Details of the Drug

General Information of Drug (ID: DM15F0X)

Drug Name
Gefitinib
Synonyms
Gefitini; IRE; Iressa; Irressat; Gefitinib [USAN]; ZD 1839; ZD1839; Iressa (TN); Iressa(TM); ZD-1839; CU-00000000396-1; Gefitinib,Iressa, ZD1839; Gefitinib (JAN/USAN/INN); ZD-1839, Iressa, Gefitinib; N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamide; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine; N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; 4-(3'-Chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline; 6-(3-morpholinopropoxy)-N-(3-chloro-4-fluorophenyl)-7-methoxyquinazolin-4-amine
Indication
Disease Entry ICD 11 Status REF
Colon adenocarcinoma N.A. Approved [1]
Glioblastoma 2A00 Approved [1]
Lung cancer 2C25.0 Approved [1]
Non-small-cell lung cancer 2C25.Y Approved [1]
Rectal adenocarcinoma 2B92 Approved [1]
Rectum mucinous adenocarcinoma N.A. Approved [1]
Solid tumour/cancer 2A00-2F9Z Approved [2]
Head and neck cancer 2D42 Phase 3 [2]
Urethral cancer 2C93 Phase 2 [2]
Colon cancer 2B90.Z Investigative [1]
Colon mucinous adenocarcinoma N.A. Investigative [1]
⏷ Show the Full List of Indication(s)
Therapeutic Class
Anticancer Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 446.9
Logarithm of the Partition Coefficient (xlogp) 4.1
Rotatable Bond Count (rotbonds) 8
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 8
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Bioavailability
60% of drug becomes completely available to its intended biological destination(s) [4]
Clearance
The clearance of drug is 595 mL/min []
Elimination
2% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 48 hours [5]
Metabolism
The drug is metabolized via the hepatic []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 8 micromolar/kg/day [6]
Unbound Fraction
The unbound fraction of drug in plasma is 0.089% [5]
Vd
The volume of distribution (Vd) of drug is 1400 L []
Water Solubility
The ability of drug to dissolve in water is measured as 0.0017 mg/mL [3]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Diarrhea rs2231142 ABCG2 OTW8V2V1 [7]
Chemical Identifiers
Formula
C22H24ClFN4O3
IUPAC Name
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
Canonical SMILES
COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
InChI
InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)
InChIKey
XGALLCVXEZPNRQ-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
123631
ChEBI ID
CHEBI:49668
CAS Number
184475-35-2
DrugBank ID
DB00317
TTD ID
D09XZB
VARIDT ID
DR00423
INTEDE ID
DR0764
ACDINA ID
D00299
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [8]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [9]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [10]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [10]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [11]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [12]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [13]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [12]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
14-3-3 protein sigma (SFN) OTLJCZ1U 1433S_HUMAN Gene/Protein Processing [14]
Adenosine receptor A1 (ADORA1) OTI7X39E AA1R_HUMAN Gene/Protein Processing [14]
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Protein Interaction/Cellular Processes [15]
Amphiregulin (AREG) OTJFOR67 AREG_HUMAN Drug Response [16]
Aurora kinase A (AURKA) OTMX0HYT AURKA_HUMAN Drug Response [17]
Autophagy protein 5 (ATG5) OT4T5SMS ATG5_HUMAN Gene/Protein Processing [18]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Gene/Protein Processing [19]
Bcl-2-like protein 11 (BCL2L11) OTNQQWFJ B2L11_HUMAN Drug Response [20]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [21]
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_HUMAN Drug Response [7]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Colon adenocarcinoma
ICD Disease Classification
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Epidermal growth factor receptor (EGFR) DTT EGFR 1.04E-65 -0.89 -1.53
P-glycoprotein 1 (ABCB1) DTP P-GP 3.61E-73 -1.15E+00 -1.66E+00
Breast cancer resistance protein (ABCG2) DTP BCRP 1.46E-65 -1.41E+00 -1.41E+00
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 4.86E-01 -5.39E-02 -2.84E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.12E-01 9.67E-03 3.43E-02
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 2.56E-19 -3.06E-01 -6.18E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 6.51E-02 -2.38E-02 -9.58E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.87E-03 -6.67E-02 -2.12E-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 Gefitinib
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Larotrectinib DM26CQR Moderate Decreased metabolism of Gefitinib caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [22]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [23]
Armodafinil DMGB035 Minor Increased metabolism of Gefitinib caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [24]
LEE011 DMMX75K Moderate Decreased metabolism of Gefitinib caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [22]
Epirubicin DMPDW6T Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Epirubicin. Solid tumour/cancer [2A00-2F9Z] [25]
Coadministration of a Drug Treating the Disease Different from Gefitinib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [25]
Thioguanine DM7NKEV Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Thioguanine. Acute myeloid leukaemia [2A60] [26]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Gefitinib caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [22]
Arn-509 DMT81LZ Moderate Increased metabolism of Gefitinib caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [22]
Mitotane DMU1GX0 Moderate Increased metabolism of Gefitinib caused by Mitotane mediated induction of CYP450 enzyme. Adrenal cancer [2D11] [22]
Donepezil DMIYG7Z Minor Decreased metabolism of Gefitinib caused by Donepezil mediated inhibition of CYP450 enzyme. Alzheimer disease [8A20] [27]
Dronedarone DMA8FS5 Moderate Decreased metabolism of Gefitinib caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [22]
Nifedipine DMSVOZT Moderate Decreased metabolism of Gefitinib caused by Nifedipine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [22]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [28]
Methylphenobarbital DMDSWAG Moderate Increased metabolism of Gefitinib caused by Methylphenobarbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [22]
Voriconazole DMAOL2S Moderate Decreased metabolism of Gefitinib caused by Voriconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [22]
Posaconazole DMUL5EW Moderate Decreased metabolism of Gefitinib caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [22]
Zafirlukast DMHNQOG Moderate Decreased metabolism of Gefitinib caused by Zafirlukast mediated inhibition of CYP450 enzyme. Asthma [CA23] [22]
Ciprofloxacin XR DM2NLS9 Moderate Decreased metabolism of Gefitinib caused by Ciprofloxacin XR mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [22]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Gefitinib caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [22]
Clarithromycin DM4M1SG Moderate Decreased metabolism of Gefitinib caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [22]
Chloramphenicol DMFXEWT Moderate Decreased metabolism of Gefitinib caused by Chloramphenicol mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [22]
Rabeprazole DMMZXIW Moderate Decreased absorption of Gefitinib due to altered gastric pH caused by Rabeprazole. Bacterial infection [1A00-1C4Z] [29]
Telithromycin DMZ4P3A Moderate Decreased metabolism of Gefitinib caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [22]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Gefitinib and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [30]
Talazoparib DM1KS78 Moderate Decreased clearance of Gefitinib due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [31]
Lapatinib DM3BH1Y Moderate Decreased metabolism of Gefitinib caused by Lapatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [22]
Tucatinib DMBESUA Moderate Decreased metabolism of Gefitinib caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [22]
Phenylbutazone DMAYL0T Moderate Increased metabolism of Gefitinib caused by Phenylbutazone mediated induction of CYP450 enzyme. Chronic pain [MG30] [22]
Mifepristone DMGZQEF Moderate Decreased metabolism of Gefitinib caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [25]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Gefitinib caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [22]
Aminoglutethimide DMWFHMZ Moderate Increased metabolism of Gefitinib caused by Aminoglutethimide mediated induction of CYP450 enzyme. Cushing syndrome [5A70] [22]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Gefitinib caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [22]
MK-8228 DMOB58Q Moderate Decreased metabolism of Gefitinib caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [22]
Aprepitant DM053KT Moderate Decreased metabolism of Gefitinib caused by Aprepitant mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [32]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Gefitinib caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [22]
Duloxetine DM9BI7M Moderate Decreased metabolism of Gefitinib caused by Duloxetine mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [33]
Griseofulvin DMK54YG Moderate Increased metabolism of Gefitinib caused by Griseofulvin mediated induction of CYP450 enzyme. Dermatophytosis [1F28] [22]
Primidone DM0WX6I Moderate Increased metabolism of Gefitinib caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [22]
Felbamate DM1V5ZS Moderate Increased metabolism of Gefitinib caused by Felbamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [22]
Oxcarbazepine DM5PU6O Moderate Increased metabolism of Gefitinib caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [22]
Cenobamate DM8KLU9 Moderate Increased metabolism of Gefitinib caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [22]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Gefitinib caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [22]
Phenobarbital DMXZOCG Moderate Increased metabolism of Gefitinib caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [22]
Carbamazepine DMZOLBI Moderate Increased metabolism of Gefitinib caused by Carbamazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [22]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Cannabidiol. Epileptic encephalopathy [8A62] [23]
Timolol DM3NXRU Moderate Decreased metabolism of Gefitinib caused by Timolol mediated inhibition of CYP450 enzyme. Essential hypertension [BA00] [34]
Tazemetostat DMWP1BH Moderate Increased metabolism of Gefitinib caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [22]
Tolterodine DMSHPW8 Minor Decreased metabolism of Gefitinib caused by Tolterodine mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [35]
Darifenacin DMWXLYZ Moderate Decreased metabolism of Gefitinib caused by Darifenacin mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [36]
Itraconazole DMCR1MV Moderate Decreased metabolism of Gefitinib caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [22]
Miconazole DMPMYE8 Moderate Decreased metabolism of Gefitinib caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [22]
Ketoconazole DMPZI3Q Moderate Decreased metabolism of Gefitinib caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [22]
Dexlansoprazole DM1DBV5 Moderate Decreased absorption of Gefitinib due to altered gastric pH caused by Dexlansoprazole. Gastro-oesophageal reflux disease [DA22] [29]
Omeprazole DM471KJ Moderate Decreased absorption of Gefitinib due to altered gastric pH caused by Omeprazole. Gastro-oesophageal reflux disease [DA22] [29]
Nizatidine DMGFV3Z Moderate Decreased absorption of Gefitinib due to altered gastric pH caused by Nizatidine. Gastro-oesophageal reflux disease [DA22] [29]
Cimetidine DMH61ZB Moderate Decreased absorption of Gefitinib due to altered gastric pH caused by Cimetidine. Gastro-oesophageal reflux disease [DA22] [29]
Sulfinpyrazone DMEV954 Moderate Increased metabolism of Gefitinib caused by Sulfinpyrazone mediated induction of CYP450 enzyme. Gout [FA25] [22]
Boceprevir DMBSHMF Moderate Decreased metabolism of Gefitinib caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [22]
Telaprevir DMMRV29 Moderate Decreased metabolism of Gefitinib caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [22]
Isoniazid DM5JVS3 Moderate Decreased metabolism of Gefitinib caused by Isoniazid mediated inhibition of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [22]
Rifampin DMA8J1G Moderate Increased metabolism of Gefitinib caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [22]
Rifapentine DMCHV4I Moderate Increased metabolism of Gefitinib caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [22]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Brentuximab vedotin. Hodgkin lymphoma [2B30] [37]
Delavirdine DM3NF5G Moderate Decreased metabolism of Gefitinib caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Fosamprenavir DM4W9B3 Moderate Decreased metabolism of Gefitinib caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Gefitinib caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Efavirenz DMC0GSJ Moderate Increased metabolism of Gefitinib caused by Efavirenz mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Saquinavir DMG814N Moderate Decreased metabolism of Gefitinib caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Etravirine DMGV8QU Moderate Increased metabolism of Gefitinib caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Amprenavir DMLMXE0 Moderate Decreased metabolism of Gefitinib caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Darunavir DMN3GCH Moderate Decreased metabolism of Gefitinib caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Atazanavir DMSYRBX Moderate Decreased metabolism of Gefitinib caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Ritonavir DMU764S Moderate Decreased metabolism of Gefitinib caused by Ritonavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [22]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Gefitinib and Mipomersen. Hyper-lipoproteinaemia [5C80] [38]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Gefitinib and Teriflunomide. Hyper-lipoproteinaemia [5C80] [39]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Gefitinib and BMS-201038. Hyper-lipoproteinaemia [5C80] [40]
Verapamil DMA7PEW Moderate Decreased metabolism of Gefitinib caused by Verapamil mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [22]
Diltiazem DMAI7ZV Moderate Decreased metabolism of Gefitinib caused by Diltiazem mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [22]
Conivaptan DM1V329 Moderate Decreased metabolism of Gefitinib caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [22]
Givosiran DM5PFIJ Moderate Decreased metabolism of Gefitinib caused by Givosiran mediated inhibition of CYP450 enzyme. Inborn porphyrin/heme metabolism error [5C58] [41]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Gefitinib caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [22]
Amobarbital DM0GQ8N Moderate Increased metabolism of Gefitinib caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [22]
Methotrexate DM2TEOL Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Methotrexate. Leukaemia [2A60-2B33] [23]
Crizotinib DM4F29C Moderate Decreased metabolism of Gefitinib caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [22]
Brigatinib DM7W94S Moderate Increased metabolism of Gefitinib caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [42]
Ceritinib DMB920Z Moderate Decreased metabolism of Gefitinib caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [22]
PF-06463922 DMKM7EW Moderate Increased metabolism of Gefitinib caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [22]
Dacomitinib DMOH8VY Moderate Decreased metabolism of Gefitinib caused by Dacomitinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [43]
Selpercatinib DMZR15V Moderate Decreased metabolism of Gefitinib caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [22]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [44]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Idelalisib. Mature B-cell leukaemia [2A82] [45]
IPI-145 DMWA24P Moderate Decreased metabolism of Gefitinib caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [22]
Clofarabine DMCVJ86 Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Clofarabine. Mature B-cell lymphoma [2A85] [46]
Arry-162 DM1P6FR Moderate Decreased clearance of Gefitinib due to the transporter inhibition by Arry-162. Melanoma [2C30] [25]
Vemurafenib DM62UG5 Moderate Increased metabolism of Gefitinib caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [22]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Gefitinib caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [22]
Danazol DML8KTN Moderate Decreased metabolism of Gefitinib caused by Danazol mediated inhibition of CYP450 enzyme. Menstrual cycle bleeding disorder [GA20] [22]
Ubrogepant DM749I3 Moderate Decreased clearance of Gefitinib due to the transporter inhibition by Ubrogepant. Migraine [8A80] [47]
Rimegepant DMHOAUG Moderate Decreased clearance of Gefitinib due to the transporter inhibition by Rimegepant. Migraine [8A80] [48]
Exjade DMHPRWG Moderate Decreased metabolism of Gefitinib caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [49]
Rifabutin DM1YBHK Moderate Increased metabolism of Gefitinib caused by Rifabutin mediated induction of CYP450 enzyme. Mycobacterium infection [1B10-1B21] [22]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Gefitinib caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [22]
Nilotinib DM7HXWT Moderate Decreased metabolism of Gefitinib caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [22]
Imatinib DM7RJXL Moderate Decreased metabolism of Gefitinib caused by Imatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [22]
Dasatinib DMJV2EK Moderate Decreased metabolism of Gefitinib caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [22]
Omacetaxine mepesuccinate DMPU2WX Moderate Additive immunosuppressive effects by the combination of Gefitinib and Omacetaxine mepesuccinate. Myeloproliferative neoplasm [2A20] [50]
Modafinil DMYILBE Minor Increased metabolism of Gefitinib caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [24]
Netupitant DMEKAYI Moderate Decreased metabolism of Gefitinib caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [22]
Entrectinib DMMPTLH Moderate Decreased metabolism of Gefitinib caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [22]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Gefitinib caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [22]
Codeine DMJX6ZG Moderate Decreased metabolism of Gefitinib caused by Codeine mediated inhibition of CYP450 enzyme. Pain [MG30-MG3Z] [51]
Abametapir DM2RX0I Moderate Decreased metabolism of Gefitinib caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [52]
Ranitidine DM0GUSX Moderate Decreased absorption of Gefitinib due to altered gastric pH caused by Ranitidine. Peptic ulcer [DA61] [29]
Esomeprazole DM7BN0X Moderate Decreased absorption of Gefitinib due to altered gastric pH caused by Esomeprazole. Peptic ulcer [DA61] [29]
Famotidine DMRL3AB Moderate Decreased absorption of Gefitinib due to altered gastric pH caused by Famotidine. Peptic ulcer [DA61] [29]
Lefamulin DME6G97 Moderate Decreased metabolism of Gefitinib caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [53]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Gefitinib caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [22]
Enzalutamide DMGL19D Moderate Increased metabolism of Gefitinib caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [22]
Bicalutamide DMZMSPF Moderate Decreased metabolism of Gefitinib caused by Bicalutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [22]
Verteporfin DMIY6DB Moderate Increased risk of photosensitivity reactions by the combination of Gefitinib and Verteporfin. Psoriasis [EA90] [23]
Bosentan DMIOGBU Moderate Increased metabolism of Gefitinib caused by Bosentan mediated induction of CYP450 enzyme. Pulmonary hypertension [BB01] [22]
Riociguat DMXBLMP Moderate Decreased metabolism of Gefitinib caused by Riociguat mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [39]
Dexamethasone DMMWZET Moderate Increased metabolism of Gefitinib caused by Dexamethasone mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [22]
Nafcillin DMN9RPO Moderate Increased metabolism of Gefitinib caused by Nafcillin mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [22]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Gefitinib and Leflunomide. Rheumatoid arthritis [FA20] [39]
Thioridazine DM35M8J Major Decreased metabolism of Gefitinib caused by Thioridazine mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [54]
Aripiprazole DM3NUMH Moderate Decreased metabolism of Gefitinib caused by Aripiprazole mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [55]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Gefitinib caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [22]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Gefitinib caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [23]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Gefitinib and Naltrexone. Substance abuse [6C40] [56]
Fostamatinib DM6AUHV Moderate Decreased clearance of Gefitinib due to the transporter inhibition by Fostamatinib. Thrombocytopenia [3B64] [57]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Gefitinib due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [58]
Elagolix DMB2C0E Moderate Increased metabolism of Gefitinib caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [22]
Amiodarone DMUTEX3 Moderate Decreased metabolism of Gefitinib caused by Amiodarone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [22]
⏷ Show the Full List of 130 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
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Carmellose sodium E00625 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 300 E00651 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
⏷ Show the Full List of 8 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Gefitinib 250 mg tablet 250 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Gefitinib FDA Label
2 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: 4941).
3 BDDCS applied to over 900 drugs
4 Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
5 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
6 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
7 Pharmacogenetics of ABCG2 and adverse reactions to gefitinib. J Natl Cancer Inst. 2006 Dec 6;98(23):1739-42.
8 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
9 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.
10 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
11 Gefitinib-phenytoin interaction is not correlated with the C-erythromycin breath test in healthy male volunteers. Br J Clin Pharmacol. 2009 Aug;68(2):226-37.
12 Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res. 2007 Jun 15;13(12):3731-7.
13 Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol. Clin Pharmacokinet. 2005;44(10):1067-81.
14 Identification of genes linked to gefitinib treatment in prostate cancer cell lines with or without resistance to androgen: a clue to application of gefitinib to hormone-resistant prostate cancer. Oncol Rep. 2006 Jun;15(6):1453-60.
15 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.
16 Prediction of sensitivity of advanced non-small cell lung cancers to gefitinib (Iressa, ZD1839). Hum Mol Genet. 2004 Dec 15;13(24):3029-43. doi: 10.1093/hmg/ddh331. Epub 2004 Oct 20.
17 Aurora-A promotes gefitinib resistance via a NF-B signaling pathway in p53 knockdown lung cancer cells. Biochem Biophys Res Commun. 2011 Feb 11;405(2):168-72. doi: 10.1016/j.bbrc.2011.01.001. Epub 2011 Jan 7.
18 EGFR tyrosine kinase inhibitors activate autophagy as a cytoprotective response in human lung cancer cells. PLoS One. 2011;6(6):e18691. doi: 10.1371/journal.pone.0018691. Epub 2011 Jun 2.
19 Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. doi: 10.1016/j.taap.2017.09.017. Epub 2017 Sep 21.
20 BIM induction of apoptosis triggered by EGFR-sensitive and resistance cell lines of non-small-cell lung cancer. Med Oncol. 2011 Jun;28(2):572-7. doi: 10.1007/s12032-010-9470-y. Epub 2010 Mar 17.
21 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
22 Li J, Zhao M, He P, Hidalgo M, Baker SD "Differential metabolism of gefitinib and erlotinib by human cytochrome p450 enzymes." Clin Cancer Res 13 (2007): 3731-7. [PMID: 17575239]
23 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
24 Doherty MM, Charman WN "The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism?" Clin Pharmacokinet 41 (2002): 235-53. [PMID: 11978143]
25 Cerner Multum, Inc. "Australian Product Information.".
26 Product Information. Aubagio (teriflunomide). Genzyme Corporation, Cambridge, MA.
27 Product Information. Aricept (donepezil). Pfizer US Pharmaceuticals, New York, NY.
28 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
29 Product Information. Iressa (gefitinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
30 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
31 Product Information. Talzenna (talazoparib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
32 Charasson V, Haaz MC, Robert J "Determination of Drug Interactions Occurring with the Metabolic Pathways of Irinotecan." Drug Metab Dispos 30 (2002): 731-733. [PMID: 12019202]
33 Product Information. Cymbalta (duloxetine). Lilly, Eli and Company, Indianapolis, IN.
34 Edeki TI, He HB, Wood AJJ "Pharmacogenetic explanation for excessive beta-blockade following timolol eye drops: potential for oral-ophthalmic drug interaction." JAMA 274 (1995): 1611-3. [PMID: 7474246]
35 Brynne N, Svanstrom C, AbergWistedt A, Hallen B, Bertilsson L "Fluoxetine inhibits the metabolism of tolterodin-pharmacokinetic implications and proposed clinical relevance." Br J Clin Pharmacol 48 (1999): 553-63. [PMID: 10583026]
36 Product Information. Enablex (darifenacin). Novartis Pharmaceuticals, East Hanover, NJ.
37 Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA.
38 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
39 Canadian Pharmacists Association.
40 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
41 Product Information. Givlaari (givosiran). Alnylam Pharmaceuticals, Cambridge, MA.
42 Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
43 Product Information. Vizimpro (dacomitinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
44 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]
45 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
46 Product Information. Clolar (clofarabine). sanofi-aventis, Bridgewater, NJ.
47 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
48 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
49 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
50 Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
51 Caraco Y, Sheller J, Wood AJJ "Impact of ethnic origin and quinidine coadministration on codeine's disposition and pharmacodynamic effects." J Pharmacol Exp Ther 290 (1999): 413-22. [PMID: 10381807]
52 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
53 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
54 Abernethy DR, Greenblatt DJ, Steel K, Shader RI "Impairment of hepatic drug oxidation by propoxyphene." Ann Intern Med 97 (1982): 223-4. [PMID: 7103282]
55 Product Information. Abilify (aripiprazole). Bristol-Myers Squibb, Princeton, NJ.
56 Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
57 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
58 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".