General Information of Drug (ID: DMKSQG0)

Drug Name
Tiagabine
Synonyms
tiagabine; 115103-54-3; Gabitril; Tiagabinum; Tiagabina; (R)-Tiagabine; Tiagabinum [INN-Latin]; Tiagabina [INN-Spanish]; Tiagabine [INN:BAN]; Tiagabine [INN]; Abbott-70569; UNII-Z80I64HMNP; Tiagabine (INN); ABBOTT-70569-1; Gabitril (TN); CHEMBL1027; Z80I64HMNP; ABT-569; CHEBI:9586; NO-328; (-)-(R)-1-(4,4-Bis(3-methyl-2-thienyl)-3-butenyl)nipecotic acid; A-70569-1; (R)-1-(4,4-Bis(3-methylthiophen-2-yl)but-3-en-1-yl)piperidine-3-carboxylic acid; Gabatril; NO 329; Gabitril; NO-329; Tiagabina [INN-Spanish];Tiagabine (INN); N-(4,4-di(3-methylthien-2-yl)but-3-enyl)nipecotic acid; (3R)-1-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]piperidine-3-carboxylic acid; (3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl]piperidine-3-carboxylic acid; [3H]tiagabine
Indication
Disease Entry ICD 11 Status REF
Epilepsy 8A60-8A68 Approved [1]
Anxiety disorder 6B00-6B0Z Phase 2 [1]
Therapeutic Class
Anticonvulsants
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 375.6
Logarithm of the Partition Coefficient (xlogp) 2.7
Rotatable Bond Count (rotbonds) 6
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
Absorption
The absorption of drug is over 95% []
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [2]
Bioavailability
90% of drug becomes completely available to its intended biological destination(s) [3]
Clearance
The clearance of drug is 109 mL/min in healthy subjects []
Elimination
2% of drug is excreted from urine in the unchanged form [2]
Half-life
The concentration or amount of drug in body reduced by one-half in 7 - 9 hours [4]
Metabolism
The drug is metabolized via the 3A isoform subfamily of hepatic cytochrome P450 []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 2.84911 micromolar/kg/day [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.04% [4]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 1.1 L/kg [4]
Water Solubility
The ability of drug to dissolve in water is measured as 0.03 mg/mL [2]
Chemical Identifiers
Formula
C20H25NO2S2
IUPAC Name
(3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl]piperidine-3-carboxylic acid
Canonical SMILES
CC1=C(SC=C1)C(=CCCN2CCC[C@H](C2)C(=O)O)C3=C(C=CS3)C
InChI
InChI=1S/C20H25NO2S2/c1-14-7-11-24-18(14)17(19-15(2)8-12-25-19)6-4-10-21-9-3-5-16(13-21)20(22)23/h6-8,11-12,16H,3-5,9-10,13H2,1-2H3,(H,22,23)/t16-/m1/s1
InChIKey
PBJUNZJWGZTSKL-MRXNPFEDSA-N
Cross-matching ID
PubChem CID
60648
ChEBI ID
CHEBI:9586
CAS Number
115103-54-3
DrugBank ID
DB00906
TTD ID
D0ED7U
VARIDT ID
DR01016
INTEDE ID
DR1588
ACDINA ID
D00673
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
GABA transporter GAT-1 (SLC6A1) TTPRKM0 SC6A1_HUMAN Inhibitor [6]
Gamma-aminobutyric acid uptake (GABAU) TTV9MQG NOUNIPROTAC Inhibitor [7]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [8]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [9]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Aromatase (CYP19A1) OTZ6XF74 CP19A_HUMAN Gene/Protein Processing [10]
Sodium- and chloride-dependent GABA transporter 1 (SLC6A1) OTLCJJF3 SC6A1_HUMAN Gene/Protein Processing [11]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Epilepsy
ICD Disease Classification 8A60-8A68
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
GABA transporter GAT-1 (SLC6A1) DTT SLC6A1 4.99E-02 -0.24 -0.62
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 6.60E-01 2.51E-02 8.26E-02
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 8.62E-03 1.37E-01 8.67E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 2.51E-01 8.39E-02 5.00E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.93E-04 -6.16E-01 -2.64E+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 Tiagabine
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Cenobamate DM8KLU9 Moderate Increased metabolism of Tiagabine caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [12]
Stiripentol DMMSDOY Moderate Decreased metabolism of Tiagabine caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [13]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Tiagabine caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [14]
Rufinamide DMWE60C Moderate Increased metabolism of Tiagabine caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [15]
Phenobarbital DMXZOCG Moderate Increased metabolism of Tiagabine caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [14]
Coadministration of a Drug Treating the Disease Different from Tiagabine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Dronedarone DMA8FS5 Moderate Decreased metabolism of Tiagabine caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [16]
Posaconazole DMUL5EW Moderate Decreased metabolism of Tiagabine caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [15]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Tiagabine caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [17]
Telithromycin DMZ4P3A Moderate Decreased metabolism of Tiagabine caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [18]
Lapatinib DM3BH1Y Moderate Decreased metabolism of Tiagabine caused by Lapatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [19]
Tucatinib DMBESUA Moderate Decreased metabolism of Tiagabine caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [20]
Levomilnacipran DMV26S8 Moderate Antagonize the effect of Tiagabine when combined with Levomilnacipran. Chronic pain [MG30] [21]
MK-8228 DMOB58Q Moderate Decreased metabolism of Tiagabine caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [22]
Sertraline DM0FB1J Moderate Antagonize the effect of Tiagabine when combined with Sertraline. Depression [6A70-6A7Z] [21]
Vilazodone DM4LECQ Moderate Antagonize the effect of Tiagabine when combined with Vilazodone. Depression [6A70-6A7Z] [21]
Vortioxetine DM6F1PU Moderate Antagonize the effect of Tiagabine when combined with Vortioxetine. Depression [6A70-6A7Z] [21]
Milnacipran DMBFE74 Moderate Antagonize the effect of Tiagabine when combined with Milnacipran. Depression [6A70-6A7Z] [21]
Escitalopram DMFK9HG Moderate Antagonize the effect of Tiagabine when combined with Escitalopram. Depression [6A70-6A7Z] [21]
Desvenlafaxine DMHD4PE Moderate Antagonize the effect of Tiagabine when combined with Desvenlafaxine. Depression [6A70-6A7Z] [21]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Tiagabine and Esketamine. Depression [6A70-6A7Z] [23]
Tazemetostat DMWP1BH Moderate Increased metabolism of Tiagabine caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [24]
Itraconazole DMCR1MV Moderate Decreased metabolism of Tiagabine caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [25]
Boceprevir DMBSHMF Moderate Decreased metabolism of Tiagabine caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [26]
Telaprevir DMMRV29 Moderate Decreased metabolism of Tiagabine caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [27]
Rifapentine DMCHV4I Moderate Increased metabolism of Tiagabine caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [28]
Fosamprenavir DM4W9B3 Moderate Decreased metabolism of Tiagabine caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [29]
Saquinavir DMG814N Moderate Decreased metabolism of Tiagabine caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [30]
Etravirine DMGV8QU Moderate Increased metabolism of Tiagabine caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [31]
Darunavir DMN3GCH Moderate Decreased metabolism of Tiagabine caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [32]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Tiagabine caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [33]
Brigatinib DM7W94S Moderate Increased metabolism of Tiagabine caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [34]
Ceritinib DMB920Z Moderate Decreased metabolism of Tiagabine caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [15]
PF-06463922 DMKM7EW Moderate Increased metabolism of Tiagabine caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [35]
Selpercatinib DMZR15V Moderate Decreased metabolism of Tiagabine caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [15]
Hydroxychloroquine DMSIVND Moderate Antagonize the effect of Tiagabine when combined with Hydroxychloroquine. Malaria [1F40-1F45] [23]
Idelalisib DM602WT Moderate Decreased metabolism of Tiagabine caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [36]
IPI-145 DMWA24P Moderate Decreased metabolism of Tiagabine caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [37]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Tiagabine caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [15]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Tiagabine and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [38]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Tiagabine and Lasmiditan. Migraine [8A80] [39]
Exjade DMHPRWG Moderate Decreased metabolism of Tiagabine caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [40]
Flibanserin DM70DTN Moderate Additive CNS depression effects by the combination of Tiagabine and Flibanserin. Mood disorder [6A60-6E23] [41]
Thalidomide DM70BU5 Moderate Additive CNS depression effects by the combination of Tiagabine and Thalidomide. Multiple myeloma [2A83] [42]
Nilotinib DM7HXWT Moderate Decreased metabolism of Tiagabine caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [43]
Dasatinib DMJV2EK Moderate Decreased metabolism of Tiagabine caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [44]
Apraclonidine DMO4PVE Moderate Additive CNS depression effects by the combination of Tiagabine and Apraclonidine. Optic nerve disorder [9C40] [45]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Tiagabine caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [46]
Buprenorphine DMPRI8G Major Additive CNS depression effects by the combination of Tiagabine and Buprenorphine. Pain [MG30-MG3Z] [47]
Abametapir DM2RX0I Moderate Decreased metabolism of Tiagabine caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [48]
Lefamulin DME6G97 Moderate Decreased metabolism of Tiagabine caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [49]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Tiagabine caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [50]
Enzalutamide DMGL19D Moderate Increased metabolism of Tiagabine caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [51]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Tiagabine and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [52]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Tiagabine caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [53]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Tiagabine caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [15]
Larotrectinib DM26CQR Moderate Decreased metabolism of Tiagabine caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [23]
Armodafinil DMGB035 Minor Increased metabolism of Tiagabine caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [54]
LEE011 DMMX75K Moderate Decreased metabolism of Tiagabine caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [55]
Pitolisant DM8RFNJ Moderate Increased metabolism of Tiagabine caused by Pitolisant mediated induction of CYP450 enzyme. Somnolence [MG42] [15]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Tiagabine caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [56]
⏷ Show the Full List of 55 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
FD&C blue no. 2 E00446 2723854 Colorant
Quinoline yellow WS E00309 24671 Colorant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Sunset yellow FCF E00255 17730 Colorant
Ascorbic acid E00579 54670067 Acidulant; Antioxidant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Butylhydroxyanisole E00308 24667 Antimicrobial preservative; Antioxidant
Crospovidone E00626 Not Available Disintegrant
Hydroxypropyl cellulose E00632 Not Available Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; 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
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
Pregelatinized starch E00674 Not Available Binding agent; Diluent; Disintegrant
⏷ Show the Full List of 20 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Tiagabine 12 mg tablet 12 mg Oral Tablet Oral
Tiagabine 16 mg tablet 16 mg Oral Tablet Oral
Tiagabine 2 mg tablet 2 mg Oral Tablet Oral
Tiagabine 4 mg tablet 4 mg Oral Tablet Oral
Tiagabine Hydrochloride 2mg tablet 2mg Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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