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
Arteriosclerosis BD40 Approved [1]
Atherosclerosis BD40 Approved [1]
Coronary heart disease BA80.Z Approved [1]
Cystic fibrosis CA25 Approved [1]
Depression 6A70-6A7Z Approved [1]
Hypercholesterolaemia 5C80.0 Approved [2]
Hyperlipidemia 5C80.Z Approved [1]
Hyperlipidemia, familial combined, LPL related N.A. Approved [1]
Hypertriglyceridemia 5C80.1 Approved [1]
Pneumonia CA40 Approved [1]
Primary hypercholesterolemia 5C80.00 Approved [1]
Prostate carcinoma N.A. Approved [1]
Rhinitis FA20 Approved [1]
Type-1/2 diabetes 5A10-5A11 Approved [1]
Stroke 8B20 Investigative [1]
⏷ Show the Full List of Indication(s)
Therapeutic Class
Anticholesteremic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 418.6
Logarithm of the Partition Coefficient (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 []
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 [5]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.3652 micromolar/kg/day [6]
Water Solubility
The ability of drug to dissolve in water is measured as 0.03 mg/mL [4]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Acute myocardial infarction Not Available MMP3 OTGBI74Z [7]
Arteriosclerosis Not Available CES1 OT9L0LR8 [7]
Cardiovascular disorder rs20455 KIF6 OTDH3MR4 [8]
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
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

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 [9]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [10]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [11]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [12]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [13]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [14]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [15]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Substrate [15]
Cytochrome P450 3A5 (CYP3A5)
Main DME
DEIBDNY CP3A5_HUMAN Substrate [16]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [17]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Substrate [15]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_HUMAN Substrate [15]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-2 (PLCG2) OTGVC9MY PLCG2_HUMAN Gene/Protein Processing [18]
3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMGCR) OTRT3F3U HMDH_HUMAN Drug Response [19]
5-hydroxytryptamine receptor 3B (HTR3B) OTMGIYRE 5HT3B_HUMAN Drug Response [20]
5-hydroxytryptamine receptor 7 (HTR7) OT44DEWB 5HT7R_HUMAN Drug Response [20]
7-dehydrocholesterol reductase (DHCR7) OTLILBUI DHCR7_HUMAN Gene/Protein Processing [21]
72 kDa type IV collagenase (MMP2) OT5NIWA2 MMP2_HUMAN Gene/Protein Processing [22]
Advanced glycosylation end product-specific receptor (AGER) OTPY0IH7 RAGE_HUMAN Gene/Protein Processing [23]
Aldehyde dehydrogenase, dimeric NADP-preferring (ALDH3A1) OTAYZZE6 AL3A1_HUMAN Gene/Protein Processing [18]
Aldo-keto reductase family 1 member C1 (AKR1C1) OTQKR4CM AK1C1_HUMAN Gene/Protein Processing [18]
Aldo-keto reductase family 1 member C3 (AKR1C3) OTU2SXBA AK1C3_HUMAN Gene/Protein Processing [24]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Arteriosclerosis
ICD Disease Classification BD40
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] [25]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Simvastatin and Teriflunomide. Hyper-lipoproteinaemia [5C80] [26]
BMS-201038 DMQTAGO Major Decreased metabolism of Simvastatin caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [27]
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] [28]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Simvastatin caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [29]
Midostaurin DMI6E0R Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Midostaurin. Acute myeloid leukaemia [2A60] [30]
Arn-509 DMT81LZ Moderate Increased metabolism of Simvastatin caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [30]
Emapalumab DMZG5WL Moderate Altered metabolism of Simvastatin due to Emapalumab alters the formation of CYP450 enzymes. Adaptive immunity immunodeficiency [4A01] [30]
Siltuximab DMGEATB Moderate Altered metabolism of Simvastatin due to Siltuximab alters the formation of CYP450 enzymes. Anemia [3A00-3A9Z] [30]
Dronedarone DMA8FS5 Major Decreased clearance of Simvastatin due to the transporter inhibition by Dronedarone. Angina pectoris [BA40] [31]
Nifedipine DMSVOZT Moderate Decreased metabolism of Simvastatin caused by Nifedipine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [32]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [33]
Posaconazole DMUL5EW Major Decreased metabolism of Simvastatin caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [28]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Simvastatin caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [34]
Clarithromycin DM4M1SG Major Decreased metabolism of Simvastatin caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [35]
Troleandomycin DMUZNIG Major Decreased metabolism of Simvastatin caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [35]
Telithromycin DMZ4P3A Major Decreased metabolism of Simvastatin caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [36]
Ag-221 DMS0ZBI Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Ag-221. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [28]
Erdafitinib DMI782S Moderate Increased metabolism of Simvastatin caused by Erdafitinib mediated induction of CYP450 enzyme. Bladder cancer [2C94] [37]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Simvastatin and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [38]
Talazoparib DM1KS78 Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [39]
Lapatinib DM3BH1Y Moderate Decreased metabolism of Simvastatin caused by Lapatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [32]
Tucatinib DMBESUA Major Decreased metabolism of Simvastatin caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [40]
Palbociclib DMD7L94 Moderate Decreased metabolism of Simvastatin caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [32]
Anisindione DM2C48U Minor Increased plasma concentration of Simvastatin and Anisindione due to competitive binding of plasma proteins. Coagulation defect [3B10] [41]
Mifepristone DMGZQEF Major Decreased metabolism of Simvastatin caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [42]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Simvastatin caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [32]
Lumacaftor DMCLWDJ Major Increased metabolism of Simvastatin caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [28]
Ivacaftor DMZC1HS Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Ivacaftor. Cystic fibrosis [CA25] [43]
MK-8228 DMOB58Q Major Decreased clearance of Simvastatin due to the transporter inhibition by MK-8228. Cytomegaloviral disease [1D82] [44]
Aprepitant DM053KT Moderate Decreased metabolism of Simvastatin caused by Aprepitant mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [32]
Nefazodone DM4ZS8M Major Decreased metabolism of Simvastatin caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [40]
Oxcarbazepine DM5PU6O Moderate Increased metabolism of Simvastatin caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [45]
Stiripentol DMMSDOY Moderate Decreased metabolism of Simvastatin caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [46]
Rufinamide DMWE60C Moderate Increased metabolism of Simvastatin caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [30]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Simvastatin caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [30]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Cannabidiol. Epileptic encephalopathy [8A62] [30]
Itraconazole DMCR1MV Major Decreased metabolism of Simvastatin caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [26]
Miconazole DMPMYE8 Moderate Decreased metabolism of Simvastatin caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [30]
Ketoconazole DMPZI3Q Major Decreased metabolism of Simvastatin caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [47]
Boceprevir DMBSHMF Major Decreased metabolism of Simvastatin caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [35]
Simeprevir DMLUA9D Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Simeprevir. Hepatitis virus infection [1E50-1E51] [48]
Telaprevir DMMRV29 Major Decreased metabolism of Simvastatin caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [35]
Rifampin DMA8J1G Major Increased metabolism of Simvastatin caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [49]
Rifapentine DMCHV4I Moderate Increased metabolism of Simvastatin caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [50]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Brentuximab vedotin. Hodgkin lymphoma [2B30] [51]
Delavirdine DM3NF5G Major Decreased metabolism of Simvastatin caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [52]
Fosamprenavir DM4W9B3 Major Decreased metabolism of Simvastatin caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
Fostemsavir DM50ILT Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [54]
Cobicistat DM6L4H2 Major Decreased metabolism of Simvastatin caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [40]
Tipranavir DM8HJX6 Major Decreased metabolism of Simvastatin caused by Tipranavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
Saquinavir DMG814N Major Decreased metabolism of Simvastatin caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
Etravirine DMGV8QU Moderate Increased metabolism of Simvastatin caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [55]
Zalcitabine DMH7MUV Moderate Increased risk of peripheral neuropathy by the combination of Simvastatin and Zalcitabine. Human immunodeficiency virus disease [1C60-1C62] [56]
Amprenavir DMLMXE0 Major Decreased metabolism of Simvastatin caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
Darunavir DMN3GCH Major Decreased metabolism of Simvastatin caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
Atazanavir DMSYRBX Major Decreased metabolism of Simvastatin caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
Levamlodipine DM92S6N Major Decreased metabolism of Simvastatin caused by Levamlodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [57]
Conivaptan DM1V329 Major Decreased metabolism of Simvastatin caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [35]
Lesinurad DMUR64T Moderate Increased metabolism of Simvastatin caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [58]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Simvastatin caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [32]
Suvorexant DM0E6S3 Moderate Decreased metabolism of Simvastatin caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [32]
Crizotinib DM4F29C Moderate Decreased metabolism of Simvastatin caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [32]
Brigatinib DM7W94S Moderate Increased metabolism of Simvastatin caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [59]
Porfimer Sodium DM7ZWNY Moderate Increased risk of photosensitivity reactions by the combination of Simvastatin and Porfimer Sodium. Lung cancer [2C25] [60]
Ceritinib DMB920Z Major Decreased metabolism of Simvastatin caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [40]
PF-06463922 DMKM7EW Moderate Increased metabolism of Simvastatin caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [61]
Osimertinib DMRJLAT Moderate Increased metabolism of Simvastatin caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [30]
Selpercatinib DMZR15V Moderate Decreased metabolism of Simvastatin caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [32]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [62]
Idelalisib DM602WT Major Decreased metabolism of Simvastatin caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [40]
IPI-145 DMWA24P Moderate Decreased metabolism of Simvastatin caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [32]
Arry-162 DM1P6FR Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Arry-162. Melanoma [2C30] [28]
LGX818 DMNQXV8 Moderate Increased metabolism of Simvastatin caused by LGX818 mediated induction of CYP450 enzyme. Melanoma [2C30] [63]
Dabrafenib DMX6OE3 Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Dabrafenib. Melanoma [2C30] [28]
Danazol DML8KTN Major Decreased metabolism of Simvastatin caused by Danazol mediated inhibition of CYP450 enzyme. Menstrual cycle bleeding disorder [GA20] [34]
Exjade DMHPRWG Moderate Decreased metabolism of Simvastatin caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [64]
Thalidomide DM70BU5 Moderate Increased risk of peripheral neuropathy by the combination of Simvastatin and Thalidomide. Multiple myeloma [2A83] [56]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Simvastatin caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [32]
Dasatinib DMJV2EK Moderate Decreased metabolism of Simvastatin caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [32]
Modafinil DMYILBE Moderate Increased metabolism of Simvastatin caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [28]
Netupitant DMEKAYI Moderate Decreased metabolism of Simvastatin caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [34]
Entrectinib DMMPTLH Moderate Decreased metabolism of Simvastatin caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [32]
Olaparib DM8QB1D Moderate Decreased metabolism of Simvastatin caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [28]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Simvastatin caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [32]
Abametapir DM2RX0I Moderate Decreased metabolism of Simvastatin caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [65]
Esomeprazole DM7BN0X Moderate Increased plasma concentrations of Simvastatin and Esomeprazole due to competitive inhibition of the same metabolic pathway. Peptic ulcer [DA61] [49]
Lefamulin DME6G97 Moderate Decreased metabolism of Simvastatin caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [66]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Simvastatin caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [67]
Enzalutamide DMGL19D Moderate Increased metabolism of Simvastatin caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [68]
Darolutamide DMV7YFT Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [30]
Bicalutamide DMZMSPF Moderate Decreased metabolism of Simvastatin caused by Bicalutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [32]
Ustekinumab DMHTYK3 Moderate Altered metabolism of Simvastatin due to Ustekinumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [30]
Ixekizumab DMXW92T Moderate Altered metabolism of Simvastatin due to Ixekizumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [30]
Tocilizumab DM7J6OR Moderate Altered metabolism of Simvastatin due to Tocilizumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [30]
Canakinumab DM8HLO5 Moderate Altered metabolism of Simvastatin due to Canakinumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [30]
Rilonacept DMGLUQS Moderate Altered metabolism of Simvastatin due to Rilonacept alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [30]
Sarilumab DMOGNXY Moderate Altered metabolism of Simvastatin due to Sarilumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [30]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Simvastatin and Leflunomide. Rheumatoid arthritis [FA20] [26]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Simvastatin caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [32]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Simvastatin caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [30]
Larotrectinib DM26CQR Moderate Decreased metabolism of Simvastatin caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [32]
Armodafinil DMGB035 Moderate Increased metabolism of Simvastatin caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [28]
LEE011 DMMX75K Moderate Decreased metabolism of Simvastatin caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [32]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Simvastatin and Naltrexone. Substance abuse [6C40] [69]
Warfarin DMJYCVW Minor Increased plasma concentration of Simvastatin and Warfarin due to competitive binding of plasma proteins. Supraventricular tachyarrhythmia [BC81] [41]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Simvastatin caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [70]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Simvastatin due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [71]
Brilinta DMBR01X Moderate Decreased metabolism of Simvastatin caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [30]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Simvastatin and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [72]
Tacrolimus DMZ7XNQ Moderate Increased plasma concentrations of Simvastatin and Tacrolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [72]
Albiglutide DM1JEGF Minor Altered absorption of Simvastatin due to GI dynamics variation caused by Albiglutide. Type 2 diabetes mellitus [5A11] [46]
Dapagliflozin DM28UJG Minor Increased plasma concentrations of Simvastatin and Dapagliflozin due to competitive inhibition of the same metabolic pathway. Type 2 diabetes mellitus [5A11] [73]
Amiodarone DMUTEX3 Major Decreased metabolism of Simvastatin caused by Amiodarone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [74]
⏷ 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 Simvastatin FDA Label
2 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).
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 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.
6 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
7 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
8 Association of the Trp719Arg polymorphism in kinesin-like protein 6 with myocardial infarction and coronary heart disease in 2 prospective trials: the CARE and WOSCOPS trials. J Am Coll Cardiol. 2008 Jan 29;51(4):435-43. doi: 10.1016/j.jacc.2007.05.057.
9 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.
10 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
11 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
12 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.
13 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.
14 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.
15 Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
16 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.
17 Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance. Clin Pharmacol Ther. 2006 Dec;80(6):565-81.
18 Simvastatin inactivates beta1-integrin and extracellular signal-related kinase signaling and inhibits cell proliferation in head and neck squamous cell carcinoma cells. Cancer Sci. 2007 Jun;98(6):890-9.
19 Alternative splicing of 3-hydroxy-3-methylglutaryl coenzyme A reductase is associated with plasma low-density lipoprotein cholesterol response to simvastatin. Circulation. 2008 Jul 22;118(4):355-62. doi: 10.1161/CIRCULATIONAHA.108.773267. Epub 2008 Jun 16.
20 Physiogenomic association of statin-related myalgia to serotonin receptors. Muscle Nerve. 2007 Sep;36(3):329-35. doi: 10.1002/mus.20871.
21 Hydroxychloroquine decreases human MSC-derived osteoblast differentiation and mineralization in vitro. J Cell Mol Med. 2018 Feb;22(2):873-882. doi: 10.1111/jcmm.13373. Epub 2017 Oct 3.
22 Impaired migration of trophoblast cells caused by simvastatin is associated with decreased membrane IGF-I receptor, MMP2 activity and HSP27 expression. Hum Reprod. 2007 Apr;22(4):1161-7. doi: 10.1093/humrep/del464. Epub 2006 Dec 11.
23 Suppression of RAGE as a basis of simvastatin-dependent plaque stabilization in type 2 diabetes. Arterioscler Thromb Vasc Biol. 2006 Dec;26(12):2716-23.
24 In-vivo effects of simvastatin and rosuvastatin on global gene expression in peripheral blood leucocytes in a human inflammation model. Pharmacogenet Genomics. 2008 Feb;18(2):109-20.
25 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
26 Canadian Pharmacists Association.
27 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
28 Cerner Multum, Inc. "Australian Product Information.".
29 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
30 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
31 Holtzman CW, Wiggins BS, Spinler SA "Role of P-glycoprotein in statin drug interactions." Pharmacotherapy 26 (2006): 1601-7. [PMID: 17064205]
32 Agbin NE, Brater DC, Hall SD "Interaction of diltiazem with lovastatin and pravastatin." Clin Pharmacol Ther 61 (1997): 201. [PMID: 9797793]
33 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
34 Andreou ER, Ledger S "Potential drug interaction between simvastatin and danazol causing rhabdomyolysis." Can J Clin Pharmacol 10 (2003): 172-4. [PMID: 14712320]
35 Ayanian JZ, Fuchs CS, Stone RM "Lovastatin and rhabdomyolysis." Ann Intern Med 109 (1988): 682-3. [PMID: 3421582]
36 Product Information. Ketek (telithromycin). Aventis Pharmaceuticals, Bridgewater, NJ.
37 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
38 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
39 Product Information. Talzenna (talazoparib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
40 Alderman CP "Possible interaction between nefazodone and pravastatin." Ann Pharmacother 33 (1999): 871. [PMID: 10466919]
41 Gaw A, Wosornu D "Simvastatin during warfarin therapy in hyperlipoproteinaemia." Lancet 340 (1992): 979-80. [PMID: 1357387]
42 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]
43 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
44 Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ.
45 Product Information. Trileptal (oxcarbazepine) Novartis Pharmaceuticals, East Hanover, NJ.
46 EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
47 Akram K, Rao S, Parker M "A lesson for everyone in drug-drug interactions." Int J Cardiol 118 (2007): e19-20. [PMID: 17368833]
48 Product Information. Olysio (simeprevir). Janssen Pharmaceuticals, Titusville, NJ.
49 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]
50 Product Information. Priftin (rifapentine). Hoechst Marion-Roussel Inc, Kansas City, MO.
51 Product Information. Accolate (zafirlukast). Zeneca Pharmaceuticals, Wilmington, DE.
52 Product Information. Rescriptor (delavirdine). Pharmacia and Upjohn, Kalamazoo, MI.
53 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]
54 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
55 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
56 Argov Z, Mastaglia FL "Drug-induced peripheral neuropathies." Br Med J 1 (1979): 663-6. [PMID: 219931]
57 Product Information. Zocor (simvastatin). Merck & Co, Inc, West Point, PA.
58 Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
59 Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
60 Blakely KM, Drucker AM, Rosen CF "Drug-induced photosensitivity-an update: Culprit drugs, prevention and management." Drug Saf 42 (2019): 827-47. [PMID: 30888626]
61 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
62 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]
63 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
64 Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
65 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
66 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
67 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
68 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]
69 Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
70 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
71 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
72 Barshes NR, Goodpastor SE, Goss JA "Sirolimus-atorvastatin drug interaction in the pancreatic islet transplant recipient." Transplantation 76 (2003): 1649-50. [PMID: 14702546]
73 Product Information. Farxiga (dapagliflozin). Bristol-Myers Squibb, Princeton, NJ.
74 Chouhan UM, Chakrabarti S, Millward LJ "Simvastatin interaction with clarithromycin and amiodarone causing myositis." Ann Pharmacother 39 (2005): 1760-1. [PMID: 16159992]