General Information of Drug (ID: DM5SXUV)

Drug Name
Repaglinide
Synonyms
Actulin; GlucoNorm; NovoNorm; Prandin; Repaglinida; Repaglinidum; Glaxo Wellcome brand of replaginide; Novo Nordisk brand of repaglinide; Repaglinide [USAN]; Novo Nordisk brand 2 of repaglinide; AG-EE 388; AG-EE 388 ZW; AG-EE 623 ZW; AGEE-623ZW; GlucoNorm (TN); NN-623; NovoNorm (TN); Prandin (TN); Repa-glinide; Repaglinida [INN-Spanish]; Repaglinidum [INN-Latin]; SMP-508; AG-EE-388; AG-EE-623 ZW; Prandin, GlucoNorm, NovoNorm, Repaglinide; Repaglinide (JAN/USP/INN); Repaglinide, (+-)-isomer; (+)-2-Ethoxy-alpha-(((S)-alpha-isobutyl-o-piperidinobenzyl)carbamoyl)-p-toluic acid; (S)-(+)-2-Ethoxy-4-[N-[1-(2-piperidinophenyl)-3-methyl-1-butyl]aminocarbonylmethyl]benzoic acid; (S)-2-Ethoxy-4-(2-((methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)-benzoic acid; (S)-2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)-phenyl)butyl)amino)-2-oxoethyl)-benzoic acid; 111GE012; 2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)benzoic acid; 2-ethoxy-4-(2-{[(1S)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino}-2-oxoethyl)benzoic acid; 2-ethoxy-4-[2-({(1S)-3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl}amino)-2-oxoethyl]benzoic acid; 2-ethoxy-4-[2-[[(1S)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino]-2-oxoethyl]benzoic acid; 2-ethoxy-N-(alpha-(2-methyl-1-propyl)-2-piperidinobenzyl)-4-carbamoylmethylbenzoic acid
Indication
Disease Entry ICD 11 Status REF
Diabetic complication 5A2Y Approved [1], [2]
Therapeutic Class
Hypoglycemic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 452.6
Topological Polar Surface Area (xlogp) 5.2
Rotatable Bond Count (rotbonds) 10
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Bioavailability
56% of drug becomes completely available to its intended biological destination(s) [4]
Clearance
The drug present in the plasma can be removed from the body at the rate of 7.8 mL/min/kg [5]
Elimination
1.5% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 1 hours [5]
Metabolism
The drug is metabolized via oxidation and dealkylation by cytochrome P450 3A4 and 2C9 to form the major dicarboxylic acid derivative (M2) [6]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.473 micromolar/kg/day [7]
Unbound Fraction
The unbound fraction of drug in plasma is 0.015% [5]
Vd
The volume of distribution (Vd) of drug is 31 L [8]
Chemical Identifiers
Formula
C27H36N2O4
IUPAC Name
2-ethoxy-4-[2-[[(1S)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino]-2-oxoethyl]benzoic acid
Canonical SMILES
CCOC1=C(C=CC(=C1)CC(=O)N[C@@H](CC(C)C)C2=CC=CC=C2N3CCCCC3)C(=O)O
InChI
InChI=1S/C27H36N2O4/c1-4-33-25-17-20(12-13-22(25)27(31)32)18-26(30)28-23(16-19(2)3)21-10-6-7-11-24(21)29-14-8-5-9-15-29/h6-7,10-13,17,19,23H,4-5,8-9,14-16,18H2,1-3H3,(H,28,30)(H,31,32)/t23-/m0/s1
InChIKey
FAEKWTJYAYMJKF-QHCPKHFHSA-N
Cross-matching ID
PubChem CID
65981
ChEBI ID
CHEBI:8805
CAS Number
135062-02-1
DrugBank ID
DB00912
TTD ID
D0N5YA
VARIDT ID
DR00446
INTEDE ID
DR1404
ACDINA ID
D00587

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
ATP-binding cassette transporter C8 (ABCC8) TTP835K ABCC8_HUMAN Blocker [9], [10], [11]
ATP-binding cassette transporter C9 (ABCC9) TTEF5MJ ABCC9_HUMAN Blocker [9], [10], [11]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_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]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [14]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [13]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Diabetic complication
ICD Disease Classification 5A2Y
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
ATP-binding cassette transporter C9 (ABCC9) DTT ABCC9 6.51E-01 0.02 0.06
ATP-binding cassette transporter C9 (ABCC9) DTT ABCC9 8.46E-01 0.02 0.22
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 2.41E-01 -2.63E-02 -8.50E-02
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 5.54E-01 -1.65E-02 -1.24E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 8.29E-01 -5.44E-03 -2.25E-02
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 4.23E-03 9.31E-02 4.30E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 2.41E-01 3.17E-02 2.29E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 5.67E-01 5.11E-02 1.35E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 2.13E-01 4.03E-02 2.50E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 8.21E-02 8.17E-02 4.35E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Repaglinide
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Pioglitazone DMKJ485 Moderate Increased metabolism of Repaglinide caused by Pioglitazone mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [63]
Coadministration of a Drug Treating the Disease Different from Repaglinide (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Moderate Increased metabolism of Repaglinide caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [64]
Arn-509 DMT81LZ Moderate Increased metabolism of Repaglinide caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [64]
Dronedarone DMA8FS5 Moderate Decreased metabolism of Repaglinide caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [64]
Nifedipine DMSVOZT Moderate Decreased metabolism of Repaglinide caused by Nifedipine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [64]
Oxymetholone DMFXUT8 Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Oxymetholone. Aplastic anaemia [3A70] [65]
Posaconazole DMUL5EW Moderate Decreased metabolism of Repaglinide caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [64]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Repaglinide caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [66]
Clarithromycin DM4M1SG Moderate Decreased metabolism of Repaglinide caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [64]
Sulfamethoxazole DMB08GE Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Sulfamethoxazole. Bacterial infection [1A00-1C4Z] [65]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Repaglinide caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [64]
Telithromycin DMZ4P3A Moderate Decreased metabolism of Repaglinide caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [64]
Ag-221 DMS0ZBI Moderate Decreased clearance of Repaglinide due to the transporter inhibition by Ag-221. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [67]
Pexidartinib DMS2J0Z Moderate Increased metabolism of Repaglinide caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [64]
Lapatinib DM3BH1Y Moderate Decreased metabolism of Repaglinide caused by Lapatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [64]
Tucatinib DMBESUA Moderate Decreased metabolism of Repaglinide caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [64]
Fluoxymesterone DMUHCF1 Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Fluoxymesterone. Breast cancer [2C60-2C6Y] [65]
Fenofibric acid DMGO2MC Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Fenofibric acid. Cardiovascular disease [BA00-BE2Z] [65]
Ketoprofen DMRKXPT Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Ketoprofen. Chronic pain [MG30] [65]
Ardeparin DMYRX8B Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Ardeparin. Coronary thrombosis [BA43] [65]
Lumacaftor DMCLWDJ Moderate Increased metabolism of Repaglinide caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [68]
MK-8228 DMOB58Q Moderate Decreased metabolism of Repaglinide caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [64]
Sertraline DM0FB1J Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Sertraline. Depression [6A70-6A7Z] [65]
Vilazodone DM4LECQ Moderate Decreased metabolism of Repaglinide caused by Vilazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [64]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Repaglinide caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [64]
Selegiline DM6034S Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Selegiline. Depression [6A70-6A7Z] [65]
Vortioxetine DM6F1PU Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Vortioxetine. Depression [6A70-6A7Z] [65]
Isocarboxazid DMAF1NB Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Isocarboxazid. Depression [6A70-6A7Z] [65]
Escitalopram DMFK9HG Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Escitalopram. Depression [6A70-6A7Z] [65]
Felbamate DM1V5ZS Moderate Increased metabolism of Repaglinide caused by Felbamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [64]
Cenobamate DMGOVHA Moderate Increased metabolism of Repaglinide caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [64]
Stiripentol DMMSDOY Moderate Decreased metabolism of Repaglinide caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [64]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Repaglinide caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [64]
Phenobarbital DMXZOCG Moderate Increased metabolism of Repaglinide caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [64]
Tazemetostat DMWP1BH Moderate Decreased metabolism of Repaglinide caused by Tazemetostat mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [64]
Miconazole DMPMYE8 Moderate Decreased metabolism of Repaglinide caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [64]
Ketoconazole DMPZI3Q Moderate Decreased metabolism of Repaglinide caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [64]
Ripretinib DM958QB Moderate Decreased metabolism of Repaglinide caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [64]
Sunitinib DMCBJSR Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Sunitinib. Gastrointestinal stromal tumour [2B5B] [65]
Sulfinpyrazone DMEV954 Moderate Increased metabolism of Repaglinide caused by Sulfinpyrazone mediated induction of CYP450 enzyme. Gout [FA25] [64]
Boceprevir DMBSHMF Moderate Decreased metabolism of Repaglinide caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [64]
Telaprevir DMMRV29 Moderate Decreased metabolism of Repaglinide caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [64]
Rifampin DMA8J1G Moderate Increased metabolism of Repaglinide caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [64]
Rifapentine DMCHV4I Moderate Increased metabolism of Repaglinide caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [64]
Fosamprenavir DM4W9B3 Moderate Increased metabolism of Repaglinide caused by Fosamprenavir mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [69]
Fostemsavir DM50ILT Moderate Decreased clearance of Repaglinide due to the transporter inhibition by Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [70]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Repaglinide caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [64]
Saquinavir DMG814N Moderate Increased metabolism of Repaglinide caused by Saquinavir mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [69]
Etravirine DMGV8QU Moderate Increased metabolism of Repaglinide caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [64]
Darunavir DMN3GCH Moderate Antagonize the effect of Repaglinide when combined with Darunavir. Human immunodeficiency virus disease [1C60-1C62] [69]
Atazanavir DMSYRBX Moderate Increased metabolism of Repaglinide caused by Atazanavir mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [69]
Bempedoic acid DM1CI9R Moderate Decreased clearance of Repaglinide due to the transporter inhibition by Bempedoic acid. Hyper-lipoproteinaemia [5C80] [71]
Gemfibrozil DMD8Q3J Major Decreased clearance of Repaglinide due to the transporter inhibition by Gemfibrozil. Hyper-lipoproteinaemia [5C80] [64]
Fenofibrate DMFKXDY Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Fenofibrate. Hyper-lipoproteinaemia [5C80] [65]
Teriflunomide DMQ2FKJ Moderate Decreased metabolism of Repaglinide caused by Teriflunomide mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [72]
Captopril DM458UM Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Captopril. Hypertension [BA00-BA04] [65]
Probenecid DMMFWOJ Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Probenecid. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [65]
Balsalazide DMO091F Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Balsalazide. Indeterminate colitis [DD72] [65]
Meclofenamic acid DM05FXR Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Meclofenamic acid. Inflammatory spondyloarthritis [FA92] [73]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Repaglinide caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [64]
Amobarbital DM0GQ8N Moderate Increased metabolism of Repaglinide caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [64]
Crizotinib DM4F29C Moderate Decreased metabolism of Repaglinide caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [64]
PF-06463922 DMKM7EW Moderate Increased metabolism of Repaglinide caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [64]
Selpercatinib DMZR15V Moderate Decreased metabolism of Repaglinide caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [64]
Hydroxychloroquine DMSIVND Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Hydroxychloroquine. Malaria [1F40-1F45] [65]
Sulphadoxine DMZI2UF Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Sulphadoxine. Malaria [1F40-1F45] [65]
Idelalisib DM602WT Moderate Decreased metabolism of Repaglinide caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [64]
IPI-145 DMWA24P Moderate Decreased metabolism of Repaglinide caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [64]
Vemurafenib DM62UG5 Moderate Increased metabolism of Repaglinide caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [64]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Repaglinide caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [67]
Exjade DMHPRWG Moderate Decreased metabolism of Repaglinide caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [74]
Mecasermin DM1O3BY Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Mecasermin. Multiple structural anomalies syndrome [LD2F] [65]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Repaglinide caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [64]
Nilotinib DM7HXWT Moderate Decreased metabolism of Repaglinide caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [64]
Netupitant DMEKAYI Moderate Decreased metabolism of Repaglinide caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [66]
Olaparib DM8QB1D Moderate Decreased clearance of Repaglinide due to the transporter inhibition by Olaparib. Ovarian cancer [2C73] [67]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Repaglinide caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [64]
Aspirin DM672AH Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Aspirin. Pain [MG30-MG3Z] [73]
Ibuprofen DM8VCBE Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Ibuprofen. Pain [MG30-MG3Z] [65]
Safinamide DM0YWJC Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Safinamide. Parkinsonism [8A00] [65]
Rasagiline DM3WKQ4 Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Rasagiline. Parkinsonism [8A00] [65]
Abametapir DM2RX0I Moderate Decreased metabolism of Repaglinide caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [75]
Lefamulin DME6G97 Moderate Decreased metabolism of Repaglinide caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [76]
Choline salicylate DM8P137 Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Choline salicylate. Postoperative inflammation [1A00-CA43] [65]
Bromfenac DMKB79O Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Bromfenac. Postoperative inflammation [1A00-CA43] [65]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Repaglinide caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [64]
ABIRATERONE DM8V75C Moderate Decreased metabolism of Repaglinide caused by ABIRATERONE mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [64]
Enzalutamide DMGL19D Moderate Increased metabolism of Repaglinide caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [64]
Darolutamide DMV7YFT Moderate Decreased clearance of Repaglinide due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [77]
Bicalutamide DMZMSPF Moderate Decreased metabolism of Repaglinide caused by Bicalutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [64]
Salsalate DM13P4C Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Salsalate. Rheumatoid arthritis [FA20] [65]
Oxaprozin DM9UB0P Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Oxaprozin. Rheumatoid arthritis [FA20] [65]
Salicyclic acid DM2F8XZ Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Salicyclic acid. Seborrhoeic dermatitis [EA81] [73]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Repaglinide caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [64]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Repaglinide caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [77]
Larotrectinib DM26CQR Moderate Decreased metabolism of Repaglinide caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [67]
Ifosfamide DMCT3I8 Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Ifosfamide. Solid tumour/cancer [2A00-2F9Z] [65]
Armodafinil DMGB035 Moderate Increased metabolism of Repaglinide caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [64]
LEE011 DMMX75K Moderate Decreased metabolism of Repaglinide caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [64]
Methyltestosterone DMWLFGO Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Methyltestosterone. Solid tumour/cancer [2A00-2F9Z] [65]
Pitolisant DM8RFNJ Moderate Increased metabolism of Repaglinide caused by Pitolisant mediated induction of CYP450 enzyme. Somnolence [MG42] [77]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Repaglinide caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [78]
Eltrombopag DMOGFIX Moderate Decreased clearance of Repaglinide due to the transporter inhibition by Eltrombopag. Thrombocytopenia [3B64] [79]
Pramlintide DM0EZ9Q Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Pramlintide. Type-1/2 diabete [5A10-5A11] [65]
Olsalazine DMZW9HA Moderate Increased risk of hypoglycemia by the combination of Repaglinide and Olsalazine. Ulcerative colitis [DD71] [65]
Elagolix DMB2C0E Moderate Increased metabolism of Repaglinide caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [64]
Amiodarone DMUTEX3 Moderate Decreased metabolism of Repaglinide caused by Amiodarone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [64]
⏷ Show the Full List of 106 DDI Information of This Drug

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

DIG
DIG Name DIG ID PubChem CID Functional Classification
FD&C blue no. 1 E00263 19700 Colorant
Meglumine E00181 8567 Buffering agent
Quinoline yellow WS E00309 24671 Colorant
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Butylhydroxyanisole E00308 24667 Antimicrobial preservative; Antioxidant
Calcium hydrogenphosphate E00294 24441 Diluent
Carmellose sodium E00625 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Glycerin E00026 753 Antimicrobial preservative; Emollient; Flavoring agent; Humectant; Lubricant; Plasticizing agent; Solvent; Suppository base; Tonicity agent; Viscosity-controlling agent
Magnesium stearate E00208 11177 lubricant
Poloxamer 188 E00645 Not Available Emulsifying agent; Solubilizing agent; Surfactant
Poloxamer 407 E00646 Not Available Emulsifying agent; Solubilizing agent; Surfactant
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
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
⏷ Show the Full List of 17 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Repaglinide 0.5 mg tablet 0.5 mg Oral Tablet Oral
Repaglinide 1 mg tablet 1 mg Oral Tablet Oral
Repaglinide 2 mg tablet 2 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: 6841).
2 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 077571.
3 BDDCS applied to over 900 drugs
4 Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
5 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
6 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
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 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
9 Metformin/Repaglinide (PrandiMet) for type 2 diabetes. Med Lett Drugs Ther. 2009 Jun 1;51(1313):41-3.
10 Pharmacological modulation of K(ATP) channels. Biochem Soc Trans. 2002 Apr;30(2):333-9.
11 Clinical pharmacokinetics and pharmacodynamics of repaglinide. Clin Pharmacokinet. 2002;41(7):471-83.
12 Disease-Associated Changes in Drug Transporters May Impact the Pharmacokinetics and/or Toxicity of Drugs: A White Paper From the International Transporter Consortium. Clin Pharmacol Ther. 2018 Nov;104(5):900-915.
13 Drug-drug and food-drug pharmacokinetic interactions with new insulinotropic agents repaglinide and nateglinide. Clin Pharmacokinet. 2007;46(2):93-108.
14 Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism. Br J Clin Pharmacol. 2010 Dec;70(6):870-80.
15 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
16 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
17 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
18 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
19 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
20 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
21 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
22 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
23 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
24 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
25 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
26 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
27 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.
28 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.
29 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.
30 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
31 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.
32 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.
33 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
34 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.
35 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
36 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
37 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
38 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
39 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.
40 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
41 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
42 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
43 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
44 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
45 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.
46 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.
47 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.
48 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
49 FDA Drug Development and Drug Interactions
50 Expression of an activating mutation in the gene encoding the KATP channel subunit Kir6.2 in mouse pancreatic beta cells recapitulates neonatal diabetes. J Clin Invest. 2009 Jan;119(1):80-90.
51 Mechanism of disopyramide-induced hypoglycaemia in a patient with Type 2 diabetes. Diabet Med. 2009 Jan;26(1):76-8.
52 A functional role of the C-terminal 42 amino acids of SUR2A and SUR2B in the physiology and pharmacology of cardiovascular ATP-sensitive K(+) chann... J Mol Cell Cardiol. 2005 Jul;39(1):1-6.
53 BTS-67582 (Knoll Pharmaceuticals Co). IDrugs. 1999 Apr;2(4):355-9.
54 Effects of KRN2391 on ionic currents in rabbit femoral arterial myocytes
55 Analysis of the differential modulation of sulphonylurea block of beta-cell and cardiac ATP-sensitive K+ (K(ATP)) channels by Mg-nucleotides. J Physiol. 2003 Feb 15;547(Pt 1):159-68.
56 The mitochondrial K(ATP) channel opener BMS-191095 reduces neuronal damage after transient focal cerebral ischemia in rats.J Cereb Blood Flow Metab.2007 Feb;27(2):348-55.
57 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
58 Diabetes and insulin secretion: the ATP-sensitive K+ channel (K ATP) connection.Diabetes.2005 Nov;54(11):3065-72.
59 Structural basis for the interference between nicorandil and sulfonylurea action. Diabetes. 2001 Oct;50(10):2253-9.
60 Attenuation of hyperinsulinemia by NN414, a SUR1/Kir6.2 selective K-adenosine triphosphate channel opener, improves glucose tolerance and lipid profile in obese Zucker rats.Metabolism.2004 Apr;53(4):441-7.
61 Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas. J Med Chem. 2001 Mar 29;44(7):1085-98.
62 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: 2944).
63 Product Information. Actos (pioglitazone) Takeda Pharmaceuticals America, Lincolnshire, IL.
64 Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT "CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide." Br J Clin Pharmacol 56 (2003): 305-14. [PMID: 12919179]
65 Abad S, Moachon L, Blanche P, Bavoux F, Sicard D, Salmon-Ceron D "Possible interaction between glicazide, fluconazole and sulfamethoxazole resulting in severe hypoglycaemia." Br J Clin Pharmacol 52 (2001): 456-7. [PMID: 11678792]
66 Hatorp V, Hansen KT, Thomsen MS "Influence of drugs interacting with CYP3A4 on the pharmacokinetics, pharmacodynamics, and safety of the prandial glucose regulator repaglinide." J Clin Pharmacol 43 (2003): 649-60. [PMID: 12817528]
67 Cerner Multum, Inc. "Australian Product Information.".
68 Cerner Multum, Inc. "Canadian Product Information.".
69 Dube MP, Johnson DL, Currier JS, Leedom JM "Protease inhibitor-associated hyperglycaemia." Lancet 350 (1997): 713-4. [PMID: 9291911]
70 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
71 Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
72 Product Information. Aubagio (teriflunomide). Genzyme Corporation, Cambridge, MA.
73 Christensen LK, Hansen JM, Kristensen M "Sulphaphenazole-induced hypoglycemic attacks in tolbutamide-treated diabetics." Lancet 2 (1963): 1298-301. [PMID: 14071924]
74 Canadian Pharmacists Association.
75 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
76 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
77 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
78 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
79 Allred AJ, Bowen CJ, Park JW, et al. "Eltrombopag increases plasma rosuvastatin exposure in healthy volunteers." Br J Clin Pharmacol 72 (2011): 321-9. [PMID: 21434975]