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Identification
NameErlotinib
Accession NumberDB00530  (APRD00951)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionErlotinib hydrochloride (trade name Tarceva, Genentech/OSIP, originally coded as OSI-774) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer. Similar to gefitinib, erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. Erlotinib has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders.
Structure
Thumb
Synonyms
[6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)-amine
Erlotinib
OSI-774
External Identifiers
  • CP358774
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PMS-erlotinibtablet100 mgoralPharmascience Inc2016-07-28Not applicableCanada
PMS-erlotinibtablet150 mgoralPharmascience Inc2016-07-28Not applicableCanada
Tarcevatablet25 mgoralHoffmann La Roche Limited2007-01-05Not applicableCanada
Tarcevatablet25 mg/1oralGenentech, Inc.2005-04-30Not applicableUs
TarcevaFilm coated tablets25 mgOral useRoche Registration Limited2005-09-19Not applicableEu
Tarcevatablet150 mg/1oralPhysicians Total Care, Inc.2005-10-13Not applicableUs
Tarcevatablet100 mgoralHoffmann La Roche Limited2005-07-19Not applicableCanada
Tarcevatablet100 mg/1oralGenentech, Inc.2005-04-30Not applicableUs
TarcevaFilm coated tablets100 mgOral useRoche Registration Limited2005-09-19Not applicableEu
Tarcevatablet100 mg/1oralPhysicians Total Care, Inc.2005-11-21Not applicableUs
Tarcevatablet150 mgoralHoffmann La Roche Limited2005-07-19Not applicableCanada
Tarcevatablet150 mg/1oralGenentech, Inc.2005-04-30Not applicableUs
TarcevaFilm coated tablets150 mgOral useRoche Registration Limited2005-09-19Not applicableEu
Tarcevatablet100 mg/1oralAvera Mc Kennan Hospital2015-04-01Not applicableUs
Tarcevatablet25 mg/1oralPhysicians Total Care, Inc.2005-07-01Not applicableUs
Teva-erlotinibtablet100 mgoralTeva Canada Limited2014-12-08Not applicableCanada
Teva-erlotinibtablet150 mgoralTeva Canada Limited2014-12-08Not applicableCanada
Teva-erlotinibtablet25 mgoralTeva Canada Limited2014-12-08Not 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
Erlotinib Hydrochloride
183319-69-9
Thumb
  • InChI Key: GTTBEUCJPZQMDZ-UHFFFAOYSA-N
  • Monoisotopic Mass: 429.145533978
  • Average Mass: 429.897
DBSALT000064
Categories
UNIIJ4T82NDH7E
CAS number183321-74-6
WeightAverage: 393.4357
Monoisotopic: 393.168856239
Chemical FormulaC22H23N3O4
InChI KeyInChIKey=AAKJLRGGTJKAMG-UHFFFAOYSA-N
InChI
InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25)
IUPAC Name
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
SMILES
COCCOC1=C(OCCOC)C=C2C(NC3=CC=CC(=C3)C#C)=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
  • Aminopyrimidine
  • Alkyl aryl ether
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Azacycle
  • Secondary amine
  • Ether
  • Dialkyl ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Also for use, in combination with gemcitabine, as the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer.
PharmacodynamicsNot Available
Mechanism of actionThe mechanism of clinical antitumor action of erlotinib is not fully characterized. Erlotinib inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR). Specificity of inhibition with regard to other tyrosine kinase receptors has not been fully characterized. EGFR is expressed on the cell surface of normal cells and cancer cells.
Related Articles
AbsorptionErlotinib is about 60% absorbed after oral administration and its bioavailability is substantially increased by food to almost 100%. Peak plasma levels occur 4 hours after dosing. The solubility of erlotinib is pH dependent. Solubility decreases pH increases. Smoking also decrease the exposure of erlotinib.
Volume of distribution

Apparent volume of distribution = 232 L

Protein binding93% protein bound to albumin and alpha-1 acid glycoprotein (AAG)
Metabolism

Metabolism occurs in the liver. In vitro assays of cytochrome P450 metabolism showed that erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2, and the extrahepatic isoform CYP1A1.

Route of eliminationFollowing a 100 mg oral dose, 91% of the dose was recovered in which 83% was in feces (1% of the dose as unchanged parent compound) and 8% in urine (0.3% of the dose as unchanged parent compound).
Half lifeMedian half-life of 36.2 hours.
Clearance

Smokers have a 24% higher rate of erlotinib clearance.

ToxicitySymptoms of overdose include diarrhea, rash, and liver transaminase elevation. The most common adverse reactions (>50%) in NSCLC are rash, diarrhea, anorexia and fatigue. The most common adverse reactions (>50%) in pancreatic cancer are fatigue, rash, nausea and anorexia.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Erlotinib Action PathwayDrug actionSMP00472
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+0.9359
Blood Brain Barrier+0.9376
Caco-2 permeable+0.5737
P-glycoprotein substrateSubstrate0.5982
P-glycoprotein inhibitor IInhibitor0.5958
P-glycoprotein inhibitor IINon-inhibitor0.6169
Renal organic cation transporterNon-inhibitor0.7171
CYP450 2C9 substrateNon-substrate0.7942
CYP450 2D6 substrateNon-substrate0.7611
CYP450 3A4 substrateSubstrate0.5886
CYP450 1A2 substrateInhibitor0.7826
CYP450 2C9 inhibitorNon-inhibitor0.5739
CYP450 2D6 inhibitorNon-inhibitor0.6329
CYP450 2C19 inhibitorInhibitor0.598
CYP450 3A4 inhibitorInhibitor0.7194
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7911
Ames testAMES toxic0.5195
CarcinogenicityNon-carcinogens0.9551
BiodegradationNot ready biodegradable0.9907
Rat acute toxicity2.3958 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8158
hERG inhibition (predictor II)Non-inhibitor0.6776
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Osi pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Film coated tabletsOral use100 mg
Film coated tabletsOral use150 mg
Film coated tabletsOral use25 mg
Tabletoral100 mg/1
Tabletoral100 mg
Tabletoral150 mg/1
Tabletoral150 mg
Tabletoral25 mg/1
Tabletoral25 mg
Prices
Unit descriptionCostUnit
Tarceva 150 mg tablet163.98USD tablet
Tarceva 100 mg tablet144.98USD 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)
CA2216796 No2003-09-022015-06-06Canada
CA2514977 No2010-06-222024-02-11Canada
US5747498 Yes1999-05-082019-05-08Us
US6900221 Yes2001-05-092021-05-09Us
US7087613 Yes2001-05-092021-05-09Us
USRE41065 Yes1999-05-082019-05-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityVery slightly soluble (hydrochloride salt - maximal solubility of approximately 0.4 mg/mL occurs at a pH of approximately 2)Not Available
logP2.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00891 mg/mLALOGPS
logP3.13ALOGPS
logP3.2ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)16.14ChemAxon
pKa (Strongest Basic)4.59ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area74.73 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity107.79 m3·mol-1ChemAxon
Polarizability43.48 Å3ChemAxon
Number of Rings3ChemAxon
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

US5747498
General References
  1. Raymond E, Faivre S, Armand JP: Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy. Drugs. 2000;60 Suppl 1:15-23; discussion 41-2. [PubMed:11129168 ]
  2. Li Z, Xu M, Xing S, Ho WT, Ishii T, Li Q, Fu X, Zhao ZJ: Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth. J Biol Chem. 2007 Feb 9;282(6):3428-32. Epub 2006 Dec 18. [PubMed:17178722 ]
  3. Dudek AZ, Kmak KL, Koopmeiners J, Keshtgarpour M: Skin rash and bronchoalveolar histology correlates with clinical benefit in patients treated with gefitinib as a therapy for previously treated advanced or metastatic non-small cell lung cancer. Lung Cancer. 2006 Jan;51(1):89-96. Epub 2005 Nov 14. [PubMed:16290256 ]
  4. Jones HE, Goddard L, Gee JM, Hiscox S, Rubini M, Barrow D, Knowlden JM, Williams S, Wakeling AE, Nicholson RI: Insulin-like growth factor-I receptor signalling and acquired resistance to gefitinib (ZD1839; Iressa) in human breast and prostate cancer cells. Endocr Relat Cancer. 2004 Dec;11(4):793-814. [PubMed:15613453 ]
  5. Blum G, Gazit A, Levitzki A: Substrate competitive inhibitors of IGF-1 receptor kinase. Biochemistry. 2000 Dec 26;39(51):15705-12. [PubMed:11123895 ]
External Links
ATC CodesL01XE03
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (999 KB)
MSDSDownload (107 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Erlotinib can be increased when it is combined with Abiraterone.
AcetaminophenThe serum concentration of Erlotinib can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Erlotinib.
AfatinibThe serum concentration of Erlotinib can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Erlotinib can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Erlotinib can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Erlotinib can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Erlotinib can be increased when it is combined with Alfentanil.
Aluminum hydroxideThe serum concentration of Erlotinib can be decreased when it is combined with Aluminum hydroxide.
Aluminum phosphateThe serum concentration of Erlotinib can be decreased when it is combined with Aluminum phosphate.
AmantadineThe serum concentration of Erlotinib can be increased when it is combined with Amantadine.
Aminohippuric acidThe serum concentration of Erlotinib can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Erlotinib can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Erlotinib can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Erlotinib can be increased when it is combined with Amlodipine.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Erlotinib.
AmprenavirThe serum concentration of Erlotinib can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Erlotinib can be increased when it is combined with Amsacrine.
AprepitantThe serum concentration of Erlotinib can be increased when it is combined with Aprepitant.
ArtemetherThe metabolism of Erlotinib can be decreased when combined with Artemether.
AsenapineThe serum concentration of Erlotinib can be decreased when it is combined with Asenapine.
AstemizoleThe serum concentration of Erlotinib can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Erlotinib can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Erlotinib can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Erlotinib can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Erlotinib can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Erlotinib can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Erlotinib can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Erlotinib can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Erlotinib can be increased when it is combined with Bepridil.
BetaxololThe metabolism of Erlotinib can be decreased when combined with Betaxolol.
BevacizumabBevacizumab may increase the cardiotoxic activities of Erlotinib.
BexaroteneThe serum concentration of Erlotinib can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Erlotinib can be increased when it is combined with Biperiden.
Bismuth SubcitrateThe serum concentration of Erlotinib can be decreased when it is combined with Bismuth Subcitrate.
BoceprevirThe serum concentration of Erlotinib can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Erlotinib can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Erlotinib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Erlotinib can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Erlotinib can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Erlotinib can be increased when it is combined with Buprenorphine.
BupropionThe metabolism of Erlotinib can be decreased when combined with Bupropion.
BuspironeThe serum concentration of Erlotinib can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Erlotinib can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Erlotinib can be increased when it is combined with Caffeine.
Calcium carbonateThe serum concentration of Erlotinib can be decreased when it is combined with Calcium carbonate.
CanagliflozinThe serum concentration of Erlotinib can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Erlotinib can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Erlotinib can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Erlotinib can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Erlotinib can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Erlotinib can be increased when it is combined with Caspofungin.
CelecoxibThe metabolism of Erlotinib can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Erlotinib can be increased when it is combined with Ceritinib.
ChloroquineThe serum concentration of Erlotinib can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Erlotinib can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Erlotinib can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Erlotinib can be increased when it is combined with Chlorprothixene.
CholecalciferolThe metabolism of Erlotinib can be decreased when combined with Cholecalciferol.
CholesterolThe serum concentration of Erlotinib can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Erlotinib can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Erlotinib can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Erlotinib can be decreased when it is combined with Cimetidine.
CinacalcetThe metabolism of Erlotinib can be decreased when combined with Cinacalcet.
CiprofloxacinThe serum concentration of Erlotinib can be increased when it is combined with Ciprofloxacin.
CitalopramThe serum concentration of Erlotinib can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Erlotinib can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Erlotinib can be decreased when combined with Clemastine.
ClobazamThe metabolism of Erlotinib can be decreased when combined with Clobazam.
ClofazimineThe serum concentration of Erlotinib can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Erlotinib can be increased when it is combined with Clomipramine.
ClopidogrelThe metabolism of Erlotinib can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Erlotinib can be decreased when combined with Clotrimazole.
ClozapineThe metabolism of Erlotinib can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Erlotinib can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Erlotinib can be decreased when combined with Cocaine.
ColchicineThe serum concentration of Erlotinib can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Erlotinib can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Erlotinib can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Erlotinib can be decreased when combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Erlotinib.
CyclosporineThe metabolism of Erlotinib can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Erlotinib can be decreased when it is combined with Cyproterone acetate.
DabrafenibThe serum concentration of Erlotinib can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Erlotinib can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Erlotinib can be increased when it is combined with Dactinomycin.
DarifenacinThe metabolism of Erlotinib can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Erlotinib can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Erlotinib can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Erlotinib can be decreased when it is combined with Daunorubicin.
DeferasiroxThe serum concentration of Erlotinib can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Erlotinib can be decreased when combined with Delavirdine.
DesipramineThe serum concentration of Erlotinib can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Erlotinib.
DesloratadineThe serum concentration of Erlotinib can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Erlotinib can be decreased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Erlotinib can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Erlotinib can be increased when it is combined with Diclofenac.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Erlotinib.
DigoxinDigoxin may decrease the cardiotoxic activities of Erlotinib.
DihydroergotamineThe metabolism of Erlotinib can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Erlotinib can be decreased when combined with Diltiazem.
DiphenhydramineThe metabolism of Erlotinib can be decreased when combined with Diphenhydramine.
DipyridamoleThe serum concentration of Erlotinib can be increased when it is combined with Dipyridamole.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Erlotinib.
DoxazosinThe serum concentration of Erlotinib can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Erlotinib can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Erlotinib can be decreased when it is combined with Doxorubicin.
DoxycyclineThe metabolism of Erlotinib can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Erlotinib can be increased when it is combined with Dronabinol.
DronedaroneThe metabolism of Erlotinib can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Erlotinib can be decreased when combined with Duloxetine.
EfavirenzThe serum concentration of Erlotinib can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Erlotinib can be increased when it is combined with Elbasvir.
EliglustatThe metabolism of Erlotinib can be decreased when combined with Eliglustat.
EnalaprilThe serum concentration of Erlotinib can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Erlotinib can be increased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Erlotinib can be decreased when it is combined with Epinastine.
ErgonovineThe serum concentration of Erlotinib can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Erlotinib can be increased when it is combined with Ergotamine.
ErythromycinThe metabolism of Erlotinib can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Erlotinib can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe serum concentration of Erlotinib can be decreased when it is combined with Esomeprazole.
EstramustineThe serum concentration of Erlotinib can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Erlotinib can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Erlotinib can be decreased when it is combined with Estrone.
EtoposideThe serum concentration of Erlotinib can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Erlotinib can be decreased when it is combined with Etravirine.
FamotidineThe serum concentration of Erlotinib can be decreased when it is combined with Famotidine.
FelodipineThe serum concentration of Erlotinib can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Erlotinib can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Erlotinib can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Erlotinib can be increased when it is combined with Fidaxomicin.
FluconazoleThe metabolism of Erlotinib can be decreased when combined with Fluconazole.
FluoxetineThe serum concentration of Erlotinib can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Erlotinib can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Erlotinib can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Erlotinib can be increased when it is combined with Flurazepam.
FluvoxamineThe metabolism of Erlotinib can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Erlotinib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Erlotinib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Erlotinib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Erlotinib can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Erlotinib can be increased when it is combined with Gefitinib.
GemfibrozilThe metabolism of Erlotinib can be decreased when combined with Gemfibrozil.
GenisteinThe serum concentration of Erlotinib can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Erlotinib can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Erlotinib can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Erlotinib can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Erlotinib can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Erlotinib can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Erlotinib can be increased when it is combined with Hydrocortisone.
IdelalisibThe serum concentration of Erlotinib can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Erlotinib can be decreased when combined with Imatinib.
ImipramineThe serum concentration of Erlotinib can be increased when it is combined with Imipramine.
IndinavirThe serum concentration of Erlotinib can be decreased when it is combined with Indinavir.
IndomethacinThe serum concentration of Erlotinib can be increased when it is combined with Indomethacin.
IrbesartanThe metabolism of Erlotinib can be decreased when combined with Irbesartan.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Erlotinib.
IsavuconazoniumThe metabolism of Erlotinib can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Erlotinib can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Erlotinib can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Erlotinib can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Erlotinib can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Erlotinib can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Erlotinib can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of Erlotinib can be increased when it is combined with Ketoconazole.
LansoprazoleThe serum concentration of Erlotinib can be decreased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Erlotinib can be increased when it is combined with Lapatinib.
LevofloxacinThe serum concentration of Erlotinib can be increased when it is combined with Levofloxacin.
LevothyroxineThe serum concentration of Erlotinib can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Erlotinib can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Erlotinib can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Erlotinib can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Erlotinib can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Erlotinib can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Erlotinib can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Erlotinib can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Erlotinib can be increased when it is combined with Loratadine.
LorcaserinThe metabolism of Erlotinib can be decreased when combined with Lorcaserin.
LosartanThe serum concentration of Erlotinib can be increased when it is combined with Losartan.
LovastatinThe metabolism of Erlotinib can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Erlotinib can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Erlotinib can be decreased when it is combined with Lumacaftor.
LumefantrineThe metabolism of Erlotinib can be decreased when combined with Lumefantrine.
MagaldrateThe serum concentration of Erlotinib can be decreased when it is combined with Magaldrate.
Magnesium carbonateThe serum concentration of Erlotinib can be decreased when it is combined with Magnesium carbonate.
Magnesium hydroxideThe serum concentration of Erlotinib can be decreased when it is combined with Magnesium hydroxide.
Magnesium oxideThe serum concentration of Erlotinib can be decreased when it is combined with Magnesium oxide.
Magnesium TrisilicateThe serum concentration of Erlotinib can be decreased when it is combined with Magnesium Trisilicate.
MaprotilineThe serum concentration of Erlotinib can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Erlotinib can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Erlotinib can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Erlotinib can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Erlotinib can be increased when it is combined with Meprobamate.
MethadoneThe serum concentration of Erlotinib can be increased when it is combined with Methadone.
MethanthelineThe serum concentration of Erlotinib can be decreased when it is combined with Methantheline.
MethotrimeprazineThe metabolism of Erlotinib can be decreased when combined with Methotrimeprazine.
MetiamideThe serum concentration of Erlotinib can be decreased when it is combined with Metiamide.
MetoprololThe serum concentration of Erlotinib can be increased when it is combined with Metoprolol.
MexiletineThe metabolism of Erlotinib can be decreased when combined with Mexiletine.
MibefradilThe serum concentration of Erlotinib can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Erlotinib can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Erlotinib can be decreased when it is combined with Midazolam.
MifepristoneThe metabolism of Erlotinib can be decreased when combined with Mifepristone.
MirabegronThe metabolism of Erlotinib can be decreased when combined with Mirabegron.
MitomycinThe serum concentration of Erlotinib can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Erlotinib can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Erlotinib can be decreased when it is combined with Mitoxantrone.
ModafinilThe serum concentration of Erlotinib can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Erlotinib can be increased when it is combined with Morphine.
NafcillinThe serum concentration of Erlotinib can be decreased when it is combined with Nafcillin.
NaltrexoneThe serum concentration of Erlotinib can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Erlotinib can be increased when it is combined with Naringenin.
NefazodoneThe serum concentration of Erlotinib can be decreased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Erlotinib can be decreased when it is combined with Nelfinavir.
NeostigmineThe serum concentration of Erlotinib can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Erlotinib can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Erlotinib can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Erlotinib can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Erlotinib can be decreased when it is combined with Nifedipine.
NilotinibThe metabolism of Erlotinib can be decreased when combined with Nilotinib.
NisoldipineThe serum concentration of Erlotinib can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Erlotinib can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Erlotinib can be increased when it is combined with Nitrendipine.
NizatidineThe serum concentration of Erlotinib can be decreased when it is combined with Nizatidine.
NorethisteroneThe serum concentration of Erlotinib can be decreased when it is combined with Norethisterone.
OlanzapineThe serum concentration of Erlotinib can be decreased when it is combined with Olanzapine.
OlaparibThe metabolism of Erlotinib can be decreased when combined with Olaparib.
OmeprazoleThe serum concentration of Erlotinib can be decreased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Erlotinib can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Erlotinib.
P-NitrophenolThe serum concentration of Erlotinib can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Erlotinib can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Erlotinib can be increased when it is combined with Palbociclib.
Palmitic AcidThe serum concentration of Erlotinib can be increased when it is combined with Palmitic Acid.
PanobinostatThe metabolism of Erlotinib can be decreased when combined with Panobinostat.
PantoprazoleThe serum concentration of Erlotinib can be decreased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Erlotinib can be increased when it is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Erlotinib.
Peginterferon alfa-2bThe serum concentration of Erlotinib can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe serum concentration of Erlotinib can be decreased when it is combined with Pentobarbital.
PerindoprilThe serum concentration of Erlotinib can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Erlotinib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Erlotinib can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Erlotinib can be increased when it is combined with Pimozide.
PioglitazoneThe metabolism of Erlotinib can be decreased when combined with Pioglitazone.
Platelet Activating FactorThe serum concentration of Erlotinib can be decreased when it is combined with Platelet Activating Factor.
PonatinibThe serum concentration of Erlotinib can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Erlotinib can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Erlotinib can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Erlotinib can be increased when it is combined with Prazosin.
PrednisoneThe serum concentration of Erlotinib can be increased when it is combined with Prednisone.
PrimidoneThe serum concentration of Erlotinib can be decreased when it is combined with Primidone.
ProbenecidThe serum concentration of Erlotinib can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Erlotinib can be decreased when it is combined with Progesterone.
PromazineThe metabolism of Erlotinib can be decreased when combined with Promazine.
PromethazineThe serum concentration of Erlotinib can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Erlotinib can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Erlotinib can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Erlotinib can be increased when it is combined with Protriptyline.
QuercetinThe serum concentration of Erlotinib can be increased when it is combined with Quercetin.
QuinacrineThe serum concentration of Erlotinib can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Erlotinib can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Erlotinib can be increased when it is combined with Quinine.
RabeprazoleThe serum concentration of Erlotinib can be decreased when it is combined with Rabeprazole.
RanitidineThe serum concentration of Erlotinib can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Erlotinib can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Erlotinib can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Erlotinib can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Erlotinib can be decreased when it is combined with Reserpine.
RifabutinThe serum concentration of Erlotinib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Erlotinib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Erlotinib can be decreased when it is combined with Rifapentine.
RilpivirineThe serum concentration of Erlotinib can be increased when it is combined with Rilpivirine.
RitonavirThe serum concentration of Erlotinib can be decreased when it is combined with Ritonavir.
RolapitantThe serum concentration of Erlotinib can be increased when it is combined with Rolapitant.
RopiniroleThe metabolism of Erlotinib can be decreased when combined with Ropinirole.
RosiglitazoneThe metabolism of Erlotinib can be decreased when combined with Rosiglitazone.
Roxatidine acetateThe serum concentration of Erlotinib can be decreased when it is combined with Roxatidine acetate.
SaquinavirThe serum concentration of Erlotinib can be decreased when it is combined with Saquinavir.
ScopolamineThe serum concentration of Erlotinib can be increased when it is combined with Scopolamine.
SecobarbitalThe metabolism of Erlotinib can be increased when combined with Secobarbital.
SelegilineThe serum concentration of Erlotinib can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Erlotinib can be increased when it is combined with Sertraline.
SildenafilThe metabolism of Erlotinib can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Erlotinib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Erlotinib can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Erlotinib can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Erlotinib can be decreased when it is combined with Sirolimus.
SorafenibThe serum concentration of Erlotinib can be increased when it is combined with Sorafenib.
SpironolactoneThe serum concentration of Erlotinib can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Erlotinib can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Erlotinib can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Erlotinib can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Erlotinib can be decreased when it is combined with Streptozocin.
SulfamethoxazoleThe metabolism of Erlotinib can be decreased when combined with Sulfamethoxazole.
SulfinpyrazoneThe serum concentration of Erlotinib can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe metabolism of Erlotinib can be decreased when combined with Sulfisoxazole.
SumatriptanThe serum concentration of Erlotinib can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Erlotinib can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Erlotinib can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Erlotinib can be decreased when it is combined with Tacrolimus.
TAK-390MRThe serum concentration of Erlotinib can be decreased when it is combined with TAK-390MR.
TamoxifenThe serum concentration of Erlotinib can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Erlotinib can be increased when it is combined with Taurocholic Acid.
TelaprevirThe serum concentration of Erlotinib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Erlotinib can be increased when it is combined with Telithromycin.
TelmisartanThe serum concentration of Erlotinib can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Erlotinib can be increased when it is combined with Temsirolimus.
TenofovirThe metabolism of Erlotinib can be decreased when combined with Tenofovir.
TerazosinThe serum concentration of Erlotinib can be increased when it is combined with Terazosin.
TerbinafineThe metabolism of Erlotinib can be decreased when combined with Terbinafine.
TerfenadineThe serum concentration of Erlotinib can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Erlotinib can be decreased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Erlotinib can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Erlotinib can be increased when it is combined with Testosterone.
TheophyllineThe metabolism of Erlotinib can be decreased when combined with Theophylline.
ThioridazineThe metabolism of Erlotinib can be decreased when combined with Thioridazine.
TicagrelorThe serum concentration of Erlotinib can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Erlotinib can be decreased when combined with Ticlopidine.
TipranavirThe metabolism of Erlotinib can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Erlotinib can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Erlotinib can be increased when it is combined with Tolvaptan.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Erlotinib.
TranylcypromineThe metabolism of Erlotinib can be decreased when combined with Tranylcypromine.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Erlotinib.
TrazodoneThe serum concentration of Erlotinib can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Erlotinib can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Erlotinib can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Erlotinib can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Erlotinib can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Erlotinib can be increased when it is combined with Troleandomycin.
VemurafenibThe serum concentration of Erlotinib can be increased when it is combined with Vemurafenib.
VenlafaxineThe metabolism of Erlotinib can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Erlotinib can be decreased when combined with Verapamil.
VinblastineThe serum concentration of Erlotinib can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Erlotinib can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Erlotinib can be increased when it is combined with Vinorelbine.
VoriconazoleThe serum concentration of Erlotinib can be increased when it is combined with Voriconazole.
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Erlotinib.
ZimelidineThe serum concentration of Erlotinib can be increased when it is combined with Zimelidine.
ZiprasidoneThe metabolism of Erlotinib can be decreased when combined with Ziprasidone.
Food Interactions
  • Take at least 1 hour before or 2 hours after any food.
  • Take with a glass of water.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Ubiquitin protein ligase binding
Specific Function:
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TGFA/TGF-alpha, amphiregulin, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on ke...
Gene Name:
EGFR
Uniprot ID:
P00533
Molecular Weight:
134276.185 Da
References
  1. Kim TE, Murren JR: Erlotinib OSI/Roche/Genentech. Curr Opin Investig Drugs. 2002 Sep;3(9):1385-95. [PubMed:12498017 ]
  2. Laird AD, Cherrington JM: Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents. Expert Opin Investig Drugs. 2003 Jan;12(1):51-64. [PubMed:12517254 ]
  3. Delbaldo C, Faivre S, Raymond E: [Epidermal growth factor inhibitors]. Rev Med Interne. 2003 Jun;24(6):372-83. [PubMed:12814826 ]
  4. Bulgaru AM, Mani S, Goel S, Perez-Soler R: Erlotinib (Tarceva): a promising drug targeting epidermal growth factor receptor tyrosine kinase. Expert Rev Anticancer Ther. 2003 Jun;3(3):269-79. [PubMed:12820772 ]
  5. Akita RW, Sliwkowski MX: Preclinical studies with Erlotinib (Tarceva). Semin Oncol. 2003 Jun;30(3 Suppl 7):15-24. [PubMed:12840797 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and is...
Gene Name:
NR1I2
Uniprot ID:
O75469
Molecular Weight:
49761.245 Da
References
  1. Harmsen S, Meijerman I, Beijnen JH, Schellens JH: Nuclear receptor mediated induction of cytochrome P450 3A4 by anticancer drugs: a key role for the pregnane X receptor. Cancer Chemother Pharmacol. 2009 Jun;64(1):35-43. doi: 10.1007/s00280-008-0842-3. Epub 2008 Oct 7. [PubMed:18839173 ]
  2. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]

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. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. Johnson JR, Cohen M, Sridhara R, Chen YF, Williams GM, Duan J, Gobburu J, Booth B, Benson K, Leighton J, Hsieh LS, Chidambaram N, Zimmerman P, Pazdur R: Approval summary for erlotinib for treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Clin Cancer Res. 2005 Sep 15;11(18):6414-21. [PubMed:16166415 ]
  3. 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 ]
  4. Hamilton M, Wolf JL, Rusk J, Beard SE, Clark GM, Witt K, Cagnoni PJ: Effects of smoking on the pharmacokinetics of erlotinib. Clin Cancer Res. 2006 Apr 1;12(7 Pt 1):2166-71. [PubMed:16609030 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. 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
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. Lu JF, Eppler SM, Wolf J, Hamilton M, Rakhit A, Bruno R, Lum BL: Clinical pharmacokinetics of erlotinib in patients with solid tumors and exposure-safety relationship in patients with non-small cell lung cancer. Clin Pharmacol Ther. 2006 Aug;80(2):136-45. [PubMed:16890575 ]
  3. Johnson JR, Cohen M, Sridhara R, Chen YF, Williams GM, Duan J, Gobburu J, Booth B, Benson K, Leighton J, Hsieh LS, Chidambaram N, Zimmerman P, Pazdur R: Approval summary for erlotinib for treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Clin Cancer Res. 2005 Sep 15;11(18):6414-21. [PubMed:16166415 ]
  4. 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 ]
  5. Hamilton M, Wolf JL, Rusk J, Beard SE, Clark GM, Witt K, Cagnoni PJ: Effects of smoking on the pharmacokinetics of erlotinib. Clin Cancer Res. 2006 Apr 1;12(7 Pt 1):2166-71. [PubMed:16609030 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. Johnson JR, Cohen M, Sridhara R, Chen YF, Williams GM, Duan J, Gobburu J, Booth B, Benson K, Leighton J, Hsieh LS, Chidambaram N, Zimmerman P, Pazdur R: Approval summary for erlotinib for treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Clin Cancer Res. 2005 Sep 15;11(18):6414-21. [PubMed:16166415 ]
  3. 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
substrate
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. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. 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:
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. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. Hamilton M, Wolf JL, Rusk J, Beard SE, Clark GM, Witt K, Cagnoni PJ: Effects of smoking on the pharmacokinetics of erlotinib. Clin Cancer Res. 2006 Apr 1;12(7 Pt 1):2166-71. [PubMed:16609030 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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, retinoid and xenobiotics. Preferentially oxidizes 17beta-estradiol to the carcinogenic 4-hydroxy derivative, and a variety of procarcinogenic compou...
Gene Name:
CYP1B1
Uniprot ID:
Q16678
Molecular Weight:
60845.33 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. 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
inhibitor
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da
References
  1. Liu Y, Ramirez J, House L, Ratain MJ: The UGT1A1*28 polymorphism correlates with erlotinib's effect on SN-38 glucuronidation. Eur J Cancer. 2010 Jul;46(11):2097-103. doi: 10.1016/j.ejca.2010.04.022. Epub 2010 May 23. [PubMed:20580994 ]

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
inhibitor
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. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Marchetti S, de Vries NA, Buckle T, Bolijn MJ, van Eijndhoven MA, Beijnen JH, Mazzanti R, van Tellingen O, Schellens JH: Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice. Mol Cancer Ther. 2008 Aug;7(8):2280-7. doi: 10.1158/1535-7163.MCT-07-2250. [PubMed:18723475 ]
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Drug created on June 13, 2005 07:24 / Updated on September 24, 2016 03:31