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Identification
NameAfatinib
Accession NumberDB08916
TypeSmall Molecule
GroupsApproved
DescriptionAfatinib is a tyrosine kinase inhibitor which is a 4-anilinoquinazoline. It is prepared has the dimaleate salt. FDA approved on July 12, 2013.
Structure
Thumb
Synonyms
Afatinibum
BIBW 2992
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Gilotriftablet, film coated30 mg/1oralBoehringer Ingelheim Pharmaceuticals, Inc.2013-07-12Not applicableUs
Gilotriftablet, film coated40 mg/1oralBoehringer Ingelheim Pharmaceuticals, Inc.2013-07-12Not applicableUs
Gilotriftablet, film coated20 mg/1oralBoehringer Ingelheim Pharmaceuticals, Inc.2013-07-12Not applicableUs
Giotriftablet30 mgoralBoehringer Ingelheim (Canada) Ltd Ltee2014-01-17Not applicableCanada
Giotriftablet40 mgoralBoehringer Ingelheim (Canada) Ltd Ltee2014-01-17Not applicableCanada
Giotriftablet20 mgoralBoehringer Ingelheim (Canada) Ltd Ltee2014-01-17Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Afatinib Dimaleate
Thumb
  • InChI Key: USNRYVNRPYXCSP-JUGPPOIOSA-N
  • Monoisotopic Mass: 717.184912835
  • Average Mass: 718.083
DBSALT000005
Categories
UNII41UD74L59M
CAS number850140-72-6
WeightAverage: 485.938
Monoisotopic: 485.162995603
Chemical FormulaC24H25ClFN5O3
InChI KeyInChIKey=ULXXDDBFHOBEHA-CWDCEQMOSA-N
InChI
InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
IUPAC Name
(2E)-N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[(3S)-oxolan-3-yloxy]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide
SMILES
CN(C)C\C=C\C(=O)NC1=C(O[[email protected]]2CCOC2)C=C2N=CN=C(NC3=CC(Cl)=C(F)C=C3)C2=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
  • N-arylamide
  • Halobenzene
  • Fluorobenzene
  • Chlorobenzene
  • Aminopyrimidine
  • Alkyl aryl ether
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Saccharide
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Aryl chloride
  • Heteroaromatic compound
  • Oxolane
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Secondary amine
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationAfatinib is a kinase inhibitor indicated for the first-line treatment of patient with metastatic non-small cell lung cancer (NSCLC) whose tumours have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.
PharmacodynamicsAfatinib did not effect the QTc interval.
Mechanism of actionAfatinib is an irreversible kinase inhibitor and binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) to inhibit tyrosine kinase autophosphorylation. This results in a downregulation of ErbB signalling and subsequent inhibition of proliferation of cell lines expressing wild-type EGFR, selected EGFR exon 19 deletion mutations, or exon 21 L858R mutations. It also inhibited in vitro proliferation of cell lines overexpressing HER2. Overall, tumour growth was inhibited.
Related Articles
AbsorptionFollowing oral administration, time to peak plasma concentration (Tmax) is 2 to 5 hours. The geometric mean relative bioavailability of 20 mg tablets was 92% as compared to an oral solution. Food decreases Cmax and AUC relative to the fasted state.
Volume of distributionNot Available
Protein binding95% bound to human plasma protein.
Metabolism

Enzymatic metabolism of afatinib is minimal. Covalent adducts to proteins are the major circulating metabolites.

Route of eliminationExcretion of afatinib is primarily via the feces (85%), with 4% recovered in the urine following a single oral dose of afatinib solution. The parent compound accounted for 88% of the recovered dose.
Half lifeCancer patients, repeat dosing = 37 hours
ClearanceNot Available
ToxicityMost common adverse reactions (≥20%) are diarrhea, rash/dermatitis, acneiform, stomatitis, paronychia, dry skin, decreased appetite, pruritus.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
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 ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.8717
Caco-2 permeable-0.5342
P-glycoprotein substrateSubstrate0.744
P-glycoprotein inhibitor IInhibitor0.6776
P-glycoprotein inhibitor IIInhibitor0.9036
Renal organic cation transporterNon-inhibitor0.7154
CYP450 2C9 substrateNon-substrate0.7919
CYP450 2D6 substrateNon-substrate0.8034
CYP450 3A4 substrateSubstrate0.7504
CYP450 1A2 substrateNon-inhibitor0.5236
CYP450 2C9 inhibitorNon-inhibitor0.7294
CYP450 2D6 inhibitorNon-inhibitor0.7625
CYP450 2C19 inhibitorNon-inhibitor0.5877
CYP450 3A4 inhibitorNon-inhibitor0.6486
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7096
Ames testNon AMES toxic0.5695
CarcinogenicityNon-carcinogens0.8692
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5643 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8956
hERG inhibition (predictor II)Inhibitor0.7228
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet, film coatedoral20 mg/1
Tablet, film coatedoral30 mg/1
Tablet, film coatedoral40 mg/1
Tabletoral20 mg
Tabletoral30 mg
Tabletoral40 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6251912 No1998-07-292018-07-29Us
US8426586 No2009-10-102029-10-10Us
US8545884 No2009-12-192029-12-19Us
USRE43431 No2002-01-222022-01-22Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0128 mg/mLALOGPS
logP3.77ALOGPS
logP3.76ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)12.49ChemAxon
pKa (Strongest Basic)8.81ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area88.61 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity131.38 m3·mol-1ChemAxon
Polarizability50.07 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesL01XE13
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (427 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Afatinib.
AcetaminophenThe serum concentration of Afatinib can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Afatinib.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Afatinib can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Afatinib can be decreased when it is combined with Aldosterone.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Afatinib.
AlectinibThe serum concentration of Afatinib can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Afatinib can be increased when it is combined with Alfentanil.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Afatinib.
AmantadineThe serum concentration of Afatinib can be increased when it is combined with Amantadine.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Afatinib.
Aminohippuric acidThe serum concentration of Afatinib can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Afatinib can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Afatinib can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Afatinib can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Afatinib can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Afatinib can be increased when it is combined with Amsacrine.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Afatinib.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Afatinib.
AstemizoleThe serum concentration of Afatinib can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Afatinib can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Afatinib can be increased when it is combined with Atenolol.
AtorvastatinThe serum concentration of Afatinib can be increased when it is combined with Atorvastatin.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Afatinib.
AzelastineThe serum concentration of Afatinib can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Afatinib can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Afatinib can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Afatinib can be increased when it is combined with Bepridil.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Afatinib.
BevacizumabBevacizumab may increase the cardiotoxic activities of Afatinib.
BiperidenThe serum concentration of Afatinib can be increased when it is combined with Biperiden.
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Afatinib.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Afatinib.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Afatinib.
BromocriptineThe serum concentration of Afatinib can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Afatinib can be increased when it is combined with Buprenorphine.
BuspironeThe serum concentration of Afatinib can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Afatinib can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Afatinib can be increased when it is combined with Caffeine.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Afatinib.
CanagliflozinThe serum concentration of Afatinib can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Afatinib can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Afatinib can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Afatinib can be decreased when it is combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Afatinib.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Afatinib.
CarvedilolThe serum concentration of Afatinib can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Afatinib can be increased when it is combined with Caspofungin.
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Afatinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Afatinib.
ChloroquineThe serum concentration of Afatinib can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Afatinib can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Afatinib can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Afatinib can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Afatinib can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Afatinib can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Afatinib can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Afatinib can be decreased when it is combined with Cimetidine.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Afatinib.
CiprofloxacinThe serum concentration of Afatinib can be increased when it is combined with Ciprofloxacin.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Afatinib.
CitalopramThe serum concentration of Afatinib can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Afatinib can be increased when it is combined with Clarithromycin.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Afatinib.
ClofazimineThe serum concentration of Afatinib can be increased when it is combined with Clofazimine.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Afatinib.
ClomipramineThe serum concentration of Afatinib can be increased when it is combined with Clomipramine.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Afatinib.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Afatinib.
ClotrimazoleThe serum concentration of Afatinib can be decreased when it is combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Afatinib.
CobicistatThe serum concentration of Afatinib can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Afatinib.
ColchicineThe serum concentration of Afatinib can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Afatinib can be increased when it is combined with Colforsin.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Afatinib.
CrizotinibThe serum concentration of Afatinib can be increased when it is combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Afatinib.
CyclosporineThe serum concentration of Afatinib can be decreased when it is combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Afatinib.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Afatinib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Afatinib.
DaclatasvirThe serum concentration of Afatinib can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Afatinib can be increased when it is combined with Dactinomycin.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Afatinib.
DasatinibThe serum concentration of Afatinib can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Afatinib can be decreased when it is combined with Daunorubicin.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Afatinib.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Afatinib.
DesipramineThe serum concentration of Afatinib can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Afatinib.
DesloratadineThe serum concentration of Afatinib can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Afatinib can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Afatinib.
DextromethorphanThe serum concentration of Afatinib can be increased when it is combined with Dextromethorphan.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Afatinib.
DiclofenacThe serum concentration of Afatinib can be increased when it is combined with Diclofenac.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Afatinib.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Afatinib.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Afatinib.
DigoxinDigoxin may decrease the cardiotoxic activities of Afatinib.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Afatinib.
DihydroergotamineThe serum concentration of Afatinib can be increased when it is combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Afatinib.
DiltiazemThe serum concentration of Afatinib can be increased when it is combined with Diltiazem.
DipyridamoleThe serum concentration of Afatinib can be increased when it is combined with Dipyridamole.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Afatinib.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Afatinib.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Afatinib.
DoxazosinThe serum concentration of Afatinib can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Afatinib can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Afatinib can be decreased when it is combined with Doxorubicin.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Afatinib.
DronabinolThe serum concentration of Afatinib can be increased when it is combined with Dronabinol.
DronedaroneThe serum concentration of Afatinib can be increased when it is combined with Dronedarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Afatinib.
ElbasvirThe serum concentration of Afatinib can be increased when it is combined with Elbasvir.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Afatinib.
EltrombopagThe serum concentration of Afatinib can be increased when it is combined with Eltrombopag.
EnalaprilThe serum concentration of Afatinib can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Afatinib can be increased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Afatinib.
ErgonovineThe serum concentration of Afatinib can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Afatinib can be increased when it is combined with Ergotamine.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Afatinib.
ErythromycinThe serum concentration of Afatinib can be decreased when it is combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Afatinib.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Afatinib.
EstramustineThe serum concentration of Afatinib can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Afatinib can be decreased when it is combined with Estriol.
EstriolThe serum concentration of Estriol can be increased when it is combined with Afatinib.
EstroneThe serum concentration of Afatinib can be decreased when it is combined with Estrone.
EstroneThe serum concentration of Estrone can be increased when it is combined with Afatinib.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Afatinib.
EtoposideThe serum concentration of Afatinib can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Afatinib can be increased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Afatinib.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Afatinib.
FelodipineThe serum concentration of Afatinib can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Afatinib can be increased when it is combined with Fentanyl.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Afatinib.
FexofenadineThe serum concentration of Afatinib can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Afatinib can be increased when it is combined with Fidaxomicin.
FluconazoleThe serum concentration of Afatinib can be increased when it is combined with Fluconazole.
FluoxetineThe serum concentration of Afatinib can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Afatinib can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Afatinib can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Afatinib can be increased when it is combined with Flurazepam.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Afatinib.
FluvoxamineThe serum concentration of Afatinib can be increased when it is combined with Fluvoxamine.
GefitinibThe serum concentration of Afatinib can be increased when it is combined with Gefitinib.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Afatinib.
GenisteinThe serum concentration of Afatinib can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Afatinib can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Afatinib can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Afatinib can be increased when it is combined with Gramicidin D.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Afatinib.
GrepafloxacinThe serum concentration of Afatinib can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Afatinib can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Afatinib can be increased when it is combined with Hydrocortisone.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Afatinib.
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Afatinib.
ImatinibThe serum concentration of Afatinib can be increased when it is combined with Imatinib.
ImipramineThe serum concentration of Afatinib can be increased when it is combined with Imipramine.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Afatinib.
IndinavirThe serum concentration of Afatinib can be decreased when it is combined with Indinavir.
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Afatinib.
IndomethacinThe serum concentration of Afatinib can be increased when it is combined with Indomethacin.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Afatinib.
IsavuconazoniumThe serum concentration of Afatinib can be increased when it is combined with Isavuconazonium.
ItraconazoleThe serum concentration of Afatinib can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Afatinib can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Afatinib can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Afatinib can be increased when it is combined with Ketamine.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Afatinib.
KetoconazoleThe serum concentration of Afatinib can be increased when it is combined with Ketoconazole.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Afatinib.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Afatinib.
LansoprazoleThe serum concentration of Afatinib can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Afatinib can be increased when it is combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Afatinib.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Afatinib.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Afatinib.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Afatinib.
LevofloxacinThe serum concentration of Afatinib can be increased when it is combined with Levofloxacin.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Afatinib.
LevothyroxineThe serum concentration of Afatinib can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Afatinib can be increased when it is combined with Lidocaine.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Afatinib.
LiothyronineThe serum concentration of Afatinib can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Afatinib can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Afatinib can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Afatinib can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Afatinib can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Afatinib can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Afatinib can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Afatinib can be increased when it is combined with Losartan.
LovastatinThe serum concentration of Afatinib can be increased when it is combined with Lovastatin.
LumacaftorThe serum concentration of Afatinib can be decreased when it is combined with Lumacaftor.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Afatinib.
MaprotilineThe serum concentration of Afatinib can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Afatinib can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Afatinib can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Afatinib can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Afatinib can be increased when it is combined with Meprobamate.
MethadoneThe serum concentration of Afatinib can be increased when it is combined with Methadone.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Afatinib.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Afatinib.
MetoprololThe serum concentration of Afatinib can be increased when it is combined with Metoprolol.
MibefradilThe serum concentration of Afatinib can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Afatinib can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Afatinib can be decreased when it is combined with Midazolam.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Afatinib.
MifepristoneThe serum concentration of Afatinib can be decreased when it is combined with Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Afatinib.
MitomycinThe serum concentration of Afatinib can be increased when it is combined with Mitomycin.
MitoxantroneThe serum concentration of Afatinib can be decreased when it is combined with Mitoxantrone.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Afatinib.
MorphineThe serum concentration of Afatinib can be increased when it is combined with Morphine.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Afatinib.
NadololThe serum concentration of Nadolol can be increased when it is combined with Afatinib.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Afatinib.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Afatinib.
NaltrexoneThe serum concentration of Afatinib can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Afatinib can be increased when it is combined with Naringenin.
NefazodoneThe serum concentration of Afatinib can be decreased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Afatinib can be decreased when it is combined with Nelfinavir.
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Afatinib.
NeostigmineThe serum concentration of Afatinib can be increased when it is combined with Neostigmine.
NicardipineThe serum concentration of Afatinib can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Afatinib can be decreased when it is combined with Nifedipine.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Afatinib.
NilotinibThe serum concentration of Afatinib can be increased when it is combined with Nilotinib.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Afatinib.
NisoldipineThe serum concentration of Afatinib can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Afatinib can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Afatinib can be increased when it is combined with Nitrendipine.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Afatinib.
NorethisteroneThe serum concentration of Afatinib can be decreased when it is combined with Norethisterone.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Afatinib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Afatinib.
OmeprazoleThe serum concentration of Afatinib can be increased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Osimertinib can be increased when it is combined with Afatinib.
OuabainOuabain may decrease the cardiotoxic activities of Afatinib.
P-NitrophenolThe serum concentration of Afatinib can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Afatinib can be increased when it is combined with Paclitaxel.
Palmitic AcidThe serum concentration of Afatinib can be increased when it is combined with Palmitic Acid.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Afatinib.
PantoprazoleThe serum concentration of Afatinib can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Afatinib can be increased when it is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Afatinib.
PerindoprilThe serum concentration of Afatinib can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Afatinib can be decreased when it is combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Afatinib.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Afatinib.
PimozideThe serum concentration of Afatinib can be increased when it is combined with Pimozide.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Afatinib.
Platelet Activating FactorThe serum concentration of Afatinib can be decreased when it is combined with Platelet Activating Factor.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Afatinib.
PonatinibThe serum concentration of Afatinib can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Afatinib can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Afatinib can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Afatinib can be increased when it is combined with Prazosin.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Afatinib.
PrednisoneThe serum concentration of Afatinib can be increased when it is combined with Prednisone.
ProbenecidThe serum concentration of Afatinib can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Afatinib can be decreased when it is combined with Progesterone.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Afatinib.
PromethazineThe serum concentration of Afatinib can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Afatinib can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Afatinib can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Afatinib can be increased when it is combined with Protriptyline.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Afatinib.
QuercetinThe serum concentration of Afatinib can be increased when it is combined with Quercetin.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Afatinib.
QuinacrineThe serum concentration of Afatinib can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Afatinib can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Afatinib can be increased when it is combined with Quinine.
RanitidineThe serum concentration of Afatinib can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Afatinib.
ReboxetineThe serum concentration of Afatinib can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Afatinib can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Afatinib can be decreased when it is combined with Reserpine.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Afatinib.
RifampicinThe serum concentration of Afatinib can be decreased when it is combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Afatinib.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Afatinib.
RilpivirineThe serum concentration of Afatinib can be increased when it is combined with Rilpivirine.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Afatinib.
RitonavirThe serum concentration of Afatinib can be decreased when it is combined with Ritonavir.
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Afatinib.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Afatinib.
RolapitantThe serum concentration of Afatinib can be increased when it is combined with Rolapitant.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Afatinib.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Afatinib.
SaquinavirThe serum concentration of Afatinib can be decreased when it is combined with Saquinavir.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Afatinib.
ScopolamineThe serum concentration of Afatinib can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Afatinib can be increased when it is combined with Selegiline.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Afatinib.
SertralineThe serum concentration of Afatinib can be increased when it is combined with Sertraline.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Afatinib.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Afatinib.
SimvastatinThe serum concentration of Afatinib can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Afatinib can be decreased when it is combined with Sirolimus.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Afatinib.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Afatinib.
SorafenibThe serum concentration of Afatinib can be increased when it is combined with Sorafenib.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Afatinib.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Afatinib.
SpironolactoneThe serum concentration of Afatinib can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Afatinib can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Afatinib can be increased when it is combined with Staurosporine.
StreptozocinThe serum concentration of Afatinib can be decreased when it is combined with Streptozocin.
SulfinpyrazoneThe serum concentration of Afatinib can be increased when it is combined with Sulfinpyrazone.
SumatriptanThe serum concentration of Afatinib can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Afatinib can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Afatinib can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Afatinib can be decreased when it is combined with Tacrolimus.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Afatinib.
TamoxifenThe serum concentration of Afatinib can be decreased when it is combined with Tamoxifen.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Afatinib.
Taurocholic AcidThe serum concentration of Afatinib 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 Afatinib.
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Afatinib.
TelmisartanThe serum concentration of Afatinib can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Afatinib can be increased when it is combined with Temsirolimus.
TerazosinThe serum concentration of Afatinib can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Afatinib can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Afatinib can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Afatinib can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Afatinib can be increased when it is combined with Testosterone.
TicagrelorThe serum concentration of Afatinib can be increased when it is combined with Ticagrelor.
TimololThe serum concentration of Timolol can be increased when it is combined with Afatinib.
TolvaptanThe serum concentration of Afatinib can be increased when it is combined with Tolvaptan.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Afatinib.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Afatinib.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Afatinib.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Afatinib.
TrazodoneThe serum concentration of Afatinib can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Afatinib can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Afatinib can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Afatinib can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Afatinib can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Afatinib can be increased when it is combined with Troleandomycin.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Afatinib.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Afatinib.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Afatinib.
VenlafaxineThe serum concentration of Afatinib can be increased when it is combined with Venlafaxine.
VerapamilThe serum concentration of Afatinib can be decreased when it is combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Afatinib.
VinblastineThe serum concentration of Afatinib can be decreased when it is combined with Vinblastine.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Afatinib.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Afatinib.
VincristineThe serum concentration of Afatinib can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Afatinib can be increased when it is combined with Vinorelbine.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Afatinib.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Afatinib.
ZimelidineThe serum concentration of Afatinib can be increased when it is combined with Zimelidine.
Food Interactions
  • When given with a high-fat meal, Cmax decreases by 50% and AUC by 39% relative to the fasted state.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
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
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane signaling receptor activity
Specific Function:
Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-...
Gene Name:
ERBB2
Uniprot ID:
P04626
Molecular Weight:
137909.27 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that plays an essential role as cell surface receptor for neuregulins and EGF family members and regulates development of the heart, the central nervous system and the mammary gland, gene transcription, cell proliferation, differentiation, migration and apoptosis. Required for normal cardiac muscle differentiation during embryonic development, and for postnatal cardiomyo...
Gene Name:
ERBB4
Uniprot ID:
Q15303
Molecular Weight:
146806.865 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
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
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Drug created on July 17, 2013 15:59 / Updated on September 28, 2016 02:27