Details of the Drug

General Information of Drug (ID: DM30SGU)

Drug Name
Simvastatin
Synonyms
Cholestat; Coledis; Colemin; Corolin; Denan; Labistatin; Lipex; Lipovas; Lodales; Medipo; Nivelipol; Pantok; Rendapid; Simovil; Simvastatina; Simvastatine; Simvastatinum; Sinvacor; Sivastin; Synvinolin; Vasotenal; Zocor; Zocord; Simvast CR; Simvastatina [Spanish]; Simvastatine [French]; Simvastatinum [Latin]; MK 0733; MK 733; MK733; TNP00259; DRG-0320; KS-1113; L 644128-000U; MK-0733; MK-733; Simcard (TN); Simlup (TN); Simvacor (TN); Simvastatin & Primycin; Simvastatin, Compactin; Zocor (TN); Simvastatin [USAN:INN:BAN]; Simvastatin (JAN/USP/INN); Zocor, Simlup, Simcard, Simvacor, Simvoget, Zorced, Simvastatin; [(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] 2,2-dimethylbutanoate; Butanoic acid, 2,2-dimethyl-, (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl ester; Butanoic acid, 2,2-dimethyl-, (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-(2-((2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl)-1-naphthalenyl ester; Butanoic acid, 2,2-dimethyl-, (1S,3R,7S,8S,*aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-(2-((2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl)-1-naphthalenyl ester; (1S,3R,7S,8S,8aR)-8-{2-[(2R,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl]ethyl}-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl 2,2-dimethylbutanoate; Butanoic acid, 2,2-dimethyl-,1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)-ethyl]-1-naphthalenyl ester, [1S-[1 alpha,3 alpha,7 beta,8 beta(2S*,4S*),-8a beta; 2,2-Dimethylbutanoic acid (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl ester; 2,2-Dimethylbutyric acid, 8-ester with (4R,6R)-6-(2-((1S,2S,6R,8S,8aR)-1,2,6,7,8,8a-hexahydro-8-hydroxy-2,6-dimethyl-1-naphthyl)ethyl)tetrahydro-4-hydroxy-2H-pyran-2-one
Indication
Disease Entry ICD 11 Status REF
Hypercholesterolaemia 5C80.0 Approved [1], [2]
Therapeutic Class
Anticholesteremic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 418.6
Topological Polar Surface Area (xlogp) 4.7
Rotatable Bond Count (rotbonds) 7
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1.3-2.4 h [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Elimination
13% of the dose was excreted in urine and 60% in feces [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 4.85 hours [3]
Metabolism
The drug is metabolized via a combination of spontaneous chemical conversion and enzyme-mediated hydrolysis by nonspecific carboxyesterases in the intestinal wall, liver, and plasma [6]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.3652 micromolar/kg/day [7]
Water Solubility
The ability of drug to dissolve in water is measured as 0.03 mg/mL [4]
Chemical Identifiers
Formula
C25H38O5
IUPAC Name
[(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] 2,2-dimethylbutanoate
Canonical SMILES
CCC(C)(C)C(=O)O[C@H]1C[C@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@@H]3C[C@H](CC(=O)O3)O)C
InChI
InChI=1S/C25H38O5/c1-6-25(4,5)24(28)30-21-12-15(2)11-17-8-7-16(3)20(23(17)21)10-9-19-13-18(26)14-22(27)29-19/h7-8,11,15-16,18-21,23,26H,6,9-10,12-14H2,1-5H3/t15-,16-,18+,19+,20-,21-,23-/m0/s1
InChIKey
RYMZZMVNJRMUDD-HGQWONQESA-N
Cross-matching ID
PubChem CID
54454
ChEBI ID
CHEBI:9150
CAS Number
79902-63-9
DrugBank ID
DB00641
TTD ID
D0H0ND
VARIDT ID
DR00435
INTEDE ID
DR1485
ACDINA ID
D00625

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
HMG-CoA reductase (HMGCR) TTPADOQ HMDH_HUMAN Inhibitor [8]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [9]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [10]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [11]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [12]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [13]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [14]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Substrate [14]
Cytochrome P450 3A5 (CYP3A5)
Main DME 		DEIBDNY CP3A5_HUMAN Substrate [15]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [16]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Substrate [14]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_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 Hypercholesterolaemia
ICD Disease Classification 5C80.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
HMG-CoA reductase (HMGCR) DTT HMGCR 1.01E-05 0.65 1.53
P-glycoprotein 1 (ABCB1) DTP P-GP 3.29E-14 -7.08E-01 -1.99E+00
Breast cancer resistance protein (ABCG2) DTP BCRP 2.28E-08 -3.66E-01 -8.07E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 3.27E-01 -5.78E-02 -3.84E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 2.00E-01 5.79E-02 3.00E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 1.47E-02 -1.13E-01 -1.13E+00
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 3.65E-02 -8.90E-02 -5.58E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 4.03E-02 -1.19E-01 -5.11E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 5.05E-04 -1.51E-01 -8.87E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 3.24E-05 -3.48E-01 -1.34E+00
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 Simvastatin
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Simvastatin and Mipomersen. Hyper-lipoproteinaemia [5C80] [108]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Simvastatin and Teriflunomide. Hyper-lipoproteinaemia [5C80] [109]
BMS-201038 DMQTAGO Major Decreased metabolism of Simvastatin caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [110]
Coadministration of a Drug Treating the Disease Different from Simvastatin (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [111]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Simvastatin caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [112]
Midostaurin DMI6E0R Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Midostaurin. Acute myeloid leukaemia [2A60] [113]
Arn-509 DMT81LZ Moderate Increased metabolism of Simvastatin caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [113]
Emapalumab DMZG5WL Moderate Altered metabolism of Simvastatin due to Emapalumab alters the formation of CYP450 enzymes. Adaptive immunity immunodeficiency [4A01] [113]
Siltuximab DMGEATB Moderate Altered metabolism of Simvastatin due to Siltuximab alters the formation of CYP450 enzymes. Anemia [3A00-3A9Z] [113]
Dronedarone DMA8FS5 Major Decreased clearance of Simvastatin due to the transporter inhibition by Dronedarone. Angina pectoris [BA40] [114]
Nifedipine DMSVOZT Moderate Decreased metabolism of Simvastatin caused by Nifedipine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [115]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [116]
Posaconazole DMUL5EW Major Decreased metabolism of Simvastatin caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [111]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Simvastatin caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [117]
Clarithromycin DM4M1SG Major Decreased metabolism of Simvastatin caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [118]
Troleandomycin DMUZNIG Major Decreased metabolism of Simvastatin caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [118]
Telithromycin DMZ4P3A Major Decreased metabolism of Simvastatin caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [119]
Ag-221 DMS0ZBI Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Ag-221. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [111]
Erdafitinib DMI782S Moderate Increased metabolism of Simvastatin caused by Erdafitinib mediated induction of CYP450 enzyme. Bladder cancer [2C94] [120]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Simvastatin and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [121]
Talazoparib DM1KS78 Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [122]
Lapatinib DM3BH1Y Moderate Decreased metabolism of Simvastatin caused by Lapatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [115]
Tucatinib DMBESUA Major Decreased metabolism of Simvastatin caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [123]
Palbociclib DMD7L94 Moderate Decreased metabolism of Simvastatin caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [115]
Anisindione DM2C48U Minor Increased plasma concentration of Simvastatin and Anisindione due to competitive binding of plasma proteins. Coagulation defect [3B10] [124]
Mifepristone DMGZQEF Major Decreased metabolism of Simvastatin caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [125]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Simvastatin caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [115]
Lumacaftor DMCLWDJ Major Increased metabolism of Simvastatin caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [111]
Ivacaftor DMZC1HS Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Ivacaftor. Cystic fibrosis [CA25] [126]
MK-8228 DMOB58Q Major Decreased clearance of Simvastatin due to the transporter inhibition by MK-8228. Cytomegaloviral disease [1D82] [127]
Aprepitant DM053KT Moderate Decreased metabolism of Simvastatin caused by Aprepitant mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [115]
Nefazodone DM4ZS8M Major Decreased metabolism of Simvastatin caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [123]
Oxcarbazepine DM5PU6O Moderate Increased metabolism of Simvastatin caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [128]
Stiripentol DMMSDOY Moderate Decreased metabolism of Simvastatin caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [129]
Rufinamide DMWE60C Moderate Increased metabolism of Simvastatin caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [113]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Simvastatin caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [113]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Cannabidiol. Epileptic encephalopathy [8A62] [113]
Itraconazole DMCR1MV Major Decreased metabolism of Simvastatin caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [109]
Miconazole DMPMYE8 Moderate Decreased metabolism of Simvastatin caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [113]
Ketoconazole DMPZI3Q Major Decreased metabolism of Simvastatin caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [130]
Boceprevir DMBSHMF Major Decreased metabolism of Simvastatin caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [118]
Simeprevir DMLUA9D Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Simeprevir. Hepatitis virus infection [1E50-1E51] [131]
Telaprevir DMMRV29 Major Decreased metabolism of Simvastatin caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [118]
Rifampin DMA8J1G Major Increased metabolism of Simvastatin caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [132]
Rifapentine DMCHV4I Moderate Increased metabolism of Simvastatin caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [133]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Brentuximab vedotin. Hodgkin lymphoma [2B30] [134]
Delavirdine DM3NF5G Major Decreased metabolism of Simvastatin caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [135]
Fosamprenavir DM4W9B3 Major Decreased metabolism of Simvastatin caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [136]
Fostemsavir DM50ILT Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [137]
Cobicistat DM6L4H2 Major Decreased metabolism of Simvastatin caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [123]
Tipranavir DM8HJX6 Major Decreased metabolism of Simvastatin caused by Tipranavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [136]
Saquinavir DMG814N Major Decreased metabolism of Simvastatin caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [136]
Etravirine DMGV8QU Moderate Increased metabolism of Simvastatin caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [138]
Zalcitabine DMH7MUV Moderate Increased risk of peripheral neuropathy by the combination of Simvastatin and Zalcitabine. Human immunodeficiency virus disease [1C60-1C62] [139]
Amprenavir DMLMXE0 Major Decreased metabolism of Simvastatin caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [136]
Darunavir DMN3GCH Major Decreased metabolism of Simvastatin caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [136]
Atazanavir DMSYRBX Major Decreased metabolism of Simvastatin caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [136]
Levamlodipine DM92S6N Major Decreased metabolism of Simvastatin caused by Levamlodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [140]
Conivaptan DM1V329 Major Decreased metabolism of Simvastatin caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [118]
Lesinurad DMUR64T Moderate Increased metabolism of Simvastatin caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [141]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Simvastatin caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [115]
Suvorexant DM0E6S3 Moderate Decreased metabolism of Simvastatin caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [115]
Crizotinib DM4F29C Moderate Decreased metabolism of Simvastatin caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [115]
Brigatinib DM7W94S Moderate Increased metabolism of Simvastatin caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [142]
Porfimer Sodium DM7ZWNY Moderate Increased risk of photosensitivity reactions by the combination of Simvastatin and Porfimer Sodium. Lung cancer [2C25] [143]
Ceritinib DMB920Z Major Decreased metabolism of Simvastatin caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [123]
PF-06463922 DMKM7EW Moderate Increased metabolism of Simvastatin caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [144]
Osimertinib DMRJLAT Moderate Increased metabolism of Simvastatin caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [113]
Selpercatinib DMZR15V Moderate Decreased metabolism of Simvastatin caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [115]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [145]
Idelalisib DM602WT Major Decreased metabolism of Simvastatin caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [123]
IPI-145 DMWA24P Moderate Decreased metabolism of Simvastatin caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [115]
Arry-162 DM1P6FR Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Arry-162. Melanoma [2C30] [111]
LGX818 DMNQXV8 Moderate Increased metabolism of Simvastatin caused by LGX818 mediated induction of CYP450 enzyme. Melanoma [2C30] [146]
Dabrafenib DMX6OE3 Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Dabrafenib. Melanoma [2C30] [111]
Danazol DML8KTN Major Decreased metabolism of Simvastatin caused by Danazol mediated inhibition of CYP450 enzyme. Menstrual cycle bleeding disorder [GA20] [117]
Exjade DMHPRWG Moderate Decreased metabolism of Simvastatin caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [147]
Thalidomide DM70BU5 Moderate Increased risk of peripheral neuropathy by the combination of Simvastatin and Thalidomide. Multiple myeloma [2A83] [139]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Simvastatin caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [115]
Dasatinib DMJV2EK Moderate Decreased metabolism of Simvastatin caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [115]
Modafinil DMYILBE Moderate Increased metabolism of Simvastatin caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [111]
Netupitant DMEKAYI Moderate Decreased metabolism of Simvastatin caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [117]
Entrectinib DMMPTLH Moderate Decreased metabolism of Simvastatin caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [115]
Olaparib DM8QB1D Moderate Decreased metabolism of Simvastatin caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [111]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Simvastatin caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [115]
Abametapir DM2RX0I Moderate Decreased metabolism of Simvastatin caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [148]
Esomeprazole DM7BN0X Moderate Increased plasma concentrations of Simvastatin and Esomeprazole due to competitive inhibition of the same metabolic pathway. Peptic ulcer [DA61] [132]
Lefamulin DME6G97 Moderate Decreased metabolism of Simvastatin caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [149]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Simvastatin caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [150]
Enzalutamide DMGL19D Moderate Increased metabolism of Simvastatin caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [151]
Darolutamide DMV7YFT Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [113]
Bicalutamide DMZMSPF Moderate Decreased metabolism of Simvastatin caused by Bicalutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [115]
Ustekinumab DMHTYK3 Moderate Altered metabolism of Simvastatin due to Ustekinumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [113]
Ixekizumab DMXW92T Moderate Altered metabolism of Simvastatin due to Ixekizumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [113]
Tocilizumab DM7J6OR Moderate Altered metabolism of Simvastatin due to Tocilizumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [113]
Canakinumab DM8HLO5 Moderate Altered metabolism of Simvastatin due to Canakinumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [113]
Rilonacept DMGLUQS Moderate Altered metabolism of Simvastatin due to Rilonacept alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [113]
Sarilumab DMOGNXY Moderate Altered metabolism of Simvastatin due to Sarilumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [113]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Simvastatin and Leflunomide. Rheumatoid arthritis [FA20] [109]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Simvastatin caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [115]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Simvastatin caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [113]
Larotrectinib DM26CQR Moderate Decreased metabolism of Simvastatin caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [115]
Armodafinil DMGB035 Moderate Increased metabolism of Simvastatin caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [111]
LEE011 DMMX75K Moderate Decreased metabolism of Simvastatin caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [115]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Naltrexone. Substance abuse [6C40] [152]
Warfarin DMJYCVW Minor Increased plasma concentration of Simvastatin and Warfarin due to competitive binding of plasma proteins. Supraventricular tachyarrhythmia [BC81] [124]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Simvastatin caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [153]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [154]
Brilinta DMBR01X Moderate Decreased metabolism of Simvastatin caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [113]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Simvastatin and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [155]
Tacrolimus DMZ7XNQ Moderate Increased plasma concentrations of Simvastatin and Tacrolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [155]
Albiglutide DM1JEGF Minor Altered absorption of Simvastatin due to GI dynamics variation caused by Albiglutide. Type 2 diabetes mellitus [5A11] [129]
Dapagliflozin DM28UJG Minor Increased plasma concentrations of Simvastatin and Dapagliflozin due to competitive inhibition of the same metabolic pathway. Type 2 diabetes mellitus [5A11] [156]
Amiodarone DMUTEX3 Major Decreased metabolism of Simvastatin caused by Amiodarone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [157]
⏷ Show the Full List of 111 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
Calcium ascorbate anhydrous E00582 54740489 Antioxidant
Isopropyl alcohol E00070 3776 Antimicrobial preservative; Solvent
Kyselina citronova E00014 311 Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Ascorbic acid E00579 54670067 Acidulant; Antioxidant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Butylhydroxyanisole E00308 24667 Antimicrobial preservative; Antioxidant
Carmellose sodium E00625 Not Available Disintegrant
Citric acid monohydrate E00271 22230 Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 3350 E00652 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 4000 E00654 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
Triethyl citrate E00128 6506 Plasticizing agent; Solvent
⏷ Show the Full List of 23 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Simvastatin 80 mg tablet 80 mg Oral Tablet Oral
Simvastatin 10 mg tablet 10 mg Oral Tablet Oral
Simvastatin 40 mg tablet 40 mg Oral Tablet Oral
Simvastatin 20 mg tablet 20 mg Oral Tablet Oral
Simvastatin 5 mg tablet 5 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: 2955).
2 Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
3 Simvastatin pharmacokinetics in healthy Chinese subjects and its relations with CYP2C9, CYP3A5, ABCB1, ABCG2 and SLCO1B1 polymorphisms. Pharmazie. 2013 Feb;68(2):124-8.
4 BDDCS applied to over 900 drugs
5 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
6 Nakajima M, Nakamura S, Tokudome S, Shimada N, Yamazaki H, Yokoi T: Azelastine N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in human liver microsomes: evaluation of approach to predict the contribution of multiple CYPs. Drug Metab Dispos. 1999 Dec;27(12):1381-91.
7 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
8 Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64.
9 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
10 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
11 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.
12 A comparison of the effects of 3-hydroxy-3-methylglutaryl-coenzyme a (HMG-CoA) reductase inhibitors on the CYP3A4-dependent oxidation of mexazolam in vitro. Drug Metab Dispos. 2001 Mar;29(3):282-8.
13 Genetic polymorphisms in cytochrome P450 enzymes: effect on efficacy and tolerability of HMG-CoA reductase inhibitors. Am J Cardiovasc Drugs. 2004;4(4):247-55.
14 Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
15 In vitro metabolism of simvastatin in humans [SBT]identification of metabolizing enzymes and effect of the drug on hepatic P450s. Drug Metab Dispos. 1997 Oct;25(10):1191-9.
16 Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance. Clin Pharmacol Ther. 2006 Dec;80(6):565-81.
17 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.
18 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
19 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.
20 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
21 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.
22 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.
23 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
24 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.
25 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.
26 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
27 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
28 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
29 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics. Drug Metab Dispos. 2007 Mar;35(3):371-80.
30 Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
31 Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
32 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
33 Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
34 Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
35 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
36 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
37 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.
38 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
39 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.
40 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
41 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
42 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
43 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
44 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.
45 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.
46 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.
47 Drug Interactions Flockhart Table
48 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.
49 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
50 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
51 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
52 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
53 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.
54 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
55 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
56 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
57 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
58 Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
59 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
60 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
61 High-dose rabeprazole/amoxicillin therapy as the second-line regimen after failure to eradicate H. pylori by triple therapy with the usual doses of a proton pump inhibitor, clarithromycin and amoxicillin. Hepatogastroenterology. 2003 Nov-Dec;50(54):2274-8.
62 Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
63 Cytochrome P450 pharmacogenetics and cancer. Oncogene. 2006 Mar 13;25(11):1679-91.
64 CYP2C19*17 is associated with decreased breast cancer risk. Breast Cancer Res Treat. 2009 May;115(2):391-6.
65 Cytochromes of the P450 2C subfamily are the major enzymes involved in the O-demethylation of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):116-21.
66 Diclofenac and its derivatives as tools for studying human cytochromes P450 active sites: particular efficiency and regioselectivity of P450 2Cs. Biochemistry. 1999 Oct 26;38(43):14264-70.
67 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
68 Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33.
69 Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22.
70 Determination of UDP-glucuronosyltransferase UGT2B7 activity in human liver microsomes by ultra-performance liquid chromatography with MS detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jul 1;870(1):84-90.
71 Pharmacokinetic and pharmacodynamic interaction of lorazepam and valproic acid in relation to UGT2B7 genetic polymorphism in healthy subjects. Clin Pharmacol Ther. 2008 Apr;83(4):595-600.
72 Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168.
73 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
74 Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
75 Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
76 UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7.
77 Cerivastatin, genetic variants, and the risk of rhabdomyolysis. Pharmacogenet Genomics. 2011 May;21(5):280-8.
78 Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2011 Apr;89(4):524-8.
79 S-Naproxen and desmethylnaproxen glucuronidation by human liver microsomes and recombinant human UDP-glucuronosyltransferases (UGT): role of UGT2B7 in the elimination of naproxen. Br J Clin Pharmacol. 2005 Oct;60(4):423-33.
80 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
81 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
82 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
83 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
84 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.
85 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
86 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
87 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.
88 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
89 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
90 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
91 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.
92 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
93 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
94 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
95 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
96 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
97 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.
98 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.
99 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.
100 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
101 FDA Drug Development and Drug Interactions
102 A randomized, double-blind trial comparing the efficacy and safety of pitavastatin versus pravastatin in patients with primary hypercholesterolemia. Atherosclerosis. 2002 Jun;162(2):373-9.
103 Cholesterol-lowering effect of NK-104, a 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor, in guinea pig model of hyperlipidemia. Arzneimittelforschung. 2001;51(3):197-203.
104 New dimension of statin action on ApoB atherogenicity. Clin Cardiol. 2003 Jan;26(1 Suppl 1):I7-10.
105 Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
106 Microarray and biochemical analysis of lovastatin-induced apoptosis of squamous cell carcinomas. Neoplasia. 2002 Jul-Aug;4(4):337-46.
107 Inhibitory effect of delta-tocotrienol, a HMG CoA reductase inhibitor, on monocyte-endothelial cell adhesion. J Nutr Sci Vitaminol (Tokyo). 2002 Oct;48(5):332-7.
108 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
109 Canadian Pharmacists Association.
110 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
111 Cerner Multum, Inc. "Australian Product Information.".
112 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
113 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
114 Holtzman CW, Wiggins BS, Spinler SA "Role of P-glycoprotein in statin drug interactions." Pharmacotherapy 26 (2006): 1601-7. [PMID: 17064205]
115 Agbin NE, Brater DC, Hall SD "Interaction of diltiazem with lovastatin and pravastatin." Clin Pharmacol Ther 61 (1997): 201. [PMID: 9797793]
116 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
117 Andreou ER, Ledger S "Potential drug interaction between simvastatin and danazol causing rhabdomyolysis." Can J Clin Pharmacol 10 (2003): 172-4. [PMID: 14712320]
118 Ayanian JZ, Fuchs CS, Stone RM "Lovastatin and rhabdomyolysis." Ann Intern Med 109 (1988): 682-3. [PMID: 3421582]
119 Product Information. Ketek (telithromycin). Aventis Pharmaceuticals, Bridgewater, NJ.
120 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
121 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
122 Product Information. Talzenna (talazoparib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
123 Alderman CP "Possible interaction between nefazodone and pravastatin." Ann Pharmacother 33 (1999): 871. [PMID: 10466919]
124 Gaw A, Wosornu D "Simvastatin during warfarin therapy in hyperlipoproteinaemia." Lancet 340 (1992): 979-80. [PMID: 1357387]
125 He K, Woolf TF, Hollenberg PF "Mechanism-based inactivation of cytochrome P-450-3A4 by mifepristone (RU486)." J Pharmacol Exp Ther 288 (1999): 791-7. [PMID: 9918590]
126 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
127 Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ.
128 Product Information. Trileptal (oxcarbazepine) Novartis Pharmaceuticals, East Hanover, NJ.
129 EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
130 Akram K, Rao S, Parker M "A lesson for everyone in drug-drug interactions." Int J Cardiol 118 (2007): e19-20. [PMID: 17368833]
131 Product Information. Olysio (simeprevir). Janssen Pharmaceuticals, Titusville, NJ.
132 Bogman K, Peyer AK, Torok M, Kusters E, Drewe J "HMG-CoA reductase inhibitors and P-glycoprotein modulation." Br J Pharmacol 132 (2001): 1183-92. [PMID: 11250868]
133 Product Information. Priftin (rifapentine). Hoechst Marion-Roussel Inc, Kansas City, MO.
134 Product Information. Accolate (zafirlukast). Zeneca Pharmaceuticals, Wilmington, DE.
135 Product Information. Rescriptor (delavirdine). Pharmacia and Upjohn, Kalamazoo, MI.
136 Barry M, Mulcahy F, Merry C, Gibbons S, Back D "Pharmacokinetics and potential interactions amongst antiretroviral agents used to treat patients with HIV infection." Clin Pharmacokinet 36 (1999): 289-304. [PMID: 10320951]
137 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
138 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
139 Argov Z, Mastaglia FL "Drug-induced peripheral neuropathies." Br Med J 1 (1979): 663-6. [PMID: 219931]
140 Product Information. Zocor (simvastatin). Merck & Co, Inc, West Point, PA.
141 Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
142 Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
143 Blakely KM, Drucker AM, Rosen CF "Drug-induced photosensitivity-an update: Culprit drugs, prevention and management." Drug Saf 42 (2019): 827-47. [PMID: 30888626]
144 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
145 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]
146 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
147 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
148 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
149 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
150 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
151 Benoist G, van Oort I, et al "Drug-drug interaction potential in men treated with enzalutamide: Mind the gap." Br J Clin Pharmacol 0 (2017): epub. [PMID: 28881501]
152 Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
153 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
154 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
155 Barshes NR, Goodpastor SE, Goss JA "Sirolimus-atorvastatin drug interaction in the pancreatic islet transplant recipient." Transplantation 76 (2003): 1649-50. [PMID: 14702546]
156 Product Information. Farxiga (dapagliflozin). Bristol-Myers Squibb, Princeton, NJ.
157 Chouhan UM, Chakrabarti S, Millward LJ "Simvastatin interaction with clarithromycin and amiodarone causing myositis." Ann Pharmacother 39 (2005): 1760-1. [PMID: 16159992]