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Identification
NameGefitinib
Accession NumberDB00317  (APRD00997, DB07998)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionGefitinib (originally coded ZD1839) is a drug used in the treatment of certain types of cancer. Acting in a similar manner to erlotinib (marketed as Tarceva), gefitinib selectively targets the mutant proteins in malignant cells. It is marketed by AstraZeneca under the trade name Iressa. [Wikipedia]
Structure
Thumb
Synonyms
4-(3'-chloro-4'-Fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline
Gefitinib
Iressa
N-(3-chloro-4-Fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamine
ZD 1839
External Identifiers
  • ZD1839
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
IressaTablet250 mgOralAstrazeneca Canada Inc2003-12-17Not applicableCanada
IressaTablet, film coated250 mgOralAstra Zeneca Ab2009-06-24Not applicableEu
IressaTablet, film coated250 mgOralAstra Zeneca Ab2009-06-24Not applicableEu
IressaTablet, coated250 mg/1OralAstra Zeneca Pharmaceuticals Lp2015-07-13Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIS65743JHBS
CAS number184475-35-2
WeightAverage: 446.902
Monoisotopic: 446.152096566
Chemical FormulaC22H24ClFN4O3
InChI KeyXGALLCVXEZPNRQ-UHFFFAOYSA-N
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)
IUPAC Name
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine
SMILES
COC1=C(OCCCN2CCOCC2)C=C2C(NC3=CC(Cl)=C(F)C=C3)=NC=NC2=C1
Pharmacology
IndicationFor the continued treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of either platinum-based or docetaxel chemotherapies.
Structured Indications
PharmacodynamicsGefitinib inhibits the intracellular phosphorylation of numerous tyrosine kinases associated with transmembrane cell surface receptors, including the tyrosine kinases associated with the epidermal growth factor receptor (EGFR-TK). EGFR is expressed on the cell surface of many normal cells and cancer cells.
Mechanism of actionGefitinib inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme. Thus the function of the EGFR tyrosine kinase in activating the Ras signal transduction cascade is inhibited; and malignant cells are inhibited. Gefitinib is the first selective inhibitor of the EGFR tyrosine kinase which is also referred to as Her1 or ErbB-1. EGFR is overexpressed in the cells of certain types of human carcinomas - for example in lung and breast cancers. Overexpression leads to inappropriate activation of the apoptotic Ras signal transduction cascade, eventually leading to uncontrolled cell proliferation.
TargetKindPharmacological actionActionsOrganismUniProt ID
Epidermal growth factor receptorProteinyes
antagonist
HumanP00533 details
Related Articles
AbsorptionAbsorbed slowly after oral administration with a mean bioavailability of 60%. Peak plasma levels occurs 3-7 hours post-administration. Food does not affect the bioavailability of gefitinib.
Volume of distribution
  • 1400 L [IV administration]
Protein binding90% primarily to serum albumin and alpha 1-acid glycoproteins (independent of drug concentrations).
Metabolism

Primarily hepatic via CYP3A4. Three sites of biotransformation have been identified: metabolism of the N-propoxymorpholino-group, demethylation of the methoxy-substituent on the quinazoline, and oxidative defluorination of the halogenated phenyl group.

Route of eliminationElimination is by metabolism (primarily CYP3A4) and excretion in feces. Excretion is predominantly via the feces (86%), with renal elimination of drug and metabolites accounting for less than 4% of the administered dose.
Half life48 hours [IV administration]
Clearance
  • 595 mL/min [IV administration]
ToxicityThe acute toxicity of gefitinib up to 500 mg in clinical studies has been low. In non-clinical studies, a single dose of 12,000 mg/m2 (about 80 times the recommended clinical dose on a mg/m2 basis) was lethal to rats. Half this dose caused no mortality in mice. Symptoms of overdose include diarrhea and skin rash.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Gefitinib Action PathwayDrug actionSMP00473
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Epidermal growth factor receptor
Gene symbol: EGFR
UniProt: P00533
Not AvailableG719A/C OR (L858R and L861Q)Not AvailableAssociated with enhanced activation of the EGFR tyrosine kinase in patients with non-small cell lung cancer (NSCLC) recieving tyrosine kinase inhibitor therapy.15118073
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
ATP-binding cassette sub-family G member 2
Gene symbol: ABCG2
UniProt: Q9UNQ0
rs2231142 Not AvailableA AlleleDiarrhea17148776
ATP-binding cassette sub-family G member 2
Gene symbol: ABCG2
UniProt: Q9UNQ0
rs2231142 Not AvailableA alleleIn non-small lung cancer patients, those that are heterozygous (ABCG2 421C>A) have a higher risk of diarrhea.17148776
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Gefitinib can be increased when it is combined with Abiraterone.Approved
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Gefitinib.Approved
AcenocoumarolGefitinib may increase the anticoagulant activities of Acenocoumarol.Approved
AcetaminophenThe serum concentration of Gefitinib can be increased when it is combined with Acetaminophen.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Gefitinib.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Gefitinib.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Gefitinib.Approved
AlbendazoleThe serum concentration of Gefitinib can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Gefitinib can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Gefitinib can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Gefitinib can be increased when it is combined with Alfentanil.Approved, Illicit
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Gefitinib.Approved, Investigational
Aluminum hydroxideThe serum concentration of Gefitinib can be decreased when it is combined with Aluminum hydroxide.Approved
Aluminum phosphateThe serum concentration of Gefitinib can be decreased when it is combined with Aluminum phosphate.Approved
AmantadineThe serum concentration of Gefitinib can be increased when it is combined with Amantadine.Approved
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Gefitinib.Approved, Investigational
Aminohippuric acidThe serum concentration of Gefitinib can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe metabolism of Gefitinib can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Gefitinib can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Gefitinib can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Gefitinib can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Gefitinib can be increased when it is combined with Amsacrine.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Gefitinib.Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Gefitinib.Approved
AprepitantThe serum concentration of Gefitinib can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Gefitinib.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Gefitinib.Approved, Investigational
ArtemetherThe metabolism of Gefitinib can be decreased when combined with Artemether.Approved
AsenapineThe serum concentration of Gefitinib can be decreased when it is combined with Asenapine.Approved
AstemizoleThe serum concentration of Gefitinib can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Gefitinib can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Gefitinib can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Gefitinib can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Gefitinib can be increased when it is combined with Atorvastatin.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Gefitinib.Approved, Investigational
AzelastineThe serum concentration of Gefitinib can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Gefitinib can be increased when it is combined with Azithromycin.Approved
BenzocaineThe serum concentration of Gefitinib can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Gefitinib can be increased when it is combined with Bepridil.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Gefitinib.Approved, Vet Approved
BetaxololThe metabolism of Gefitinib can be decreased when combined with Betaxolol.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Gefitinib.Approved, Investigational
BexaroteneThe serum concentration of Gefitinib can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Gefitinib can be increased when it is combined with Biperiden.Approved
Bismuth SubcitrateThe serum concentration of Gefitinib can be decreased when it is combined with Bismuth Subcitrate.Approved
BoceprevirThe metabolism of Gefitinib can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Gefitinib can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Gefitinib can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Gefitinib.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Gefitinib.Approved
BromocriptineThe serum concentration of Gefitinib can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Gefitinib can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Gefitinib can be decreased when combined with Bupropion.Approved
BuspironeThe serum concentration of Gefitinib can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Gefitinib.Approved
CaffeineThe serum concentration of Gefitinib can be increased when it is combined with Caffeine.Approved
Calcium carbonateThe serum concentration of Gefitinib can be decreased when it is combined with Calcium carbonate.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Gefitinib.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Gefitinib.Approved
CandesartanThe serum concentration of Gefitinib can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Gefitinib can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Gefitinib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Gefitinib.Approved
CarvedilolThe serum concentration of Gefitinib can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Gefitinib can be increased when it is combined with Caspofungin.Approved
CelecoxibThe metabolism of Gefitinib can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Gefitinib can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Gefitinib.Withdrawn
ChloroquineThe serum concentration of Gefitinib can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Gefitinib can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Gefitinib can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Gefitinib can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholecalciferolThe metabolism of Gefitinib can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Gefitinib can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Gefitinib can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Gefitinib can be increased when it is combined with Cilazapril.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Gefitinib.Approved
CimetidineThe serum concentration of Gefitinib can be decreased when it is combined with Cimetidine.Approved
CinacalcetThe metabolism of Gefitinib can be decreased when combined with Cinacalcet.Approved
CiprofloxacinThe serum concentration of Gefitinib can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Gefitinib.Approved
CitalopramThe serum concentration of Gefitinib can be increased when it is combined with Citalopram.Approved
ClarithromycinThe metabolism of Gefitinib can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Gefitinib can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Gefitinib.Approved, Illicit
ClofazimineThe serum concentration of Gefitinib can be increased when it is combined with Clofazimine.Approved, Investigational
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Gefitinib.Approved, Investigational
ClomipramineThe serum concentration of Gefitinib can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Gefitinib.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Gefitinib.Approved, Nutraceutical
ClotrimazoleThe metabolism of Gefitinib can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Gefitinib.Approved
CobicistatThe serum concentration of Gefitinib can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Gefitinib.Approved
CocaineThe metabolism of Gefitinib can be decreased when combined with Cocaine.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Gefitinib.Approved
ColforsinThe serum concentration of Gefitinib can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Gefitinib can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Gefitinib.Approved
CrizotinibThe metabolism of Gefitinib can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Gefitinib.Approved, Investigational
CyclosporineThe metabolism of Gefitinib can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Gefitinib.Approved
DabrafenibThe serum concentration of Gefitinib can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Gefitinib can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Gefitinib can be increased when it is combined with Dactinomycin.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Gefitinib.Approved
DarifenacinThe metabolism of Gefitinib can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Gefitinib can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Gefitinib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Gefitinib can be decreased when it is combined with Daunorubicin.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Gefitinib.Approved
DeferasiroxThe serum concentration of Gefitinib can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Gefitinib can be decreased when combined with Delavirdine.Approved
DesipramineThe serum concentration of Gefitinib can be increased when it is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Gefitinib.Approved
DesloratadineThe serum concentration of Gefitinib can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Gefitinib can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Gefitinib can be increased when it is combined with Dextromethorphan.Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Gefitinib.Approved, Illicit, Vet Approved
DiclofenacThe serum concentration of Gefitinib can be increased when it is combined with Diclofenac.Approved, Vet Approved
DicoumarolGefitinib may increase the anticoagulant activities of Dicoumarol.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Gefitinib.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Gefitinib.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Gefitinib.Approved
DihydroergotamineThe metabolism of Gefitinib can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Gefitinib.Illicit
DiltiazemThe metabolism of Gefitinib can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Gefitinib can be decreased when combined with Diphenhydramine.Approved
DipyridamoleThe serum concentration of Gefitinib can be increased when it is combined with Dipyridamole.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Gefitinib.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Gefitinib.Approved, Investigational, Vet Approved
DoxazosinThe serum concentration of Gefitinib can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Gefitinib can be decreased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Gefitinib.Approved, Investigational
DoxorubicinThe serum concentration of Gefitinib can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Gefitinib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Gefitinib can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Gefitinib can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Gefitinib can be decreased when combined with Duloxetine.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Gefitinib.Approved
EfavirenzThe serum concentration of Gefitinib can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Gefitinib can be increased when it is combined with Elbasvir.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Gefitinib.Approved, Investigational
EliglustatThe metabolism of Gefitinib can be decreased when combined with Eliglustat.Approved
EltrombopagThe serum concentration of Gefitinib can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Gefitinib can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Gefitinib can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Gefitinib can be decreased when it is combined with Epinastine.Approved, Investigational
ErgonovineThe serum concentration of Gefitinib can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Gefitinib can be increased when it is combined with Ergotamine.Approved
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Gefitinib.Approved, Investigational
ErythromycinThe metabolism of Gefitinib can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Gefitinib can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe serum concentration of Gefitinib can be decreased when it is combined with Esomeprazole.Approved, Investigational
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Gefitinib.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Gefitinib can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Gefitinib can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Gefitinib can be decreased when it is combined with Estrone.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Gefitinib.Approved
Ethyl biscoumacetateGefitinib may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtoposideThe serum concentration of Gefitinib can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Gefitinib can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Gefitinib.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Gefitinib.Approved
FamotidineThe serum concentration of Gefitinib can be decreased when it is combined with Famotidine.Approved
FelodipineThe serum concentration of Gefitinib can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Gefitinib can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Gefitinib.Approved
FexofenadineThe serum concentration of Gefitinib can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Gefitinib.Approved
FluconazoleThe metabolism of Gefitinib can be decreased when combined with Fluconazole.Approved
FluindioneGefitinib may increase the anticoagulant activities of Fluindione.Investigational
FluoxetineThe metabolism of Gefitinib can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Gefitinib can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Gefitinib can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Gefitinib can be increased when it is combined with Flurazepam.Approved, Illicit
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Gefitinib.Approved
FluvoxamineThe metabolism of Gefitinib can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Gefitinib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Gefitinib can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Gefitinib can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Gefitinib can be increased when it is combined with Fusidic Acid.Approved
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Gefitinib.Approved
GenisteinThe serum concentration of Gefitinib can be increased when it is combined with Genistein.Investigational
GlyburideThe serum concentration of Gefitinib can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Gefitinib can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Gefitinib can be increased when it is combined with Gramicidin D.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Gefitinib.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Gefitinib.Withdrawn
HaloperidolThe serum concentration of Gefitinib can be increased when it is combined with Haloperidol.Approved
HydrocortisoneThe serum concentration of Gefitinib can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Gefitinib.Approved
IdelalisibThe serum concentration of Gefitinib can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Gefitinib can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Gefitinib can be increased when it is combined with Imipramine.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Gefitinib.Approved
IndinavirThe metabolism of Gefitinib can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Gefitinib can be increased when it is combined with Indomethacin.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Gefitinib.Approved, Investigational
IsavuconazoniumThe metabolism of Gefitinib can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Gefitinib can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Gefitinib can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Gefitinib can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Gefitinib can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Gefitinib can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Gefitinib can be increased when it is combined with Ketamine.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Gefitinib.Approved
KetoconazoleThe metabolism of Gefitinib can be decreased when combined with Ketoconazole.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Gefitinib.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Gefitinib.Approved, Investigational
LansoprazoleThe serum concentration of Gefitinib can be decreased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Gefitinib can be increased when it is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Gefitinib.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Gefitinib.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Gefitinib.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Gefitinib.Approved, Investigational
LevofloxacinThe serum concentration of Gefitinib can be increased when it is combined with Levofloxacin.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Gefitinib.Approved
LevothyroxineThe serum concentration of Gefitinib can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Gefitinib can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Gefitinib.Approved
LiothyronineThe serum concentration of Gefitinib can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Gefitinib can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Gefitinib can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Gefitinib can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Gefitinib can be increased when it is combined with Loperamide.Approved
LopinavirThe metabolism of Gefitinib can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Gefitinib can be increased when it is combined with Loratadine.Approved
LorcaserinThe metabolism of Gefitinib can be decreased when combined with Lorcaserin.Approved
LosartanThe serum concentration of Gefitinib can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Gefitinib can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Gefitinib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Gefitinib can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Gefitinib can be decreased when combined with Lumefantrine.Approved
MagaldrateThe serum concentration of Gefitinib can be decreased when it is combined with Magaldrate.Withdrawn
Magnesium carbonateThe serum concentration of Gefitinib can be decreased when it is combined with Magnesium carbonate.Approved
Magnesium hydroxideThe serum concentration of Gefitinib can be decreased when it is combined with Magnesium hydroxide.Approved
Magnesium oxideThe serum concentration of Gefitinib can be decreased when it is combined with Magnesium oxide.Approved
Magnesium TrisilicateThe serum concentration of Gefitinib can be decreased when it is combined with Magnesium Trisilicate.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Gefitinib.Approved, Investigational
MaprotilineThe serum concentration of Gefitinib can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Gefitinib can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Gefitinib can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Gefitinib can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Gefitinib can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneThe serum concentration of Gefitinib can be increased when it is combined with Methadone.Approved
MethanthelineThe serum concentration of Gefitinib can be decreased when it is combined with Methantheline.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Gefitinib.Approved
MethotrimeprazineThe metabolism of Gefitinib can be decreased when combined with Methotrimeprazine.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Gefitinib.Approved, Vet Approved
MetiamideThe serum concentration of Gefitinib can be decreased when it is combined with Metiamide.Experimental
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Gefitinib.Approved, Investigational
MibefradilThe serum concentration of Gefitinib can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Gefitinib can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Gefitinib can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Gefitinib can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Gefitinib.Approved
MitomycinThe serum concentration of Gefitinib can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Gefitinib can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Gefitinib can be decreased when it is combined with Mitoxantrone.Approved, Investigational
ModafinilThe serum concentration of Gefitinib can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Gefitinib can be increased when it is combined with Morphine.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Gefitinib.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Gefitinib.Approved
NafcillinThe serum concentration of Gefitinib can be decreased when it is combined with Nafcillin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Gefitinib.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Gefitinib.Approved, Vet Approved
NaltrexoneThe serum concentration of Gefitinib can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Gefitinib can be increased when it is combined with Naringenin.Experimental
NefazodoneThe metabolism of Gefitinib can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Gefitinib can be decreased when combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Gefitinib can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Gefitinib can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Gefitinib can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Gefitinib can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Gefitinib can be decreased when it is combined with Nifedipine.Approved
NilotinibThe metabolism of Gefitinib can be decreased when combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Gefitinib.Approved
NisoldipineThe serum concentration of Gefitinib can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Gefitinib can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Gefitinib can be increased when it is combined with Nitrendipine.Approved
NizatidineThe serum concentration of Gefitinib can be decreased when it is combined with Nizatidine.Approved
NorethisteroneThe serum concentration of Gefitinib can be decreased when it is combined with Norethisterone.Approved
OlanzapineThe serum concentration of Gefitinib can be decreased when it is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Gefitinib can be decreased when combined with Olaparib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Gefitinib.Approved
OmeprazoleThe serum concentration of Gefitinib can be decreased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Gefitinib can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Gefitinib.Approved
P-NitrophenolThe serum concentration of Gefitinib can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Gefitinib.Approved, Vet Approved
PalbociclibThe serum concentration of Gefitinib can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Gefitinib can be increased when it is combined with Palmitic Acid.Experimental
PanobinostatThe serum concentration of Gefitinib can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe serum concentration of Gefitinib can be decreased when it is combined with Pantoprazole.Approved
ParoxetineThe metabolism of Gefitinib can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Gefitinib.Approved
Peginterferon alfa-2bThe serum concentration of Gefitinib can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe serum concentration of Gefitinib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe serum concentration of Gefitinib can be increased when it is combined with Perindopril.Approved
PhenindioneGefitinib may increase the anticoagulant activities of Phenindione.Approved
PhenobarbitalThe serum concentration of Gefitinib can be decreased when it is combined with Phenobarbital.Approved
PhenprocoumonGefitinib may increase the anticoagulant activities of Phenprocoumon.Approved
PhenytoinThe serum concentration of Gefitinib can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Gefitinib can be increased when it is combined with Pimozide.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Gefitinib.Approved
Platelet Activating FactorThe serum concentration of Gefitinib can be decreased when it is combined with Platelet Activating Factor.Experimental
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Gefitinib.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Gefitinib.Approved
PosaconazoleThe metabolism of Gefitinib can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Gefitinib can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Gefitinib can be increased when it is combined with Prazosin.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Gefitinib.Approved, Vet Approved
PrednisoneThe serum concentration of Gefitinib can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe serum concentration of Gefitinib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Gefitinib can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Gefitinib can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromazineThe metabolism of Gefitinib can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe serum concentration of Gefitinib can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Gefitinib can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Gefitinib can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Gefitinib can be increased when it is combined with Protriptyline.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Gefitinib.Approved
QuercetinThe serum concentration of Gefitinib can be increased when it is combined with Quercetin.Experimental
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Gefitinib.Approved
QuinacrineThe serum concentration of Gefitinib can be increased when it is combined with Quinacrine.Approved
QuinidineThe metabolism of Gefitinib can be decreased when combined with Quinidine.Approved
QuinineThe serum concentration of Gefitinib can be increased when it is combined with Quinine.Approved
RabeprazoleThe serum concentration of Gefitinib can be decreased when it is combined with Rabeprazole.Approved, Investigational
RanitidineThe serum concentration of Gefitinib can be decreased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Gefitinib.Approved, Investigational
ReboxetineThe serum concentration of Gefitinib can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Gefitinib can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Gefitinib can be decreased when it is combined with Reserpine.Approved
RifabutinThe serum concentration of Gefitinib can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Gefitinib can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Gefitinib can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Gefitinib.Approved, Investigational
RilpivirineThe serum concentration of Gefitinib can be increased when it is combined with Rilpivirine.Approved
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Gefitinib.Approved, Investigational
RitonavirThe metabolism of Gefitinib can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Gefitinib.Approved
RolapitantThe serum concentration of Gefitinib can be increased when it is combined with Rolapitant.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Gefitinib.Approved, Investigational
RopiniroleThe metabolism of Gefitinib can be decreased when combined with Ropinirole.Approved, Investigational
Roxatidine acetateThe serum concentration of Gefitinib can be decreased when it is combined with Roxatidine acetate.Approved
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Gefitinib.Approved, Vet Approved
SaquinavirThe metabolism of Gefitinib can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Gefitinib can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Gefitinib can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Gefitinib.Approved
SertralineThe serum concentration of Gefitinib can be increased when it is combined with Sertraline.Approved
SildenafilThe metabolism of Gefitinib can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Gefitinib.Approved
SiltuximabThe serum concentration of Gefitinib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Gefitinib can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Gefitinib can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Gefitinib can be decreased when it is combined with Sirolimus.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Gefitinib.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Gefitinib.Approved
SorafenibThe serum concentration of Gefitinib can be increased when it is combined with Sorafenib.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Gefitinib.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Gefitinib.Experimental
SpironolactoneThe serum concentration of Gefitinib can be increased when it is combined with Spironolactone.Approved
St. John's WortThe serum concentration of Gefitinib can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Gefitinib can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Gefitinib can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Gefitinib can be decreased when it is combined with Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Gefitinib can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Gefitinib can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Gefitinib can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Gefitinib can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Gefitinib can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Gefitinib can be decreased when it is combined with Tacrolimus.Approved, Investigational
TAK-390MRThe serum concentration of Gefitinib can be decreased when it is combined with TAK-390MR.Investigational
TamoxifenThe serum concentration of Gefitinib can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Gefitinib can be increased when it is combined with Taurocholic Acid.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Gefitinib.Approved
TelaprevirThe metabolism of Gefitinib can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Gefitinib can be decreased when combined with Telithromycin.Approved
TelmisartanThe serum concentration of Gefitinib can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Gefitinib.Approved
TerazosinThe serum concentration of Gefitinib can be increased when it is combined with Terazosin.Approved
TerbinafineThe metabolism of Gefitinib can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe serum concentration of Gefitinib can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Gefitinib can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Gefitinib can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Gefitinib can be increased when it is combined with Testosterone.Approved, Investigational
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Gefitinib.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Gefitinib.Approved
TiclopidineThe metabolism of Gefitinib can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Gefitinib.Approved
TipranavirThe metabolism of Gefitinib can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Gefitinib can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Gefitinib.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Gefitinib.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Gefitinib.Approved, Investigational
TranylcypromineThe metabolism of Gefitinib can be decreased when combined with Tranylcypromine.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Gefitinib.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Gefitinib.Approved
TrazodoneThe serum concentration of Gefitinib can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Gefitinib can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Gefitinib can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Gefitinib can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Gefitinib can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Gefitinib can be increased when it is combined with Troleandomycin.Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Gefitinib.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Gefitinib.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Gefitinib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Gefitinib.Approved
VenlafaxineThe metabolism of Gefitinib can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Gefitinib can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Gefitinib can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Gefitinib.Approved, Investigational
VincristineThe serum concentration of Gefitinib can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineGefitinib may increase the neutropenic activities of Vinorelbine.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Gefitinib.Approved
VoriconazoleThe metabolism of Gefitinib can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinGefitinib may increase the anticoagulant activities of Warfarin.Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Gefitinib.Approved
ZimelidineThe serum concentration of Gefitinib can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Gefitinib can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Avoid fresh grapefruit and its juice during therapy as grapefruit may increase serum product levels.
  • Take without regard to meals.
References
Synthesis Reference

DrugSyn.org

US5770599
General References
  1. Pao W, Miller V, Zakowski M, Doherty J, Politi K, Sarkaria I, Singh B, Heelan R, Rusch V, Fulton L, Mardis E, Kupfer D, Wilson R, Kris M, Varmus H: EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A. 2004 Sep 7;101(36):13306-11. Epub 2004 Aug 25. [PubMed:15329413 ]
  2. Sordella R, Bell DW, Haber DA, Settleman J: Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science. 2004 Aug 20;305(5687):1163-7. Epub 2004 Jul 29. [PubMed:15284455 ]
External Links
ATC CodesL01XE02
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (80.5 KB)
MSDSDownload (59.2 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9961
Blood Brain Barrier+0.9759
Caco-2 permeable+0.5934
P-glycoprotein substrateSubstrate0.693
P-glycoprotein inhibitor IInhibitor0.7361
P-glycoprotein inhibitor IIInhibitor0.923
Renal organic cation transporterInhibitor0.5543
CYP450 2C9 substrateNon-substrate0.7853
CYP450 2D6 substrateNon-substrate0.6447
CYP450 3A4 substrateSubstrate0.6354
CYP450 1A2 substrateInhibitor0.7516
CYP450 2C9 inhibitorNon-inhibitor0.6272
CYP450 2D6 inhibitorNon-inhibitor0.6536
CYP450 2C19 inhibitorInhibitor0.644
CYP450 3A4 inhibitorInhibitor0.8206
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9309
Ames testNon AMES toxic0.5
CarcinogenicityNon-carcinogens0.9218
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5141 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.758
hERG inhibition (predictor II)Inhibitor0.8019
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Astrazeneca uk ltd
Packagers
Dosage forms
FormRouteStrength
TabletOral250 mg
Tablet, coatedOral250 mg/1
Tablet, film coatedOral250 mg
Prices
Unit descriptionCostUnit
Tarceva 150 mg tablet163.98USD tablet
Tarceva 100 mg tablet144.98USD tablet
Iressa 250 mg tablet68.08USD tablet
Tarceva 25 mg tablet52.78USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2086968 No1998-06-232013-01-08Canada
CA2215732 No2002-04-092016-04-23Canada
US5457105 No1993-01-192013-01-19Us
US5770599 No1997-05-052017-05-05Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySparingly soluble (<pH4)Not Available
logP3.2Not Available
pKa5.4 and 7.2FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.027 mg/mLALOGPS
logP4.02ALOGPS
logP3.75ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)16.11ChemAxon
pKa (Strongest Basic)6.85ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area68.74 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity117.51 m3·mol-1ChemAxon
Polarizability46.11 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassNaphthyridines
Sub ClassQuinazolines
Direct ParentQuinazolinamines
Alternative Parents
Substituents
  • Quinazolinamine
  • Anisole
  • Halobenzene
  • Fluorobenzene
  • Chlorobenzene
  • Aminopyrimidine
  • Alkyl aryl ether
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Oxazinane
  • Morpholine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Aryl chloride
  • Heteroaromatic compound
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Secondary amine
  • Ether
  • Dialkyl ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Ubiquitin protein ligase binding
Specific Function:
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TGFA/TGF-alpha, amphiregulin, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on ke...
Gene Name:
EGFR
Uniprot ID:
P00533
Molecular Weight:
134276.185 Da
References
  1. Ciardiello F, Caputo R, Bianco R, Damiano V, Pomatico G, De Placido S, Bianco AR, Tortora G: Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. Clin Cancer Res. 2000 May;6(5):2053-63. [PubMed:10815932 ]
  2. Albanell J, Codony-Servat J, Rojo F, Del Campo JM, Sauleda S, Anido J, Raspall G, Giralt J, Rosello J, Nicholson RI, Mendelsohn J, Baselga J: Activated extracellular signal-regulated kinases: association with epidermal growth factor receptor/transforming growth factor alpha expression in head and neck squamous carcinoma and inhibition by anti-epidermal growth factor receptor treatments. Cancer Res. 2001 Sep 1;61(17):6500-10. [PubMed:11522647 ]
  3. Nicholson RI, Hutcheson IR, Harper ME, Knowlden JM, Barrow D, McClelland RA, Jones HE, Wakeling AE, Gee JM: Modulation of epidermal growth factor receptor in endocrine-resistant, oestrogen receptor-positive breast cancer. Endocr Relat Cancer. 2001 Sep;8(3):175-82. [PubMed:11566608 ]
  4. Moasser MM, Basso A, Averbuch SD, Rosen N: The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61(19):7184-8. [PubMed:11585753 ]
  5. Arteaga CL, Johnson DH: Tyrosine kinase inhibitors-ZD1839 (Iressa). Curr Opin Oncol. 2001 Nov;13(6):491-8. [PubMed:11673690 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Li J, Zhao M, He P, Hidalgo M, Baker SD: Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res. 2007 Jun 15;13(12):3731-7. [PubMed:17575239 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Li J, Zhao M, He P, Hidalgo M, Baker SD: Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res. 2007 Jun 15;13(12):3731-7. [PubMed:17575239 ]
  2. Link [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Link [Link]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Shen J, Carcaboso AM, Hubbard KE, Tagen M, Wynn HG, Panetta JC, Waters CM, Elmeliegy MA, Stewart CF: Compartment-specific roles of ATP-binding cassette transporters define differential topotecan distribution in brain parenchyma and cerebrospinal fluid. Cancer Res. 2009 Jul 15;69(14):5885-92. doi: 10.1158/0008-5472.CAN-09-0700. Epub 2009 Jun 30. [PubMed:19567673 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Ozvegy-Laczka C, Hegedus T, Varady G, Ujhelly O, Schuetz JD, Varadi A, Keri G, Orfi L, Nemet K, Sarkadi B: High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. Mol Pharmacol. 2004 Jun;65(6):1485-95. [PubMed:15155841 ]
  2. An Y, Ongkeko WM: ABCG2: the key to chemoresistance in cancer stem cells? Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1529-42. doi: 10.1517/17425250903228834. [PubMed:19708828 ]
  3. Shen J, Carcaboso AM, Hubbard KE, Tagen M, Wynn HG, Panetta JC, Waters CM, Elmeliegy MA, Stewart CF: Compartment-specific roles of ATP-binding cassette transporters define differential topotecan distribution in brain parenchyma and cerebrospinal fluid. Cancer Res. 2009 Jul 15;69(14):5885-92. doi: 10.1158/0008-5472.CAN-09-0700. Epub 2009 Jun 30. [PubMed:19567673 ]
  4. Noguchi K, Kawahara H, Kaji A, Katayama K, Mitsuhashi J, Sugimoto Y: Substrate-dependent bidirectional modulation of P-glycoprotein-mediated drug resistance by erlotinib. Cancer Sci. 2009 Sep;100(9):1701-7. doi: 10.1111/j.1349-7006.2009.01213.x. Epub 2009 May 12. [PubMed:19493273 ]
  5. Shi Z, Parmar S, Peng XX, Shen T, Robey RW, Bates SE, Fu LW, Shao Y, Chen YM, Zang F, Chen ZS: The epidermal growth factor tyrosine kinase inhibitor AG1478 and erlotinib reverse ABCG2-mediated drug resistance. Oncol Rep. 2009 Feb;21(2):483-9. [PubMed:19148526 ]
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Drug created on June 13, 2005 07:24 / Updated on December 07, 2016 02:38