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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
Iressatablet, coated250 mg/1oralAstra Zeneca Pharmaceuticals Lp2015-07-13Not applicableUs
Iressatablet250 mgoralAstrazeneca Canada Inc2003-12-17Not applicableCanada
IressaFilm-coated tablet250 mgOral useAstra Zeneca Ab2009-06-24Not applicableEu
IressaFilm-coated tablet250 mgOral useAstra Zeneca Ab2009-06-24Not applicableEu
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 KeyInChIKey=XGALLCVXEZPNRQ-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
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
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.
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.
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
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
Film-coated tabletOral use250 mg
Tabletoral250 mg
Tablet, coatedoral250 mg/1
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
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)
Interactions
Drug Interactions
Drug
AbirateroneThe metabolism of Gefitinib can be decreased when combined with Abiraterone.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Gefitinib.
AcenocoumarolGefitinib may increase the anticoagulant activities of Acenocoumarol.
AcetaminophenThe serum concentration of Gefitinib can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Gefitinib.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Gefitinib.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Gefitinib.
AlbendazoleThe serum concentration of Gefitinib can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Gefitinib can be decreased when it is combined with Aldosterone.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Gefitinib.
AlectinibThe serum concentration of Gefitinib can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Gefitinib can be increased when it is combined with Alfentanil.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Gefitinib.
Aluminum hydroxideThe serum concentration of Gefitinib can be decreased when it is combined with Aluminum hydroxide.
Aluminum phosphateThe serum concentration of Gefitinib can be decreased when it is combined with Aluminum phosphate.
AmantadineThe serum concentration of Gefitinib can be increased when it is combined with Amantadine.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Gefitinib.
Aminohippuric acidThe serum concentration of Gefitinib can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Gefitinib can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Gefitinib can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Gefitinib can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Gefitinib can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Gefitinib can be increased when it is combined with Amsacrine.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Gefitinib.
AprepitantThe serum concentration of Gefitinib can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Gefitinib.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Gefitinib.
ArtemetherThe metabolism of Gefitinib can be decreased when combined with Artemether.
AsenapineThe serum concentration of Gefitinib can be decreased when it is combined with Asenapine.
AstemizoleThe serum concentration of Gefitinib can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Gefitinib.
AtenololThe serum concentration of Gefitinib can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Gefitinib can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Gefitinib can be increased when it is combined with Atorvastatin.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Gefitinib.
AzelastineThe serum concentration of Gefitinib can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Gefitinib can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Gefitinib can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Gefitinib can be increased when it is combined with Bepridil.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Gefitinib.
BetaxololThe metabolism of Gefitinib can be decreased when combined with Betaxolol.
BevacizumabBevacizumab may increase the cardiotoxic activities of Gefitinib.
BexaroteneThe serum concentration of Gefitinib can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Gefitinib can be increased when it is combined with Biperiden.
Bismuth SubcitrateThe serum concentration of Gefitinib can be decreased when it is combined with Bismuth Subcitrate.
BoceprevirThe metabolism of Gefitinib can be decreased when combined with Boceprevir.
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Gefitinib.
BortezomibThe metabolism of Gefitinib can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Gefitinib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Gefitinib.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Gefitinib.
BromocriptineThe serum concentration of Gefitinib can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Gefitinib can be increased when it is combined with Buprenorphine.
BupropionThe metabolism of Gefitinib can be decreased when combined with Bupropion.
BuspironeThe serum concentration of Gefitinib can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Gefitinib.
CaffeineThe serum concentration of Gefitinib can be increased when it is combined with Caffeine.
Calcium carbonateThe serum concentration of Gefitinib can be decreased when it is combined with Calcium carbonate.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Gefitinib.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Gefitinib.
CandesartanThe serum concentration of Gefitinib can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Gefitinib can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Gefitinib can be decreased when it is combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Gefitinib.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Gefitinib.
CarvedilolThe serum concentration of Gefitinib can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Gefitinib can be increased when it is combined with Caspofungin.
CelecoxibThe metabolism of Gefitinib can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Gefitinib can be increased when it is combined with Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Gefitinib.
ChloroquineThe serum concentration of Gefitinib can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Gefitinib can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Gefitinib can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Gefitinib can be increased when it is combined with Chlorprothixene.
CholecalciferolThe metabolism of Gefitinib can be decreased when combined with Cholecalciferol.
CholesterolThe serum concentration of Gefitinib can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Gefitinib can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Gefitinib can be increased when it is combined with Cilazapril.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Gefitinib.
CimetidineThe serum concentration of Gefitinib can be decreased when it is combined with Cimetidine.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Gefitinib.
CinacalcetThe metabolism of Gefitinib can be decreased when combined with Cinacalcet.
CiprofloxacinThe serum concentration of Gefitinib can be increased when it is combined with Ciprofloxacin.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Gefitinib.
CitalopramThe serum concentration of Gefitinib can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Gefitinib can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Gefitinib can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Gefitinib.
ClobazamThe metabolism of Gefitinib can be decreased when combined with Clobazam.
ClofazimineThe serum concentration of Gefitinib can be increased when it is combined with Clofazimine.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Gefitinib.
ClomipramineThe serum concentration of Gefitinib can be increased when it is combined with Clomipramine.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Gefitinib.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Gefitinib.
ClotrimazoleThe metabolism of Gefitinib can be decreased when combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Gefitinib.
ClozapineThe metabolism of Gefitinib can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Gefitinib can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Gefitinib.
CocaineThe metabolism of Gefitinib can be decreased when combined with Cocaine.
ColchicineThe serum concentration of Gefitinib can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Gefitinib can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Gefitinib can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Gefitinib.
CrizotinibThe metabolism of Gefitinib can be decreased when combined with Crizotinib.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Gefitinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Gefitinib.
CyclosporineThe metabolism of Gefitinib can be decreased when combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Gefitinib.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Gefitinib.
DabrafenibThe serum concentration of Gefitinib can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Gefitinib.
DaclatasvirThe serum concentration of Gefitinib can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Gefitinib can be increased when it is combined with Dactinomycin.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Gefitinib.
DarifenacinThe metabolism of Gefitinib can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Gefitinib can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Gefitinib can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Gefitinib can be decreased when it is combined with Daunorubicin.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Gefitinib.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Gefitinib.
DeferasiroxThe serum concentration of Gefitinib can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Gefitinib can be decreased when combined with Delavirdine.
DesipramineThe serum concentration of Gefitinib can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Gefitinib.
DesloratadineThe serum concentration of Gefitinib can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Gefitinib can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Gefitinib.
DextromethorphanThe serum concentration of Gefitinib can be increased when it is combined with Dextromethorphan.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Gefitinib.
DiclofenacThe serum concentration of Gefitinib can be increased when it is combined with Diclofenac.
DicoumarolGefitinib may increase the anticoagulant activities of Dicoumarol.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Gefitinib.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Gefitinib.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Gefitinib.
DigoxinDigoxin may decrease the cardiotoxic activities of Gefitinib.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Gefitinib.
DihydroergotamineThe metabolism of Gefitinib can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Gefitinib.
DiltiazemThe metabolism of Gefitinib can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Gefitinib.
DiphenhydramineThe metabolism of Gefitinib can be decreased when combined with Diphenhydramine.
DipyridamoleThe serum concentration of Gefitinib can be increased when it is combined with Dipyridamole.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Gefitinib.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Gefitinib.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Gefitinib.
DoxazosinThe serum concentration of Gefitinib can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Gefitinib can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Gefitinib can be decreased when it is combined with Doxorubicin.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Gefitinib.
DoxycyclineThe metabolism of Gefitinib can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Gefitinib can be increased when it is combined with Dronabinol.
DronedaroneThe metabolism of Gefitinib can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Gefitinib can be decreased when combined with Duloxetine.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Gefitinib.
EfavirenzThe serum concentration of Gefitinib can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Gefitinib can be increased when it is combined with Elbasvir.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Gefitinib.
EliglustatThe metabolism of Gefitinib can be decreased when combined with Eliglustat.
EltrombopagThe serum concentration of Gefitinib can be increased when it is combined with Eltrombopag.
EnalaprilThe serum concentration of Gefitinib can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Gefitinib can be increased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Gefitinib can be decreased when it is combined with Epinastine.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Gefitinib.
ErgonovineThe serum concentration of Gefitinib can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Gefitinib can be increased when it is combined with Ergotamine.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Gefitinib.
ErythromycinThe metabolism of Gefitinib can be decreased when combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Gefitinib.
Eslicarbazepine acetateThe serum concentration of Gefitinib can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe serum concentration of Gefitinib can be decreased when it is combined with Esomeprazole.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Gefitinib.
EstramustineThe serum concentration of Gefitinib can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Gefitinib can be decreased when it is combined with Estriol.
EstriolThe serum concentration of Estriol can be increased when it is combined with Gefitinib.
EstroneThe serum concentration of Gefitinib can be decreased when it is combined with Estrone.
EstroneThe serum concentration of Estrone can be increased when it is combined with Gefitinib.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Gefitinib.
Ethyl biscoumacetateGefitinib may increase the anticoagulant activities of Ethyl biscoumacetate.
EtoposideThe serum concentration of Gefitinib can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Gefitinib can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Gefitinib.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Gefitinib.
FamotidineThe serum concentration of Gefitinib can be decreased when it is combined with Famotidine.
FelodipineThe serum concentration of Gefitinib can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Gefitinib can be increased when it is combined with Fentanyl.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Gefitinib.
FexofenadineThe serum concentration of Gefitinib can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Gefitinib.
FluconazoleThe metabolism of Gefitinib can be decreased when combined with Fluconazole.
FluoxetineThe serum concentration of Gefitinib can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Gefitinib can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Gefitinib can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Gefitinib can be increased when it is combined with Flurazepam.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Gefitinib.
FluvoxamineThe metabolism of Gefitinib can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Gefitinib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Gefitinib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Gefitinib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Gefitinib can be increased when it is combined with Fusidic Acid.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Gefitinib.
GenisteinThe serum concentration of Gefitinib can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Gefitinib can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Gefitinib can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Gefitinib can be increased when it is combined with Gramicidin D.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Gefitinib.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Gefitinib.
HaloperidolThe serum concentration of Gefitinib can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Gefitinib can be increased when it is combined with Hydrocortisone.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Gefitinib.
IdelalisibThe serum concentration of Gefitinib can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Gefitinib can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Gefitinib.
ImipramineThe serum concentration of Gefitinib can be increased when it is combined with Imipramine.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Gefitinib.
IndinavirThe serum concentration of Gefitinib can be decreased when it is combined with Indinavir.
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Gefitinib.
IndomethacinThe serum concentration of Gefitinib can be increased when it is combined with Indomethacin.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Gefitinib.
IsavuconazoniumThe metabolism of Gefitinib can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Gefitinib can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Gefitinib can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Gefitinib can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Gefitinib can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Gefitinib can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Gefitinib can be increased when it is combined with Ketamine.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Gefitinib.
KetoconazoleThe serum concentration of Gefitinib can be increased when it is combined with Ketoconazole.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Gefitinib.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Gefitinib.
LansoprazoleThe serum concentration of Gefitinib can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Gefitinib can be increased when it is combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Gefitinib.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Gefitinib.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Gefitinib.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Gefitinib.
LevofloxacinThe serum concentration of Gefitinib can be increased when it is combined with Levofloxacin.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Gefitinib.
LevothyroxineThe serum concentration of Gefitinib can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Gefitinib can be increased when it is combined with Lidocaine.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Gefitinib.
LiothyronineThe serum concentration of Gefitinib can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Gefitinib can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Gefitinib can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Gefitinib can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Gefitinib can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Gefitinib can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Gefitinib can be increased when it is combined with Loratadine.
LorcaserinThe metabolism of Gefitinib can be decreased when combined with Lorcaserin.
LosartanThe serum concentration of Gefitinib can be increased when it is combined with Losartan.
LovastatinThe metabolism of Gefitinib can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Gefitinib can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Gefitinib can be decreased when it is combined with Lumacaftor.
LumefantrineThe metabolism of Gefitinib can be decreased when combined with Lumefantrine.
MagaldrateThe serum concentration of Gefitinib can be decreased when it is combined with Magaldrate.
Magnesium carbonateThe serum concentration of Gefitinib can be decreased when it is combined with Magnesium carbonate.
Magnesium hydroxideThe serum concentration of Gefitinib can be decreased when it is combined with Magnesium hydroxide.
Magnesium oxideThe serum concentration of Gefitinib can be decreased when it is combined with Magnesium oxide.
Magnesium TrisilicateThe serum concentration of Gefitinib can be decreased when it is combined with Magnesium Trisilicate.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Gefitinib.
MaprotilineThe serum concentration of Gefitinib can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Gefitinib can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Gefitinib can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Gefitinib can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Gefitinib can be increased when it is combined with Meprobamate.
MethadoneThe serum concentration of Gefitinib can be increased when it is combined with Methadone.
MethanthelineThe serum concentration of Gefitinib can be decreased when it is combined with Methantheline.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Gefitinib.
MethotrimeprazineThe metabolism of Gefitinib can be decreased when combined with Methotrimeprazine.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Gefitinib.
MetiamideThe serum concentration of Gefitinib can be decreased when it is combined with Metiamide.
MetoprololThe serum concentration of Gefitinib can be increased when it is combined with Metoprolol.
MibefradilThe serum concentration of Gefitinib can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Gefitinib can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Gefitinib can be decreased when it is combined with Midazolam.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Gefitinib.
MifepristoneThe metabolism of Gefitinib can be decreased when combined with Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Gefitinib.
MirabegronThe metabolism of Gefitinib can be decreased when combined with Mirabegron.
MitomycinThe serum concentration of Gefitinib can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Gefitinib can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Gefitinib can be decreased when it is combined with Mitoxantrone.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Gefitinib.
ModafinilThe serum concentration of Gefitinib can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Gefitinib can be increased when it is combined with Morphine.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Gefitinib.
NadololThe serum concentration of Nadolol can be increased when it is combined with Gefitinib.
NafcillinThe serum concentration of Gefitinib can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Gefitinib.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Gefitinib.
NaltrexoneThe serum concentration of Gefitinib can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Gefitinib can be increased when it is combined with Naringenin.
NefazodoneThe serum concentration of Gefitinib can be decreased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Gefitinib can be decreased when it is combined with Nelfinavir.
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Gefitinib.
NeostigmineThe serum concentration of Gefitinib can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Gefitinib can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Gefitinib can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Gefitinib can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Gefitinib can be decreased when it is combined with Nifedipine.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Gefitinib.
NilotinibThe metabolism of Gefitinib can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Gefitinib.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Gefitinib.
NisoldipineThe serum concentration of Gefitinib can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Gefitinib can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Gefitinib can be increased when it is combined with Nitrendipine.
NizatidineThe serum concentration of Gefitinib can be decreased when it is combined with Nizatidine.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Gefitinib.
NorethisteroneThe serum concentration of Gefitinib can be decreased when it is combined with Norethisterone.
OlanzapineThe serum concentration of Gefitinib can be decreased when it is combined with Olanzapine.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Gefitinib.
OlaparibThe metabolism of Gefitinib can be decreased when combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Gefitinib.
OmeprazoleThe serum concentration of Gefitinib can be increased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Gefitinib can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Gefitinib.
P-NitrophenolThe serum concentration of Gefitinib can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Gefitinib can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Gefitinib can be increased when it is combined with Palbociclib.
Palmitic AcidThe serum concentration of Gefitinib can be increased when it is combined with Palmitic Acid.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Gefitinib.
PanobinostatThe metabolism of Gefitinib can be decreased when combined with Panobinostat.
PantoprazoleThe serum concentration of Gefitinib can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Gefitinib can be increased when it is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Gefitinib.
Peginterferon alfa-2bThe serum concentration of Gefitinib can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe serum concentration of Gefitinib can be decreased when it is combined with Pentobarbital.
PerindoprilThe serum concentration of Gefitinib can be increased when it is combined with Perindopril.
PhenindioneGefitinib may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe serum concentration of Gefitinib can be decreased when it is combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Gefitinib.
PhenprocoumonGefitinib may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe serum concentration of Gefitinib can be decreased when it is combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Gefitinib.
PimozideThe serum concentration of Gefitinib can be increased when it is combined with Pimozide.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Gefitinib.
Platelet Activating FactorThe serum concentration of Gefitinib can be decreased when it is combined with Platelet Activating Factor.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Gefitinib.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Gefitinib.
PosaconazoleThe serum concentration of Gefitinib can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Gefitinib can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Gefitinib can be increased when it is combined with Prazosin.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Gefitinib.
PrednisoneThe serum concentration of Gefitinib can be increased when it is combined with Prednisone.
PrimidoneThe serum concentration of Gefitinib can be decreased when it is combined with Primidone.
ProbenecidThe serum concentration of Gefitinib can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Gefitinib can be decreased when it is combined with Progesterone.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Gefitinib.
PromazineThe metabolism of Gefitinib can be decreased when combined with Promazine.
PromethazineThe serum concentration of Gefitinib can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Gefitinib can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Gefitinib can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Gefitinib can be increased when it is combined with Protriptyline.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Gefitinib.
QuercetinThe serum concentration of Gefitinib can be increased when it is combined with Quercetin.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Gefitinib.
QuinacrineThe serum concentration of Gefitinib can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Gefitinib can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Gefitinib can be increased when it is combined with Quinine.
RabeprazoleThe serum concentration of Gefitinib can be decreased when it is combined with Rabeprazole.
RanitidineThe serum concentration of Gefitinib can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Gefitinib.
ReboxetineThe serum concentration of Gefitinib can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Gefitinib can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Gefitinib can be decreased when it is combined with Reserpine.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Gefitinib.
RifabutinThe serum concentration of Gefitinib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Gefitinib can be decreased when it is combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Gefitinib.
RifapentineThe serum concentration of Gefitinib can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Gefitinib.
RilpivirineThe serum concentration of Gefitinib can be increased when it is combined with Rilpivirine.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Gefitinib.
RitonavirThe serum concentration of Gefitinib can be decreased when it is combined with Ritonavir.
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Gefitinib.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Gefitinib.
RolapitantThe serum concentration of Gefitinib can be increased when it is combined with Rolapitant.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Gefitinib.
RopiniroleThe metabolism of Gefitinib can be decreased when combined with Ropinirole.
Roxatidine acetateThe serum concentration of Gefitinib can be decreased when it is combined with Roxatidine acetate.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Gefitinib.
SaquinavirThe serum concentration of Gefitinib can be decreased when it is combined with Saquinavir.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Gefitinib.
ScopolamineThe serum concentration of Gefitinib can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Gefitinib can be increased when it is combined with Selegiline.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Gefitinib.
SertralineThe serum concentration of Gefitinib can be increased when it is combined with Sertraline.
SildenafilThe metabolism of Gefitinib can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Gefitinib.
SiltuximabThe serum concentration of Gefitinib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Gefitinib can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Gefitinib can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Gefitinib can be decreased when it is combined with Sirolimus.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Gefitinib.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Gefitinib.
SorafenibThe serum concentration of Gefitinib can be increased when it is combined with Sorafenib.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Gefitinib.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Gefitinib.
SpironolactoneThe serum concentration of Gefitinib can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Gefitinib can be decreased when it is combined with St. John&#39;s Wort.
StaurosporineThe serum concentration of Gefitinib can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Gefitinib can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Gefitinib can be decreased when it is combined with Streptozocin.
SulfinpyrazoneThe serum concentration of Gefitinib can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe metabolism of Gefitinib can be decreased when combined with Sulfisoxazole.
SumatriptanThe serum concentration of Gefitinib can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Gefitinib can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Gefitinib can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Gefitinib can be decreased when it is combined with Tacrolimus.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Gefitinib.
TAK-390MRThe serum concentration of Gefitinib can be decreased when it is combined with TAK-390MR.
TamoxifenThe serum concentration of Gefitinib can be decreased when it is combined with Tamoxifen.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Gefitinib.
Taurocholic AcidThe serum concentration of Gefitinib can be increased when it is combined with Taurocholic Acid.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Gefitinib.
TelaprevirThe metabolism of Gefitinib can be decreased when combined with Telaprevir.
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Gefitinib.
TelithromycinThe metabolism of Gefitinib can be decreased when combined with Telithromycin.
TelmisartanThe serum concentration of Gefitinib can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Gefitinib.
TerazosinThe serum concentration of Gefitinib can be increased when it is combined with Terazosin.
TerbinafineThe metabolism of Gefitinib can be decreased when combined with Terbinafine.
TerfenadineThe serum concentration of Gefitinib can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Gefitinib can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Gefitinib can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Gefitinib can be increased when it is combined with Testosterone.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Gefitinib.
ThioridazineThe metabolism of Gefitinib can be decreased when combined with Thioridazine.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Gefitinib.
TiclopidineThe metabolism of Gefitinib can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be increased when it is combined with Gefitinib.
TipranavirThe metabolism of Gefitinib can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Gefitinib can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Gefitinib.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Gefitinib.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Gefitinib.
TranylcypromineThe metabolism of Gefitinib can be decreased when combined with Tranylcypromine.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Gefitinib.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Gefitinib.
TrazodoneThe serum concentration of Gefitinib can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Gefitinib can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Gefitinib can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Gefitinib can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Gefitinib can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Gefitinib can be increased when it is combined with Troleandomycin.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Gefitinib.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Gefitinib.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Gefitinib.
VenlafaxineThe metabolism of Gefitinib can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Gefitinib.
VerapamilThe metabolism of Gefitinib can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Gefitinib.
VinblastineThe serum concentration of Gefitinib can be decreased when it is combined with Vinblastine.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Gefitinib.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Gefitinib.
VincristineThe serum concentration of Gefitinib can be decreased when it is combined with Vincristine.
VinorelbineGefitinib may increase the neutropenic activities of Vinorelbine.
VinorelbineThe serum concentration of Gefitinib can be increased when it is combined with Vinorelbine.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Gefitinib.
VoriconazoleThe metabolism of Gefitinib can be decreased when combined with Voriconazole.
WarfarinGefitinib may increase the anticoagulant activities of Warfarin.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Gefitinib.
ZimelidineThe serum concentration of Gefitinib can be increased when it is combined with Zimelidine.
ZiprasidoneThe metabolism of Gefitinib can be decreased when combined with Ziprasidone.
Food Interactions
  • Avoid fresh grapefruit and its juice during therapy as grapefruit may increase serum product levels.
  • Take without regard to meals.

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
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  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 September 30, 2016 02:26