreased metabolism of Crizotinib caused by LGX818 mediated inhibition of CYP450 enzyme. Melanoma [2C30] [106]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Crizotinib caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [77]
Ubrogepant DM749I3 Moderate Decreased metabolism of Crizotinib caused by Ubrogepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [107]
Rimegepant DMHOAUG Moderate Decreased metabolism of Crizotinib caused by Rimegepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [108]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Crizotinib and Siponimod. Multiple sclerosis [8A40] [71]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Crizotinib and Fingolimod. Multiple sclerosis [8A40] [96]
Ozanimod DMT6AM2 Major Increased risk of prolong QT interval by the combination of Crizotinib and Ozanimod. Multiple sclerosis [8A40] [74]
Deflazacort DMV0RNS Major Decreased metabolism of Crizotinib caused by Deflazacort mediated inhibition of CYP450 enzyme. Muscular dystrophy [8C70] [77]
Fedratinib DM4ZBK6 Minor Decreased metabolism of Crizotinib caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [74]
Ruxolitinib DM7Q98D Minor Decreased metabolism of Crizotinib caused by Ruxolitinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [77]
Entrectinib DMMPTLH Major Decreased metabolism of Crizotinib caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [71]
S-297995 DM26IH8 Moderate Decreased metabolism of Crizotinib caused by S-297995 mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [77]
Olaparib DM8QB1D Major Decreased metabolism of Crizotinib caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [71]
Rucaparib DM9PVX8 Major Increased risk of prolong QT interval by the combination of Crizotinib and Rucaparib. Ovarian cancer [2C73] [74]
Triclabendazole DMPWGBR Major Increased risk of prolong QT interval by the combination of Crizotinib and Triclabendazole. Parasitic worm infestation [1F90] [74]
Istradefylline DM20VSK Moderate Decreased metabolism of Crizotinib caused by Istradefylline mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [74]
Abametapir DM2RX0I Moderate Decreased metabolism of Crizotinib caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [109]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Crizotinib and Macimorelin. Pituitary gland disorder [5A60-5A61] [110]
Lefamulin DME6G97 Major Decreased metabolism of Crizotinib caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [111]
Enzalutamide DMGL19D Major Increased metabolism of Crizotinib caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [71]
Relugolix DMK7IWL Major Increased risk of prolong QT interval by the combination of Crizotinib and Relugolix. Prostate cancer [2C82] [112]
Darolutamide DMV7YFT Minor Decreased metabolism of Crizotinib caused by Darolutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [113]
Riociguat DMXBLMP Moderate Decreased metabolism of Crizotinib caused by Riociguat mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [71]
Upadacitinib DM32B5U Moderate Decreased metabolism of Crizotinib caused by Upadacitinib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [114]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Crizotinib caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [115]
LDE225 DMM9F25 Major Decreased metabolism of Crizotinib caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [116]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Crizotinib caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [77]
Larotrectinib DM26CQR Moderate Decreased clearance of Crizotinib due to the transporter inhibition by Larotrectinib. Solid tumour/cancer [2A00-2F9Z] [71]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Crizotinib and LEE011. Solid tumour/cancer [2A00-2F9Z] [74]
Pitolisant DM8RFNJ Major Increased risk of prolong QT interval by the combination of Crizotinib and Pitolisant. Somnolence [MG42] [74]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Crizotinib caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [117]
Lenvatinib DMB1IU4 Major Increased risk of prolong QT interval by the combination of Crizotinib and Lenvatinib. Thyroid cancer [2D10] [74]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Crizotinib and Cabozantinib. Thyroid cancer [2D10] [74]
Elagolix DMB2C0E Moderate Increased metabolism of Crizotinib caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [73]
Fluticasone DMGCSVF Moderate Decreased metabolism of Crizotinib caused by Fluticasone mediated inhibition of CYP450 enzyme. Vasomotor/allergic rhinitis [CA08] [71]
Betrixaban DM2C4RF Moderate Decreased clearance of Crizotinib due to the transporter inhibition by Betrixaban. Venous thromboembolism [BD72] [118]
⏷ Show the Full List of 95 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Ammonia E00007 222 Alkalizing agent
Calcium hydrogenphosphate E00294 24441 Diluent
Eisenoxyd E00585 56841934 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Magnesium stearate E00208 11177 lubricant
Potassium hydroxide E00233 14797 Alkalizing agent
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
⏷ Show the Full List of 9 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Crizotinib 200 mg capsule 200 mg Oral Capsule Oral
Crizotinib 250 mg capsule 250 mg Oral Capsule Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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).
2 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
3 BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs
4 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
6 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
8 Met tyrosine kinase inhibitor, PF-2341066, suppresses growth and invasion of nasopharyngeal carcinoma.Drug Des Devel Ther. 2015 Aug 26;9:4897-907.
9 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
10 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.
11 Crizotinib for the treatment of non-small-cell lung cancer. Am J Health Syst Pharm. 2013 Jun 1;70(11):943-7.
12 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
13 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
14 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
15 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
16 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
17 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
18 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
19 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
20 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
21 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
22 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
23 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
24 Drug Interactions Flockhart Table
25 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
26 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
27 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
28 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
29 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
30 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
31 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
32 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
33 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
34 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
35 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
36 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
37 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
38 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
39 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
40 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
41 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
42 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
43 FDA Drug Development and Drug Interactions
44 LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001 Jun;120(7):1689-99.
45 Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.
46 Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos. 2011 Jun;39(6):1047-53.
47 Relevance of conserved lysine and arginine residues in transmembrane helices for the transport activity of organic anion transporting polypeptide 1B3. Br J Pharmacol. 2010 Feb 1;159(3):698-708.
48 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
49 Clinical pipeline report, company report or official report of Exelixis (2011).
50 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
51 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
52 Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209.
53 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. (Target id: 1815).
54 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
55 Beperminogene perplasmid for the treatment of critical limb ischemia. Expert Rev Cardiovasc Ther. 2014 Oct;12(10):1145-56.
56 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: 7948).
57 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
58 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
59 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
60 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
61 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: 7397).
62 CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90.
63 PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models. Cancer Cell. 2015 Jul 13;28(1):70-81.
64 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
65 Treatment of ALK-positive non-small cell lung cancer. Arch Pathol Lab Med. 2012 Oct;136(10):1201-4.
66 Clinical pipeline report, company report or official report of AnHeart Therapeutics.
67 National Cancer Institute Drug Dictionary (drug id 766123).
68 RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
69 Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751.
70 Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
71 Cerner Multum, Inc. "Australian Product Information.".
72 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
73 Cerner Multum, Inc. "Canadian Product Information.".
74 Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
75 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
76 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
77 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
78 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
79 Product Information. Olinvyk (oliceridine). Trevena Inc, Chesterbrook, PA.
80 Wohlt PD, Zheng L, Gunderson S, Balzar SA, Johnson BD, Fish JT "Recommendations for the use of medications with continuous enteral nutrition." Am J Health Syst Pharm 66 (2009): 1438-67. [PMID: 19667002]
81 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
82 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
83 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
84 Product Information. Talzenna (talazoparib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
85 Abbas R, Hug BA, Leister C, Burns J, Sonnichsen D "Pharmacokinetics of oral neratinib during co-administration of ketoconazole in healthy subjects." Br J Clin Pharmacol 71 (2011): 522-7. [PMID: 21395644]
86 Product Information. Verzenio (abemaciclib). Lilly, Eli and Company, Indianapolis, IN.
87 Product Information. Opsumit (macitentan). Actelion Pharmaceuticals US Inc, South San Francisco, CA.
88 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
89 Product Information. Ofev (nintedanib). Boehringer Ingelheim, Ridgefield, CT.
90 Product Information. Rexulti (brexpiprazole). Otsuka American Pharmaceuticals Inc, Rockville, MD.
91 Product Information. Aliqopa (copanlisib). Bayer Pharmaceutical Inc, West Haven, CT.
92 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
93 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
94 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
95 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
96 Canadian Pharmacists Association.
97 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
98 Product Information. Belsomra (suvorexant). Merck & Company Inc, Whitehouse Station, NJ.
99 Product Information. Hetlioz (tasimelteon). Vanda Pharmaceuticals Inc, Rockville, MD.
100 Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
101 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
102 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
103 Product Information. Imbruvica (ibrutinib). Pharmacyclics Inc, Sunnyvale, CA.
104 Product Information. Iclusig (ponatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
105 Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
106 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
107 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
108 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
109 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
110 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
111 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
112 Product Information. Orgovyx (relugolix). Myovant Sciences, Inc., Brisbane, CA.
113 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
114 Product Information. Rinvoq (upadacitinib). AbbVie US LLC, North Chicago, IL.
115 Product Information. Oxbryta (voxelotor). Global Blood Therapeutics, Inc., South San Francisco, CA.
116 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
117 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
118 Product Information. Bevyxxa (betrixaban). Portola Pharmaceuticals, South San Francisco, CA.