Details of the Drug

General Information of Drug (ID: DM2TEOL)

Drug Name
Methotrexate
Synonyms
methotrexate; 1959/5/2; Rheumatrex; Amethopterin; Metatrexan; Hdmtx; Abitrexate; Mexate; Methylaminopterinum; Methotrexatum; Antifolan; Metotrexato; Methylaminopterin; MTX; (S)-2-(4-(((2,4-Diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)pentanedioic acid; Methotrexat; Amethopterine; Maxtrex; Rasuvo; L-Amethopterin; A-Methopterin; A-Methpterin; Amethopterin L-; Folex-Pfs; Methotrexat-Ebewe; N-Bismethylpteroylglutamic acid; Methotrexate, L-; Metotressato [DCIT]; Methotextrate; Mexate-Aq; [3H]methotrexate
Indication
Disease Entry ICD 11 Status REF
leukaemia 2A60-2B33 Approved [1]
Proliferative vitreoretinopathy 9B78.2 Phase 3 [2]
Solid tumour/cancer 2A00-2F9Z Phase 3 [1]
Rheumatoid arthritis FA20 Phase 1 [3]
Prostate cancer 2C82.0 Investigative [4]
Drug Type
Small molecular drug
Structure
3D MOL is unavailable 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 454.4
Topological Polar Surface Area (xlogp) -1.8
Rotatable Bond Count (rotbonds) 9
Hydrogen Bond Donor Count (hbonddonor) 5
Hydrogen Bond Acceptor Count (hbondacc) 12
Chemical Identifiers
Formula
C20H22N8O5
IUPAC Name
(2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid
Canonical SMILES
CN(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)N[C@@H](CCC(=O)O)C(=O)O
InChI
InChI=1S/C20H22N8O5/c1-28(9-11-8-23-17-15(24-11)16(21)26-20(22)27-17)12-4-2-10(3-5-12)18(31)25-13(19(32)33)6-7-14(29)30/h2-5,8,13H,6-7,9H2,1H3,(H,25,31)(H,29,30)(H,32,33)(H4,21,22,23,26,27)/t13-/m0/s1
InChIKey
FBOZXECLQNJBKD-ZDUSSCGKSA-N
Cross-matching ID
PubChem CID
126941
ChEBI ID
CHEBI:44185
CAS Number
59-05-2
DrugBank ID
DB00563
TTD ID
D0SV8E
VARIDT ID
DR00082
INTEDE ID
DR1045
ACDINA ID
D00412

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Proton-coupled folate transporter (SLC46A1) TTY8Z2E PCFT_HUMAN Modulator [5]
Solute carrier family 19 member 1 (SLC19A1) TT09I7D S19A1_HUMAN Modulator [6]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 8 (ABCC11) DTWN7FC ABCCB_HUMAN Substrate [7]
Folate transporter 1 (SLC19A1) DTOSN46 S19A1_HUMAN Substrate [8]
Proton-coupled folate transporter (SLC46A1) DTDJEMI PCFT_HUMAN Substrate [9]
Multidrug resistance-associated protein 5 (ABCC5) DTYVM24 MRP5_HUMAN Substrate [10]
Organic anion transporter 2 (SLC22A7) DT0OC1Q S22A7_HUMAN Substrate [11]
Multidrug resistance-associated protein 3 (ABCC3) DTQ3ZHF MRP3_HUMAN Substrate [12]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [13]
Organic anion transporter 4 (SLC22A11) DT06JWZ S22AB_HUMAN Substrate [14]
Multidrug resistance-associated protein 4 (ABCC4) DTCSGPB MRP4_HUMAN Substrate [15]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [16]
Multidrug resistance-associated protein 1 (ABCC1) DTSYQGK MRP1_HUMAN Substrate [17]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [18]
Organic anion transporter 1 (SLC22A6) DTQ23VB S22A6_HUMAN Substrate [19]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [20]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [21]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Substrate [22]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [23]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Thymidylate synthase (TYMS) DEASG0Q TYSY_HUMAN Substrate [24]
Dihydrofolate reductase (DHFR) DE4EGMZ DYR_HUMAN Substrate [24]
Methylenetetrahydrofolate reductase (MTHFR) DEOXTPZ MTHR_HUMAN Substrate [24]
Folylpolyglutamate synthase (FPGS) DECWT2V FOLC_HUMAN Substrate [24]
Gamma-Glu-X carboxypeptidase (GGH) DEU7MWJ GGH_HUMAN Substrate [24]
Thiopurine methyltransferase (TPMT) DEFQ8VO TPMT_HUMAN Substrate [25]
Glutamate carboxypeptidase II (FOLH1) DEN8V7Z FOLH1_HUMAN Substrate [26]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Methotrexate (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [160]
Sodium bicarbonate DMMU6BJ Minor as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Methotrexate caused by Sodium bicarbonate mediated altered urine pH. Acidosis [5C73] [161]
Tromethamine DMOBLGK Minor as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Methotrexate caused by Tromethamine mediated altered urine pH. Acidosis [5C73] [161]
Tretinoin DM49DUI Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Tretinoin. Acne vulgaris [ED80] [162]
Isotretinoin DM4QTBN Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Isotretinoin. Acne vulgaris [ED80] [162]
Nicotinamide DMUPE07 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Nicotinamide. Acquired cutaneous blood vessel malformation [EF20] [162]
Pioglitazone DMKJ485 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Pioglitazone. Acute diabete complication [5A2Y] [162]
Midostaurin DMI6E0R Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Midostaurin. Acute myeloid leukaemia [2A60] [162]
Arn-509 DMT81LZ Moderate Accelerated clearance of Methotrexate due to the transporter induction by Arn-509. Acute myeloid leukaemia [2A60] [162]
Gilteritinib DMWQ4MZ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Gilteritinib. Acute myeloid leukaemia [2A60] [162]
Framycetin DMF8DNE Moderate Altered absorption of Methotrexate caused by Framycetin. Alcoholic liver disease [DB94] [163]
Oxandrolone DMU9MYJ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Oxandrolone. Alcoholic liver disease [DB94] [162]
Paromomycin DM1AGXN Moderate Altered absorption of Methotrexate caused by Paromomycin. Amoebiasis [1A36] [163]
Inotersen DMJ93CT Major Increased risk of nephrotoxicity by the combination of Methotrexate and Inotersen. Amyloidosis [5D00] [162]
Dronedarone DMA8FS5 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Dronedarone. Angina pectoris [BA40] [162]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [164]
Oxymetholone DMFXUT8 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Oxymetholone. Aplastic anaemia [3A70] [162]
Voriconazole DMAOL2S Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Voriconazole. Aspergillosis [1F20] [162]
Posaconazole DMUL5EW Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Posaconazole. Aspergillosis [1F20] [162]
Budesonide DMJIBAW Moderate Additive immunosuppressive effects by the combination of Methotrexate and Budesonide. Asthma [CA23] [165]
Roflumilast DMPGHY8 Moderate Additive immunosuppressive effects by the combination of Methotrexate and Roflumilast. Asthma [CA23] [162]
Zileuton DMVRIC2 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Zileuton. Asthma [CA23] [162]
Kanamycin DM2DMPO Moderate Altered absorption of Methotrexate caused by Kanamycin. Bacterial infection [1A00-1C4Z] [163]
Clavulanate DM2FGRT Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Clavulanate. Bacterial infection [1A00-1C4Z] [162]
Clarithromycin DM4M1SG Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Clarithromycin. Bacterial infection [1A00-1C4Z] [162]
Ticarcillin DM4ME02 Major Decreased elimination of Methotrexate caused by Ticarcillin mediated competitive inhibition of renal tubular secretion. Bacterial infection [1A00-1C4Z] [166]
Sulfamethoxazole DMB08GE Moderate Increased plasma concentration of Methotrexate and Sulfamethoxazole due to competitive binding of plasma proteins. Bacterial infection [1A00-1C4Z] [167]
Meticillin DMIKHN0 Major Decreased elimination of Methotrexate caused by Meticillin mediated competitive inhibition of renal tubular secretion. Bacterial infection [1A00-1C4Z] [168]
Oxytetracycline DMOVH1M Moderate Increased plasma concentration of Methotrexate and Oxytetracycline due to competitive binding of plasma proteins. Bacterial infection [1A00-1C4Z] [169]
Bacampicillin DMP54C7 Major Decreased elimination of Methotrexate caused by Bacampicillin mediated competitive inhibition of renal tubular secretion. Bacterial infection [1A00-1C4Z] [166]
Oxacillin DMTAFY4 Major Decreased elimination of Methotrexate caused by Oxacillin mediated competitive inhibition of renal tubular secretion. Bacterial infection [1A00-1C4Z] [166]
Cloxacillin DMUTL7O Major Decreased elimination of Methotrexate caused by Cloxacillin mediated competitive inhibition of renal tubular secretion. Bacterial infection [1A00-1C4Z] [166]
Amoxicillin DMUYNEI Major Decreased elimination of Methotrexate caused by Amoxicillin mediated competitive inhibition of renal tubular secretion. Bacterial infection [1A00-1C4Z] [166]
Minocycline DMVN5OH Moderate Increased plasma concentration of Methotrexate and Minocycline due to competitive binding of plasma proteins. Bacterial infection [1A00-1C4Z] [169]
Telithromycin DMZ4P3A Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Telithromycin. Bacterial infection [1A00-1C4Z] [162]
Tetracycline DMZA017 Moderate Increased plasma concentration of Methotrexate and Tetracycline due to competitive binding of plasma proteins. Bacterial infection [1A00-1C4Z] [169]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Methotrexate and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [170]
Lomustine DMMWSUL Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Lomustine. Brain cancer [2A00] [162]
Lapatinib DM3BH1Y Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Lapatinib. Breast cancer [2C60-2C6Y] [162]
LY2835219 DM93VBZ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and LY2835219. Breast cancer [2C60-2C6Y] [162]
Pralatrexate DMAO80I Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Pralatrexate. Breast cancer [2C60-2C6Y] [162]
Tucatinib DMBESUA Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Tucatinib. Breast cancer [2C60-2C6Y] [162]
Tamoxifen DMLB0EZ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Tamoxifen. Breast cancer [2C60-2C6Y] [162]
Bosutinib DMTI8YE Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Bosutinib. Breast cancer [2C60-2C6Y] [162]
Trastuzumab Emtansine DMU1LXS Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Trastuzumab Emtansine. Breast cancer [2C60-2C6Y] [162]
Fluoxymesterone DMUHCF1 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Fluoxymesterone. Breast cancer [2C60-2C6Y] [162]
Demeclocycline DMZEPFJ Moderate Increased plasma concentration of Methotrexate and Demeclocycline due to competitive binding of plasma proteins. Bronchitis [CA20] [169]
Atorvastatin DMF28YC Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Atorvastatin. Cardiovascular disease [BA00-BE2Z] [162]
Fenofibric acid DMGO2MC Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Fenofibric acid. Cardiovascular disease [BA00-BE2Z] [162]
Macitentan DMP79A1 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Macitentan. Cardiovascular disease [BA00-BE2Z] [162]
Chenodiol DMQ8JIK Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Chenodiol. Cholelithiasis [DC11] [162]
Iodipamide DMXIQYS Major Increased risk of nephrotoxicity by the combination of Methotrexate and Iodipamide. Cholelithiasis [DC11] [171]
Corticotropin DMP9TWZ Moderate Additive immunosuppressive effects by the combination of Methotrexate and Corticotropin. Chronic kidney disease [GB61] [165]
Phenylbutazone DMAYL0T Major Increased risk of nephrotoxicity by the combination of Methotrexate and Phenylbutazone. Chronic pain [MG30] [172]
Ketoprofen DMRKXPT Major Increased risk of nephrotoxicity by the combination of Methotrexate and Ketoprofen. Chronic pain [MG30] [172]
Regorafenib DMHSY1I Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Regorafenib. Colorectal cancer [2B91] [160]
Intedanib DMSTA36 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Intedanib. Colorectal cancer [2B91] [162]
Methoxyflurane DML0RAE Moderate Increased risk of nephrotoxicity by the combination of Methotrexate and Methoxyflurane. Corneal disease [9A76-9A78] [162]
Pasireotide DMHM7JS Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Pasireotide. Cushing syndrome [5A70] [162]
Ivacaftor DMZC1HS Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Ivacaftor. Cystic fibrosis [CA25] [162]
Ethanol DMDRQZU Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Ethanol. Cystitis [GC00] [162]
Nefazodone DM4ZS8M Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Nefazodone. Depression [6A70-6A7Z] [162]
Milnacipran DMBFE74 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Milnacipran. Depression [6A70-6A7Z] [162]
Polatuzumab vedotin DMF6Y0L Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Polatuzumab vedotin. Diffuse large B-cell lymphoma [2A81] [162]
PMID28454500-Compound-96 DM2A75P Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and PMID28454500-Compound-96. Discovery agent [N.A.] [162]
SODIUM CITRATE DMHPD2Y Minor as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Methotrexate caused by SODIUM CITRATE mediated altered urine pH. Discovery agent [N.A.] [161]
Benzylpenicillin DMS9503 Major Decreased elimination of Methotrexate caused by Benzylpenicillin mediated competitive inhibition of renal tubular secretion. Discovery agent [N.A.] [168]
Felbamate DM1V5ZS Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Felbamate. Epilepsy/seizure [8A61-8A6Z] [162]
Fosphenytoin DMOX3LB Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Fosphenytoin. Epilepsy/seizure [8A61-8A6Z] [162]
Ethotoin DMXWOCP Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Ethotoin. Epilepsy/seizure [8A61-8A6Z] [162]
Carbamazepine DMZOLBI Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Carbamazepine. Epilepsy/seizure [8A61-8A6Z] [162]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Cannabidiol. Epileptic encephalopathy [8A62] [162]
Mefenamic acid DMK7HFI Major Increased risk of nephrotoxicity by the combination of Methotrexate and Mefenamic acid. Female pelvic pain [GA34] [172]
Dantrolene DM1D8XY Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Dantrolene. Fever [MG26] [162]
Itraconazole DMCR1MV Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Itraconazole. Fungal infection [1F29-1F2F] [162]
Terbinafine DMI6HUW Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Terbinafine. Fungal infection [1F29-1F2F] [162]
Ketoconazole DMPZI3Q Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Ketoconazole. Fungal infection [1F29-1F2F] [162]
Amphotericin B DMTAJQE Moderate Increased risk of nephrotoxicity by the combination of Methotrexate and Amphotericin B. Fungal infection [1F29-1F2F] [160]
Atovaquone DMY4UMW Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Atovaquone. Fungal infection [1F29-1F2F] [162]
Sunitinib DMCBJSR Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Sunitinib. Gastrointestinal stromal tumour [2B5B] [162]
Lamivudine DMI347A Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Lamivudine. Hepatitis virus infection [1E50-1E51] [162]
177Lu-DOTATATE DMT8GVU Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and 177Lu-DOTATATE. Hepatitis virus infection [1E50-1E51] [162]
Rifampin DMA8J1G Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Rifampin. HIV-infected patients with tuberculosis [1B10-1B14] [162]
Fostemsavir DM50ILT Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [173]
Stavudine DM6DEK9 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Stavudine. Human immunodeficiency virus disease [1C60-1C62] [162]
Tipranavir DM8HJX6 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Tipranavir. Human immunodeficiency virus disease [1C60-1C62] [162]
Emtricitabine DMBMUWZ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Emtricitabine. Human immunodeficiency virus disease [1C60-1C62] [162]
Efavirenz DMC0GSJ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Efavirenz. Human immunodeficiency virus disease [1C60-1C62] [162]
Zalcitabine DMH7MUV Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Zalcitabine. Human immunodeficiency virus disease [1C60-1C62] [162]
Rilpivirine DMJ0QOW Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [162]
Abacavir DMMN36E Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Abacavir. Human immunodeficiency virus disease [1C60-1C62] [162]
Darunavir DMN3GCH Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Darunavir. Human immunodeficiency virus disease [1C60-1C62] [162]
Maraviroc DMTL94F Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Maraviroc. Human immunodeficiency virus disease [1C60-1C62] [162]
Bempedoic acid DM1CI9R Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Bempedoic acid. Hyper-lipoproteinaemia [5C80] [174]
Simvastatin DM30SGU Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Simvastatin. Hyper-lipoproteinaemia [5C80] [162]
Fluvastatin DM4MDJY Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Fluvastatin. Hyper-lipoproteinaemia [5C80] [162]
Fenofibrate DMFKXDY Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Fenofibrate. Hyper-lipoproteinaemia [5C80] [162]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Methotrexate and Mipomersen. Hyper-lipoproteinaemia [5C80] [175]
Rosuvastatin DMMIQ7G Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Rosuvastatin. Hyper-lipoproteinaemia [5C80] [162]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Methotrexate and Teriflunomide. Hyper-lipoproteinaemia [5C80] [176]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Methotrexate and BMS-201038. Hyper-lipoproteinaemia [5C80] [177]
Moexipril DM26E4B Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Moexipril. Hypertension [BA00-BA04] [162]
Captopril DM458UM Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Captopril. Hypertension [BA00-BA04] [162]
Methyldopa DM5I621 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Methyldopa. Hypertension [BA00-BA04] [162]
Labetalol DMK8U72 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Labetalol. Hypertension [BA00-BA04] [162]
Enalapril DMNFUZR Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Enalapril. Hypertension [BA00-BA04] [162]
Perindopril DMOPZDT Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Perindopril. Hypertension [BA00-BA04] [162]
Quinapril DMR8H31 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Quinapril. Hypertension [BA00-BA04] [162]
Sodium acetate anhydrous DMH21E0 Minor as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Methotrexate caused by Sodium acetate anhydrous mediated altered urine pH. Hypo-osmolality/hyponatraemia [5C72] [161]
Tolvaptan DMIWFRL Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [162]
Fludrocortisone DMUDIR8 Moderate Additive immunosuppressive effects by the combination of Methotrexate and Fludrocortisone. Hypo-osmolality/hyponatraemia [5C72] [165]
Pirfenidone DM6VZFQ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Pirfenidone. Idiopathic interstitial pneumonitis [CB03] [162]
Vitamin B3 DMQVRZH Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Vitamin B3. Inborn lipid metabolism error [5C52] [162]
Givosiran DM5PFIJ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Givosiran. Inborn porphyrin/heme metabolism error [5C58] [162]
Febuxostat DMDEXQ0 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Febuxostat. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [162]
Balsalazide DMO091F Moderate Increased risk of nephrotoxicity by the combination of Methotrexate and Balsalazide. Indeterminate colitis [DD72] [178]
Meclofenamic acid DM05FXR Major Increased risk of nephrotoxicity by the combination of Methotrexate and Meclofenamic acid. Inflammatory spondyloarthritis [FA92] [179]
Testosterone DM7HUNW Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Testosterone. Low bone mass disorder [FB83] [162]
Denosumab DMNI0KO Moderate Additive immunosuppressive effects by the combination of Methotrexate and Denosumab. Low bone mass disorder [FB83] [180]
Porfimer Sodium DM7ZWNY Moderate Increased risk of photosensitivity reactions by the combination of Methotrexate and Porfimer Sodium. Lung cancer [2C25] [181]
Ceritinib DMB920Z Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Ceritinib. Lung cancer [2C25] [162]
Lurbinectedin DMEFRTZ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Lurbinectedin. Lung cancer [2C25] [162]
BIBW 2992 DMTKD7Q Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and BIBW 2992. Lung cancer [2C25] [162]
Pralsetinib DMWU0I2 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Pralsetinib. Lung cancer [2C25] [162]
Capmatinib DMYCXKL Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [182]
Selpercatinib DMZR15V Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Selpercatinib. Lung cancer [2C25] [162]
Sulphadoxine DMZI2UF Moderate Increased plasma concentration of Methotrexate and Sulphadoxine due to competitive binding of plasma proteins. Malaria [1F40-1F45] [167]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [162]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [183]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Idelalisib. Mature B-cell leukaemia [2A82] [184]
IPI-145 DMWA24P Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and IPI-145. Mature B-cell leukaemia [2A82] [162]
Clofarabine DMCVJ86 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Clofarabine. Mature B-cell lymphoma [2A85] [185]
Blinatumomab DMGECIJ Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Blinatumomab. Mature B-cell lymphoma [2A85] [162]
Mercaptopurine DMTM2IK Minor Decreased metabolism of Methotrexate caused by Mercaptopurine. Mature B-cell lymphoma [2A85] [186]
Ponatinib DMYGJQO Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Ponatinib. Mature B-cell lymphoma [2A85] [162]
Cytarabine DMZD5QR Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Cytarabine. Mature B-cell lymphoma [2A85] [160]
Arry-162 DM1P6FR Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Arry-162. Melanoma [2C30] [162]
Vemurafenib DM62UG5 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Vemurafenib. Melanoma [2C30] [162]
Ipilimumab DMJTIYK Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Ipilimumab. Melanoma [2C30] [162]
Dacarbazine DMNPZL4 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Dacarbazine. Melanoma [2C30] [162]
Danazol DML8KTN Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Danazol. Menstrual cycle bleeding disorder [GA20] [162]
Lasmiditan DMXLVDT Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Lasmiditan. Migraine [8A80] [187]
Exjade DMHPRWG Major Increased risk of nephrotoxicity by the combination of Methotrexate and Exjade. Mineral absorption/transport disorder [5C64] [188]
Riluzole DMECBWN Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Riluzole. Motor neuron disease [8B60] [162]
Carfilzomib DM48K0X Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Carfilzomib. Multiple myeloma [2A83] [162]
Panobinostat DM58WKG Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Panobinostat. Multiple myeloma [2A83] [162]
Thalidomide DM70BU5 Major Additive thrombogenic effects by the combination of Methotrexate and Thalidomide. Multiple myeloma [2A83] [189]
Tecfidera DM2OVDT Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Tecfidera. Multiple sclerosis [8A40] [162]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Methotrexate and Siponimod. Multiple sclerosis [8A40] [160]
Fingolimod DM5JVAN Major Additive immunosuppressive effects by the combination of Methotrexate and Fingolimod. Multiple sclerosis [8A40] [190]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Methotrexate and Ocrelizumab. Multiple sclerosis [8A40] [191]
Ozanimod DMT6AM2 Major Additive immunosuppressive effects by the combination of Methotrexate and Ozanimod. Multiple sclerosis [8A40] [162]
Nilotinib DM7HXWT Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Nilotinib. Myeloproliferative neoplasm [2A20] [162]
Imatinib DM7RJXL Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Imatinib. Myeloproliferative neoplasm [2A20] [162]
Rolapitant DM8XP26 Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Rolapitant. Nausea/vomiting [MD90] [192]
Bupropion DM5PCS7 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Bupropion. Nicotine use disorder [6C4A] [162]
Entrectinib DMMPTLH Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Entrectinib. Non-small cell lung cancer [2C25] [162]
Orlistat DMRJSP8 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Orlistat. Obesity [5B80-5B81] [162]
Valdecoxib DMAY7H4 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Valdecoxib. Osteoarthritis [FA00-FA05] [162]
Diclofenac DMPIHLS Major Increased risk of nephrotoxicity by the combination of Methotrexate and Diclofenac. Osteoarthritis [FA00-FA05] [172]
Naproxen DMZ5RGV Major Increased risk of nephrotoxicity by the combination of Methotrexate and Naproxen. Osteoarthritis [FA00-FA05] [172]
Rucaparib DM9PVX8 Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Rucaparib. Ovarian cancer [2C73] [193]
Etodolac DM6WJO9 Major Increased risk of nephrotoxicity by the combination of Methotrexate and Etodolac. Pain [MG30-MG3Z] [172]
Ibuprofen DM8VCBE Major Increased risk of nephrotoxicity by the combination of Methotrexate and Ibuprofen. Pain [MG30-MG3Z] [172]
Pemetrexed DMMX2E6 Moderate Decreased renal excretion of Methotrexate caused by Pemetrexed mediated nephrotoxicity. Pleural mesothelioma [2C26] [194]
Prednisone DM2HG4X Moderate Additive immunosuppressive effects by the combination of Methotrexate and Prednisone. Postoperative inflammation [1A00-CA43] [165]
Hydrocortisone DMGEMB7 Moderate Additive immunosuppressive effects by the combination of Methotrexate and Hydrocortisone. Postoperative inflammation [1A00-CA43] [165]
Bromfenac DMKB79O Major Increased risk of nephrotoxicity by the combination of Methotrexate and Bromfenac. Postoperative inflammation [1A00-CA43] [172]
ABIRATERONE DM8V75C Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and ABIRATERONE. Prostate cancer [2C82] [162]
Nilutamide DMFN07X Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Nilutamide. Prostate cancer [2C82] [162]
Darolutamide DMV7YFT Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [195]
Bicalutamide DMZMSPF Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Bicalutamide. Prostate cancer [2C82] [162]
Ambrisentan DMD1QXW Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Ambrisentan. Pulmonary hypertension [BB01] [162]
Axitinib DMGVH6N Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Axitinib. Renal cell carcinoma [2C90] [162]
Temsirolimus DMS104F Major Increased risk of nephrotoxicity by the combination of Methotrexate and Temsirolimus. Renal cell carcinoma [2C90] [196]
Meloxicam DM2AR7L Major Increased risk of nephrotoxicity by the combination of Methotrexate and Meloxicam. Rheumatoid arthritis [FA20] [172]
Sulindac DM2QHZU Major Increased risk of nephrotoxicity by the combination of Methotrexate and Sulindac. Rheumatoid arthritis [FA20] [172]
Tocilizumab DM7J6OR Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Tocilizumab. Rheumatoid arthritis [FA20] [162]
Canakinumab DM8HLO5 Moderate Additive immunosuppressive effects by the combination of Methotrexate and Canakinumab. Rheumatoid arthritis [FA20] [197]
Oxaprozin DM9UB0P Major Increased risk of nephrotoxicity by the combination of Methotrexate and Oxaprozin. Rheumatoid arthritis [FA20] [172]
Rilonacept DMGLUQS Moderate Additive immunosuppressive effects by the combination of Methotrexate and Rilonacept. Rheumatoid arthritis [FA20] [197]
Golimumab DMHZV7X Major Additive immunosuppressive effects by the combination of Methotrexate and Golimumab. Rheumatoid arthritis [FA20] [198]
Sulfasalazine DMICA9H Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Sulfasalazine. Rheumatoid arthritis [FA20] [162]
Fenoprofen DML5VQ0 Major Increased risk of nephrotoxicity by the combination of Methotrexate and Fenoprofen. Rheumatoid arthritis [FA20] [172]
Dexamethasone DMMWZET Moderate Additive immunosuppressive effects by the combination of Methotrexate and Dexamethasone. Rheumatoid arthritis [FA20] [165]
Sarilumab DMOGNXY Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Sarilumab. Rheumatoid arthritis [FA20] [162]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Methotrexate and Leflunomide. Rheumatoid arthritis [FA20] [176]
Anthrax vaccine DM9GSWY Moderate Antagonize the effect of Methotrexate when combined with Anthrax vaccine. Sepsis [1G40-1G41] [199]
Tedizolid DMG2SKR Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Tedizolid. Skin and skin-structure infection [1F28-1G0Z] [162]
Larotrectinib DM26CQR Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Larotrectinib. Solid tumour/cancer [2A00-2F9Z] [162]
Methylprednisolone DM4BDON Moderate Additive immunosuppressive effects by the combination of Methotrexate and Methylprednisolone. Solid tumour/cancer [2A00-2F9Z] [165]
PDX-101 DM6OC53 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and PDX-101. Solid tumour/cancer [2A00-2F9Z] [162]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [162]
Prednisolone DMQ8FR2 Moderate Additive immunosuppressive effects by the combination of Methotrexate and Prednisolone. Solid tumour/cancer [2A00-2F9Z] [165]
Methyltestosterone DMWLFGO Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Methyltestosterone. Solid tumour/cancer [2A00-2F9Z] [162]
Disulfiram DMCL2OK Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Disulfiram. Substance abuse [6C40] [162]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Naltrexone. Substance abuse [6C40] [162]
Fostamatinib DM6AUHV Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Fostamatinib. Thrombocytopenia [3B64] [162]
Eltrombopag DMOGFIX Moderate Decreased clearance of Methotrexate due to the transporter inhibition by Eltrombopag. Thrombocytopenia [3B64] [200]
Lenvatinib DMB1IU4 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Lenvatinib. Thyroid cancer [2D10] [162]
Methimazole DM25FL8 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Methimazole. Thyrotoxicosis [5A02] [162]
Tizanidine DMR2IQ4 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Tizanidine. Tonus and reflex abnormality [MB47] [162]
Trimetrexate DMDEA85 Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Trimetrexate. Toxoplasmosis [1F57] [162]
Sirolimus DMGW1ID Major Increased risk of nephrotoxicity by the combination of Methotrexate and Sirolimus. Transplant rejection [NE84] [196]
Azathioprine DMMZSXQ Minor Decreased metabolism of Methotrexate caused by Azathioprine. Transplant rejection [NE84] [186]
Tacrolimus DMZ7XNQ Major Increased risk of nephrotoxicity by the combination of Methotrexate and Tacrolimus. Transplant rejection [NE84] [196]
Olsalazine DMZW9HA Moderate Increased risk of nephrotoxicity by the combination of Methotrexate and Olsalazine. Ulcerative colitis [DD71] [178]
Nitrofurantoin DM7PQIK Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Nitrofurantoin. Urinary tract infection [GC08] [162]
Sulfamethizole DMGCHDS Moderate Increased plasma concentration of Methotrexate and Sulfamethizole due to competitive binding of plasma proteins. Urinary tract infection [GC08] [167]
Plazomicin DMKMBES Moderate Increased risk of nephrotoxicity by the combination of Methotrexate and Plazomicin. Urinary tract infection [GC08] [160]
Carbenicillin DMLEDNK Major Decreased elimination of Methotrexate caused by Carbenicillin mediated competitive inhibition of renal tubular secretion. Urinary tract infection [GC08] [166]
Mezlocillin DMY5JEP Major Decreased elimination of Methotrexate caused by Mezlocillin mediated competitive inhibition of renal tubular secretion. Urinary tract infection [GC08] [166]
Elagolix DMB2C0E Moderate Increased risk of hepatotoxicity by the combination of Methotrexate and Elagolix. Uterine fibroid [2E86] [162]
Triamcinolone DM98IXF Moderate Additive immunosuppressive effects by the combination of Methotrexate and Triamcinolone. Vasomotor/allergic rhinitis [CA08] [165]
Ganciclovir DM1MBYQ Moderate Additive myelosuppressive effects by the combination of Methotrexate and Ganciclovir. Virus infection [1A24-1D9Z] [160]
Valaciclovir DMHKS94 Moderate Increased risk of nephrotoxicity by the combination of Methotrexate and Valaciclovir. Virus infection [1A24-1D9Z] [162]
Valganciclovir DMS2IUH Moderate Additive myelosuppressive effects by the combination of Methotrexate and Valganciclovir. Virus infection [1A24-1D9Z] [160]
⏷ Show the Full List of 217 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
Allura red AC dye E00338 33258 Colorant
FD&C blue no. 1 E00263 19700 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Quinoline yellow WS E00309 24671 Colorant
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 400 E00653 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium carbonate monohydrate E00454 2735133 Alkalizing agent; Buffering agent; Diluent; Dispersing agent
Sodium hydroxide E00234 14798 Alkalizing agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
⏷ Show the Full List of 18 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Methotrexate 15 mg tablet 15 mg Oral Tablet Oral
Methotrexate 5 mg tablet 5 mg Oral Tablet Oral
Methotrexate 10 mg tablet 10 mg Oral Tablet Oral
Methotrexate 7.5 mg tablet 7.5 mg Oral Tablet Oral
Methotrexate 2.5 mg tablet 2.5 mg Oral Tablet Oral
Methotrexate Sodium 2.5mg tablet 2.5mg Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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86 A species difference in the transport activities of H2 receptor antagonists by rat and human renal organic anion and cation transporters. J Pharmacol Exp Ther. 2005 Oct;315(1):337-45.
87 Human organic anion transporter 2 is an entecavir, but not tenofovir, transporter. Drug Metab Pharmacokinet. 2017 Feb;32(1):116-119.
88 Human organic anion transporters mediate the transport of tetracycline. Jpn J Pharmacol. 2002 Jan;88(1):69-76.
89 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
90 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
91 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
92 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
93 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
94 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
95 FDA Drug Development and Drug Interactions
96 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
97 ATP-binding cassette C transporters in human pancreatic carcinoma cell lines. Upregulation in 5-fluorouracil-resistant cells. Pancreatology. 2009;9(1-2):136-44.
98 Functional reconstitution of human ABCC3 into proteoliposomes reveals a transport mechanism with positive cooperativity. Biochemistry. 2009 May 26;48(20):4423-30.
99 Complex pharmacokinetic behavior of ezetimibe depends on abcc2, abcc3, and abcg2. Drug Metab Dispos. 2009 Aug;37(8):1698-702.
100 Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. Placenta. 2006 Nov-Dec;27(11-12):1096-102.
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102 Oral availability of cefadroxil depends on ABCC3 and ABCC4. Drug Metab Dispos. 2012 Mar;40(3):515-21.
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104 Involvement of multiple efflux transporters in hepatic disposition of fexofenadine. Mol Pharmacol. 2008 May;73(5):1474-83.
105 Induction of multiple drug transporters by efavirenz. J Pharmacol Sci. 2009 Feb;109(2):242-50.
106 Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system. Cancer Res. 2002 Jun 1;62(11):3144-50.
107 The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9.
108 Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4). Biochem J. 2003 Apr 15;371(Pt 2):361-7.
109 P-glycoprotein, but not multidrug resistance protein 4, plays a role in the systemic clearance of irinotecan and SN-38 in mice. Drug Metab Lett. 2010 Dec;4(4):195-201.
110 Polymorphisms in multidrug resistance-associated protein gene 4 is associated with outcome in childhood acute lymphoblastic leukemia. Blood. 2009 Aug 13;114(7):1383-6.
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112 Celecoxib upregulates multidrug resistance proteins in colon cancer: lack of synergy with standard chemotherapy. Curr Cancer Drug Targets. 2008 Aug;8(5):414-20.
113 Overexpression of MRP4 (ABCC4) and MRP5 (ABCC5) confer resistance to the nucleoside analogs cytarabine and troxacitabine, but not gemcitabine. Springerplus. 2014 Dec 13;3:732.
114 Cellular export of drugs and signaling molecules by the ATP-binding cassette transporters MRP4 (ABCC4) and MRP5 (ABCC5). Drug Metab Rev. 2005;37(1):253-78.
115 Interdependence of gemcitabine treatment, transporter expression, and resistance in human pancreatic carcinoma cells. Neoplasia. 2010 Sep;12(9):740-7.
116 Hyaluronan export by the ABC transporter MRP5 and its modulation by intracellular cGMP. J Biol Chem. 2007 Jul 20;282(29):20999-1004.
117 Kinetic validation of the use of carboxydichlorofluorescein as a drug surrogate for MRP5-mediated transport. Eur J Pharm Sci. 2006 Apr;27(5):524-32.
118 Role of MRP4 and MRP5 in biology and chemotherapy. AAPS PharmSci. 2002;4(3):E14.
119 The multidrug resistance protein 5 functions as an ATP-dependent export pump for cyclic nucleotides. J Biol Chem. 2000 Sep 29;275(39):30069-74.
120 The anti-influenza drug oseltamivir exhibits low potential to induce pharmacokinetic drug interactions via renal secretion-correlation of in vivo and in vitro studies. Drug Metab Dispos. 2002 Jan;30(1):13-9.
121 Expression levels of renal organic anion transporters (OATs) and their correlation with anionic drug excretion in patients with renal diseases. Pharm Res. 2004 Jan;21(1):61-7.
122 Multiple human isoforms of drug transporters contribute to the hepatic and renal transport of olmesartan, a selective antagonist of the angiotensin II AT1-receptor. Drug Metab Dispos. 2007 Dec;35(12):2166-76.
123 Interaction of zalcitabine with human organic anion transporter 1. Pharmazie. 2006 May;61(5):491-2.
124 Apical expression or expression in a non polarized cell of hOAT1 inverses regulation by epidermal growth factor (EGF) as compared to basolateral hOAT1. Cell Physiol Biochem. 2004;14(3):177-86.
125 Human renal organic anion transporter 1 (hOAT1) and its role in the nephrotoxicity of antiviral nucleotide analogs. Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):641-8.
126 Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86.
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128 Murine renal organic anion transporters mOAT1 and mOAT3 facilitate the transport of neuroactive tryptophan metabolites. Am J Physiol Cell Physiol. 2005 Nov;289(5):C1075-84.
129 Organic anion transporter 3 is involved in the brain-to-blood efflux transport of thiopurine nucleobase analogs. J Neurochem. 2004 Aug;90(4):931-41.
130 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
131 The contribution of organic anion transporters OAT1 and OAT3 to the renal uptake of rosuvastatin. J Pharmacol Exp Ther. 2007 Sep;322(3):1221-7.
132 Aspirin and probenecid inhibit organic anion transporter 3-mediated renal uptake of cilostazol and probenecid induces metabolism of cilostazol in the rat. Drug Metab Dispos. 2014 Jun;42(6):996-1007.
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134 The role of the intracellular glutamate gradient in driving organic anion transporter function.
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136 Interactions of human organic anion transporters with diuretics. J Pharmacol Exp Ther. 2004 Mar;308(3):1021-9.
137 Inhibitory effects of angiotensin II receptor antagonists and leukotriene receptor antagonists on the transport of human organic anion transporter 4. J Pharm Pharmacol. 2006 Nov;58(11):1499-505.
138 Cellular Uptake of Levocetirizine by Organic Anion Transporter 4. J Pharm Sci. 2017 Sep;106(9):2895-2898.
139 Involvement of uric acid transporters in alteration of serum uric acid level by angiotensin II receptor blockers. Pharm Res. 2008 Mar;25(3):639-46.
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147 Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology. 2001 May;142(5):2005-12.
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149 Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.
150 Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos. 2011 Jun;39(6):1047-53.
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152 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
153 Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46.
154 Human multidrug resistance protein 8 (MRP8/ABCC11), an apical efflux pump for steroid sulfates, is an axonal protein of the CNS and peripheral nervous system. Neuroscience. 2006;137(4):1247-57.
155 MRP8, ATP-binding cassette C11 (ABCC11), is a cyclic nucleotide efflux pump and a resistance factor for fluoropyrimidines 2',3'-dideoxycytidine and 9'-(2'-phosphonylmethoxyethyl)adenine. J Biol Chem. 2003 Aug 8;278(32):29509-14.
156 Tenofovir Disoproxil Fumarate Is a New Substrate of ATP-Binding Cassette Subfamily C Member 11. Antimicrob Agents Chemother. 2017 Mar 24;61(4). pii: e01725-16.
157 Antifolates in cancer therapy: structure, activity and mechanisms of drug resistance. Drug Resist Updat. 2012 Aug;15(4):183-210.
158 Characterization of uptake of folates by rat and human blood-brain barrier endothelial cells. Biofactors. 2010 May-Jun;36(3):201-9.
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