Details of the Drug

General Information of Drug (ID: DMCMBHA)

Drug Name
Erlotinib
Synonyms
Erlotinin; Tarceva; Erlotinib Base; OSI 744; R 1415; CP 358,774; CP-358774; Erlotinib(Tarceva); Tarceva (TN); CP-358,774; Erlotinib, OS-774; N-(3-ethynylphenyl)[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amine; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine; N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-Quinazolinamine; [6,7-BIS(2-METHOXY-ETHOXY)QUINAZOLINE-4-YL]-(3-ETHYNYLPHENYL)AMINE; [6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)-amine; 4-[(3-Ethynylphenyl)amino]-6,7-bis(2-methoxyethoxy)quinazoline; 4-[(3-ethynylphenyl)amino]-6,7-bis(2-methoxyethoxy)quinazoline
Indication
Disease Entry ICD 11 Status REF
Non-small-cell lung cancer 2C25.Y Approved [1], [2]
Pancreatic cancer 2C10 Phase 3 [1], [3]
Colon cancer 2B90.Z Phase 2 [1], [3]
Therapeutic Class
Anticancer Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 393.4
Topological Polar Surface Area (xlogp) 3.3
Rotatable Bond Count (rotbonds) 11
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Bioavailability
59% of drug becomes completely available to its intended biological destination(s) [5]
Clearance
The drug present in the plasma can be removed from the body at the rate of 1.69 mL/min/kg [6]
Elimination
0.3% of drug is excreted from urine in the unchanged form [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 36.2 hours [6]
Metabolism
The drug is metabolized via the liver [7]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 5.446 micromolar/kg/day [8]
Unbound Fraction
The unbound fraction of drug in plasma is 0.07% [6]
Vd
The volume of distribution (Vd) of drug is 232 L [9]
Water Solubility
The ability of drug to dissolve in water is measured as 0.4 mg/mL [4]
Chemical Identifiers
Formula
C22H23N3O4
IUPAC Name
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
Canonical SMILES
COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC
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)
InChIKey
AAKJLRGGTJKAMG-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
176870
ChEBI ID
CHEBI:114785
CAS Number
183321-74-6
DrugBank ID
DB00530
TTD ID
D07POC
VARIDT ID
DR00558
INTEDE ID
DR0603
ACDINA ID
D00239

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [10]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [11]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [12]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [13]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [14]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [14]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [14]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Non-small-cell lung cancer
ICD Disease Classification 2C25.Y
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Epidermal growth factor receptor (EGFR) DTT EGFR 5.84E-05 0.32 0.55
P-glycoprotein 1 (ABCB1) DTP P-GP 1.42E-02 -2.10E-01 -5.11E-01
Breast cancer resistance protein (ABCG2) DTP BCRP 1.07E-06 -3.94E-01 -6.94E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 7.26E-01 -3.16E-02 -1.31E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 2.45E-13 -2.29E+00 -1.44E+00
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 1.14E-01 -7.61E-02 -3.24E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 5.04E-04 -9.90E-02 -3.91E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Erlotinib
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Porfimer Sodium DM7ZWNY Moderate Increased risk of photosensitivity reactions by the combination of Erlotinib and Porfimer Sodium. Lung cancer [2C25] [75]
Ceritinib DMB920Z Moderate Decreased metabolism of Erlotinib caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [76]
PF-06463922 DMKM7EW Moderate Increased metabolism of Erlotinib caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [76]
Capmatinib DMYCXKL Moderate Decreased clearance of Erlotinib due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [77]
Coadministration of a Drug Treating the Disease Different from Erlotinib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [78]
Sodium bicarbonate DMMU6BJ Moderate Decreased absorption of Erlotinib due to altered gastric pH caused by Sodium bicarbonate. Acidosis [5C73] [78]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Erlotinib caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [76]
Midostaurin DMI6E0R Moderate Decreased clearance of Erlotinib due to the transporter inhibition by Midostaurin. Acute myeloid leukaemia [2A60] [79]
Arn-509 DMT81LZ Moderate Increased metabolism of Erlotinib caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [76]
Mitotane DMU1GX0 Moderate Increased metabolism of Erlotinib caused by Mitotane mediated induction of CYP450 enzyme. Adrenal cancer [2D11] [76]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [80]
Methylphenobarbital DMDSWAG Moderate Increased metabolism of Erlotinib caused by Methylphenobarbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [76]
Voriconazole DMAOL2S Moderate Decreased metabolism of Erlotinib caused by Voriconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [76]
Posaconazole DMUL5EW Moderate Decreased metabolism of Erlotinib caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [76]
Ciprofloxacin XR DM2NLS9 Moderate Decreased metabolism of Erlotinib caused by Ciprofloxacin XR mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [81]
Clarithromycin DM4M1SG Moderate Decreased metabolism of Erlotinib caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [76]
Rabeprazole DMMZXIW Major Decreased absorption of Erlotinib due to altered gastric pH caused by Rabeprazole. Bacterial infection [1A00-1C4Z] [78]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Erlotinib caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [76]
Telithromycin DMZ4P3A Moderate Decreased metabolism of Erlotinib caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [76]
Erdafitinib DMI782S Moderate Decreased clearance of Erlotinib due to the transporter inhibition by Erdafitinib. Bladder cancer [2C94] [82]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Erlotinib and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [83]
Lapatinib DM3BH1Y Moderate Decreased metabolism of Erlotinib caused by Lapatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [84]
Tucatinib DMBESUA Moderate Decreased metabolism of Erlotinib caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [76]
PF-04449913 DMSB068 Moderate Decreased clearance of Erlotinib due to the transporter inhibition by PF-04449913. Chronic myelomonocytic leukaemia [2A40] [79]
Phenylbutazone DMAYL0T Moderate Increased metabolism of Erlotinib caused by Phenylbutazone mediated induction of CYP450 enzyme. Chronic pain [MG30] [76]
Anisindione DM2C48U Moderate Increased plasma concentration of Erlotinib and Anisindione due to competitive binding of plasma proteins. Coagulation defect [3B10] [81]
Lumacaftor DMCLWDJ Moderate Increased metabolism of Erlotinib caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [76]
Ivacaftor DMZC1HS Moderate Decreased clearance of Erlotinib due to the transporter inhibition by Ivacaftor. Cystic fibrosis [CA25] [85]
MK-8228 DMOB58Q Moderate Decreased metabolism of Erlotinib caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [86]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Erlotinib caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [76]
SODIUM CITRATE DMHPD2Y Moderate Decreased absorption of Erlotinib due to altered gastric pH caused by SODIUM CITRATE. Discovery agent [N.A.] [78]
Primidone DM0WX6I Moderate Increased metabolism of Erlotinib caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [76]
Felbamate DM1V5ZS Moderate Increased metabolism of Erlotinib caused by Felbamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [76]
Oxcarbazepine DM5PU6O Moderate Increased metabolism of Erlotinib caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [76]
Cenobamate DMGOVHA Moderate Increased metabolism of Erlotinib caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [76]
Stiripentol DMMSDOY Moderate Decreased metabolism of Erlotinib caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [76]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Erlotinib caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [76]
Phenobarbital DMXZOCG Moderate Increased metabolism of Erlotinib caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [76]
Carbamazepine DMZOLBI Moderate Increased metabolism of Erlotinib caused by Carbamazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [76]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Erlotinib caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [76]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Cannabidiol. Epileptic encephalopathy [8A62] [79]
Tazemetostat DMWP1BH Moderate Increased metabolism of Erlotinib caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [76]
Itraconazole DMCR1MV Moderate Decreased metabolism of Erlotinib caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [76]
Miconazole DMPMYE8 Moderate Decreased metabolism of Erlotinib caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [76]
Ketoconazole DMPZI3Q Moderate Decreased metabolism of Erlotinib caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [76]
Dexlansoprazole DM1DBV5 Major Decreased absorption of Erlotinib due to altered gastric pH caused by Dexlansoprazole. Gastro-oesophageal reflux disease [DA22] [78]
Nizatidine DMGFV3Z Moderate Decreased absorption of Erlotinib due to altered gastric pH caused by Nizatidine. Gastro-oesophageal reflux disease [DA22] [78]
Sulfinpyrazone DMEV954 Moderate Increased metabolism of Erlotinib caused by Sulfinpyrazone mediated induction of CYP450 enzyme. Gout [FA25] [76]
Boceprevir DMBSHMF Moderate Decreased metabolism of Erlotinib caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [76]
Telaprevir DMMRV29 Moderate Decreased metabolism of Erlotinib caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [76]
GS-5885 DMSL3DX Moderate Decreased clearance of Erlotinib due to the transporter inhibition by GS-5885. Hepatitis virus infection [1E50-1E51] [87]
Isoniazid DM5JVS3 Moderate Decreased metabolism of Erlotinib caused by Isoniazid mediated inhibition of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [81]
Rifampin DMA8J1G Moderate Increased metabolism of Erlotinib caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [76]
Rifapentine DMCHV4I Moderate Increased metabolism of Erlotinib caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [76]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Brentuximab vedotin. Hodgkin lymphoma [2B30] [88]
Delavirdine DM3NF5G Moderate Decreased metabolism of Erlotinib caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [76]
Fosamprenavir DM4W9B3 Moderate Decreased metabolism of Erlotinib caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [76]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Erlotinib caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [76]
Efavirenz DMC0GSJ Moderate Increased metabolism of Erlotinib caused by Efavirenz mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [76]
Saquinavir DMG814N Moderate Decreased metabolism of Erlotinib caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [76]
Etravirine DMGV8QU Moderate Increased metabolism of Erlotinib caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [76]
Amprenavir DMLMXE0 Moderate Decreased metabolism of Erlotinib caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [76]
Darunavir DMN3GCH Moderate Decreased metabolism of Erlotinib caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [89]
Atazanavir DMSYRBX Moderate Decreased metabolism of Erlotinib caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [76]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Erlotinib and Mipomersen. Hyper-lipoproteinaemia [5C80] [90]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Erlotinib and Teriflunomide. Hyper-lipoproteinaemia [5C80] [91]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Erlotinib and BMS-201038. Hyper-lipoproteinaemia [5C80] [92]
Sodium zirconium cyclosilicate DMCSLZ4 Moderate Decreased absorption of Erlotinib due to altered gastric pH caused by Sodium zirconium cyclosilicate. Hyperkalaemia [5C76] [79]
Verapamil DMA7PEW Moderate Decreased metabolism of Erlotinib caused by Verapamil mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [81]
Conivaptan DM1V329 Moderate Decreased metabolism of Erlotinib caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [76]
Tolvaptan DMIWFRL Moderate Decreased clearance of Erlotinib due to the transporter inhibition by Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [78]
Amobarbital DM0GQ8N Moderate Increased metabolism of Erlotinib caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [76]
Methotrexate DM2TEOL Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Methotrexate. Leukaemia [2A60-2B33] [79]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [93]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Idelalisib. Mature B-cell leukaemia [2A82] [94]
IPI-145 DMWA24P Moderate Decreased metabolism of Erlotinib caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [95]
Clofarabine DMCVJ86 Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Clofarabine. Mature B-cell lymphoma [2A85] [96]
Ibrutinib DMHZCPO Moderate Decreased clearance of Erlotinib due to the transporter inhibition by Ibrutinib. Mature B-cell lymphoma [2A85] [79]
Vemurafenib DM62UG5 Moderate Increased metabolism of Erlotinib caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [76]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Erlotinib caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [76]
Lasmiditan DMXLVDT Moderate Decreased clearance of Erlotinib due to the transporter inhibition by Lasmiditan. Migraine [8A80] [97]
Exjade DMHPRWG Moderate Increased metabolism of Erlotinib caused by Exjade mediated induction of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [76]
Rifabutin DM1YBHK Moderate Increased metabolism of Erlotinib caused by Rifabutin mediated induction of CYP450 enzyme. Mycobacterium infection [1B10-1B21] [76]
Methoxsalen DME8FZ9 Moderate Increased risk of photosensitivity reactions by the combination of Erlotinib and Methoxsalen. Mycosis fungoides [2B01] [78]
Nilotinib DM7HXWT Moderate Decreased metabolism of Erlotinib caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [98]
Dasatinib DMJV2EK Moderate Decreased metabolism of Erlotinib caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [99]
Omacetaxine mepesuccinate DMPU2WX Moderate Additive immunosuppressive effects by the combination of Erlotinib and Omacetaxine mepesuccinate. Myeloproliferative neoplasm [2A20] [100]
Modafinil DMYILBE Minor Increased metabolism of Erlotinib caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [101]
Rolapitant DM8XP26 Moderate Decreased clearance of Erlotinib due to the transporter inhibition by Rolapitant. Nausea/vomiting [MD90] [102]
Abametapir DM2RX0I Moderate Decreased metabolism of Erlotinib caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [103]
Ranitidine DM0GUSX Moderate Decreased absorption of Erlotinib due to altered gastric pH caused by Ranitidine. Peptic ulcer [DA61] [78]
Esomeprazole DM7BN0X Major Decreased absorption of Erlotinib due to altered gastric pH caused by Esomeprazole. Peptic ulcer [DA61] [78]
Famotidine DMRL3AB Moderate Decreased absorption of Erlotinib due to altered gastric pH caused by Famotidine. Peptic ulcer [DA61] [78]
Lefamulin DME6G97 Moderate Decreased metabolism of Erlotinib caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [104]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Erlotinib caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [76]
Enzalutamide DMGL19D Moderate Increased metabolism of Erlotinib caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [76]
Bosentan DMIOGBU Moderate Increased metabolism of Erlotinib caused by Bosentan mediated induction of CYP450 enzyme. Pulmonary hypertension [BB01] [76]
Riociguat DMXBLMP Moderate Decreased metabolism of Erlotinib caused by Riociguat mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [91]
Dexamethasone DMMWZET Moderate Increased metabolism of Erlotinib caused by Dexamethasone mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [76]
Nafcillin DMN9RPO Moderate Increased metabolism of Erlotinib caused by Nafcillin mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [76]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Erlotinib and Leflunomide. Rheumatoid arthritis [FA20] [91]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Erlotinib caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [79]
Larotrectinib DM26CQR Moderate Decreased metabolism of Erlotinib caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [78]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [79]
Armodafinil DMGB035 Minor Increased metabolism of Erlotinib caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [101]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Erlotinib and Naltrexone. Substance abuse [6C40] [105]
Warfarin DMJYCVW Moderate Increased plasma concentrations of Erlotinib and Warfarin due to competitive inhibition of the same metabolic pathway. Supraventricular tachyarrhythmia [BC81] [81]
Fostamatinib DM6AUHV Moderate Decreased clearance of Erlotinib due to the transporter inhibition by Fostamatinib. Thrombocytopenia [3B64] [106]
Elagolix DMB2C0E Moderate Increased metabolism of Erlotinib caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [76]
Amiodarone DMUTEX3 Moderate Decreased metabolism of Erlotinib caused by Amiodarone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [81]
⏷ Show the Full List of 106 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF E00255 17730 Colorant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Erlotinib 25 mg tablet 25 mg Oral Tablet Oral
Erlotinib 100 mg tablet 100 mg Oral Tablet Oral
Erlotinib 150 mg tablet 150 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4920).
2 2004 approvals: the demise of the blockbuster. Nat Rev Drug Discov. 2005 Feb;4(2):93-4.
3 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
4 BDDCS applied to over 900 drugs
5 Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
6 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
7 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
8 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
9 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
10 Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
11 Functions of the breast cancer resistance protein (BCRP/ABCG2) in chemotherapy. Adv Drug Deliv Rev. 2009 Jan 31;61(1):26-33.
12 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.
13 In vitro assessment of time-dependent inhibitory effects on CYP2C8 and CYP3A activity by fourteen protein kinase inhibitors. Drug Metab Dispos. 2014 Jul;42(7):1202-9.
14 Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706.
15 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
16 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
17 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
18 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
19 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
20 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
21 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
22 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
23 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
24 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
25 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
26 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
27 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
28 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
29 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
30 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
31 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
32 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
33 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
34 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
35 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
36 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
37 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
38 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
39 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
40 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
41 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
42 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
43 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
44 Drug Interactions Flockhart Table
45 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
46 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
47 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
48 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
49 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
50 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
51 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
52 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
53 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
54 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
55 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
56 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
57 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
58 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
59 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
60 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
61 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
62 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
63 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
64 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
65 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
66 Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
67 Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
68 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
69 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
70 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1797).
71 Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
72 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
73 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
74 Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
75 Blakely KM, Drucker AM, Rosen CF "Drug-induced photosensitivity-an update: Culprit drugs, prevention and management." Drug Saf 42 (2019): 827-47. [PMID: 30888626]
76 Li J, Zhao M, He P, Hidalgo M, Baker SD "Differential metabolism of gefitinib and erlotinib by human cytochrome p450 enzymes." Clin Cancer Res 13 (2007): 3731-7. [PMID: 17575239]
77 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
78 Cerner Multum, Inc. "Australian Product Information.".
79 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
80 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
81 Product Information. Tarceva (erlotinib). Genentech, South San Francisco, CA.
82 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
83 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
84 Product Information. Tykerb (lapatinib). Novartis Pharmaceuticals, East Hanover, NJ.
85 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
86 Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ.
87 Product Information. Harvoni (ledipasvir-sofosbuvir). Gilead Sciences, Foster City, CA.
88 Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA.
89 Product Information. Prezista (darunavir). Ortho Biotech Inc, Bridgewater, NJ.
90 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
91 Canadian Pharmacists Association.
92 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
93 Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
94 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
95 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
96 Product Information. Clolar (clofarabine). sanofi-aventis, Bridgewater, NJ.
97 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
98 Product Information. Tasigna (nilotinib). Novartis Pharmaceuticals, East Hanover, NJ.
99 Product Information. Sprycel (dasatinib). Bristol-Myers Squibb, Princeton, NJ.
100 Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
101 Doherty MM, Charman WN "The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism?" Clin Pharmacokinet 41 (2002): 235-53. [PMID: 11978143]
102 Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
103 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
104 Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
105 Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
106 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.