Details of the Drug

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], [2]
Anxiety disorder	6B00-6B0Z	Phase 2	[1], [2]

Therapeutic Class

Anticonvulsants

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

375.6

Topological Polar Surface Area (xlogp)

2.7

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption: The absorption of drug is over 95% [3]
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [4]
Bioavailability: 90% of drug becomes completely available to its intended biological destination(s) [5]
Clearance: The clearance of drug is 109 mL/min in healthy subjects [6]
Elimination: 2% of drug is excreted from urine in the unchanged form [4]
Half-life: The concentration or amount of drug in body reduced by one-half in 7 - 9 hours [7]
Metabolism: The drug is metabolized via the 3A isoform subfamily of hepatic cytochrome P450 [3]
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 2.84911 micromolar/kg/day [8]
Unbound Fraction: The unbound fraction of drug in plasma is 0.04% [7]
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 [7]
Water Solubility: The ability of drug to dissolve in water is measured as 0.03 mg/mL [4]

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

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	[9]
Gamma-aminobutyric acid uptake (GABAU)	TTV9MQG	NOUNIPROTAC	Inhibitor	[10]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)_{Main DME}	DE4LYSA	CP3A4_HUMAN	Substrate	[11]
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Substrate	[12]

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Molecular Interaction Atlas (MIA)

MIA Detail

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)

MEA Detail

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	DMGOVHA	Moderate	Increased metabolism of Tiagabine caused by Cenobamate mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[44]
Stiripentol	DMMSDOY	Moderate	Decreased metabolism of Tiagabine caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[45]
Fosphenytoin	DMOX3LB	Moderate	Increased metabolism of Tiagabine caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[46]
Rufinamide	DMWE60C	Moderate	Increased metabolism of Tiagabine caused by Rufinamide mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[47]
Phenobarbital	DMXZOCG	Moderate	Increased metabolism of Tiagabine caused by Phenobarbital mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[46]
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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]	[48]
Posaconazole	DMUL5EW	Moderate	Decreased metabolism of Tiagabine caused by Posaconazole mediated inhibition of CYP450 enzyme.	Aspergillosis [1F20]	[47]
Dalfopristin	DM4LTKV	Moderate	Decreased metabolism of Tiagabine caused by Dalfopristin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[49]
Telithromycin	DMZ4P3A	Moderate	Decreased metabolism of Tiagabine caused by Telithromycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[50]
Lapatinib	DM3BH1Y	Moderate	Decreased metabolism of Tiagabine caused by Lapatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[51]
Tucatinib	DMBESUA	Moderate	Decreased metabolism of Tiagabine caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[52]
Levomilnacipran	DMV26S8	Moderate	Antagonize the effect of Tiagabine when combined with Levomilnacipran.	Chronic pain [MG30]	[53]
MK-8228	DMOB58Q	Moderate	Decreased metabolism of Tiagabine caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[54]
Sertraline	DM0FB1J	Moderate	Antagonize the effect of Tiagabine when combined with Sertraline.	Depression [6A70-6A7Z]	[53]
Vilazodone	DM4LECQ	Moderate	Antagonize the effect of Tiagabine when combined with Vilazodone.	Depression [6A70-6A7Z]	[53]
Vortioxetine	DM6F1PU	Moderate	Antagonize the effect of Tiagabine when combined with Vortioxetine.	Depression [6A70-6A7Z]	[53]
Milnacipran	DMBFE74	Moderate	Antagonize the effect of Tiagabine when combined with Milnacipran.	Depression [6A70-6A7Z]	[53]
Escitalopram	DMFK9HG	Moderate	Antagonize the effect of Tiagabine when combined with Escitalopram.	Depression [6A70-6A7Z]	[53]
Desvenlafaxine	DMHD4PE	Moderate	Antagonize the effect of Tiagabine when combined with Desvenlafaxine.	Depression [6A70-6A7Z]	[53]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Tiagabine and Esketamine.	Depression [6A70-6A7Z]	[55]
Tazemetostat	DMWP1BH	Moderate	Increased metabolism of Tiagabine caused by Tazemetostat mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[56]
Itraconazole	DMCR1MV	Moderate	Decreased metabolism of Tiagabine caused by Itraconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[57]
Boceprevir	DMBSHMF	Moderate	Decreased metabolism of Tiagabine caused by Boceprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[58]
Telaprevir	DMMRV29	Moderate	Decreased metabolism of Tiagabine caused by Telaprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[59]
Rifapentine	DMCHV4I	Moderate	Increased metabolism of Tiagabine caused by Rifapentine mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[60]
Fosamprenavir	DM4W9B3	Moderate	Decreased metabolism of Tiagabine caused by Fosamprenavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[61]
Saquinavir	DMG814N	Moderate	Decreased metabolism of Tiagabine caused by Saquinavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[62]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Tiagabine caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[63]
Darunavir	DMN3GCH	Moderate	Decreased metabolism of Tiagabine caused by Darunavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[64]
Berotralstat	DMWA2DZ	Moderate	Decreased metabolism of Tiagabine caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[65]
Brigatinib	DM7W94S	Moderate	Increased metabolism of Tiagabine caused by Brigatinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[66]
Ceritinib	DMB920Z	Moderate	Decreased metabolism of Tiagabine caused by Ceritinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[47]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Tiagabine caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[67]
Selpercatinib	DMZR15V	Moderate	Decreased metabolism of Tiagabine caused by Selpercatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[47]
Hydroxychloroquine	DMSIVND	Moderate	Antagonize the effect of Tiagabine when combined with Hydroxychloroquine.	Malaria [1F40-1F45]	[55]
Idelalisib	DM602WT	Moderate	Decreased metabolism of Tiagabine caused by Idelalisib mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[68]
IPI-145	DMWA24P	Moderate	Decreased metabolism of Tiagabine caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[69]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Tiagabine caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[47]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Tiagabine and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[70]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Tiagabine and Lasmiditan.	Migraine [8A80]	[71]
Exjade	DMHPRWG	Moderate	Decreased metabolism of Tiagabine caused by Exjade mediated inhibition of CYP450 enzyme.	Mineral absorption/transport disorder [5C64]	[72]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Tiagabine and Flibanserin.	Mood disorder [6A60-6E23]	[73]
Thalidomide	DM70BU5	Moderate	Additive CNS depression effects by the combination of Tiagabine and Thalidomide.	Multiple myeloma [2A83]	[74]
Nilotinib	DM7HXWT	Moderate	Decreased metabolism of Tiagabine caused by Nilotinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[75]
Dasatinib	DMJV2EK	Moderate	Decreased metabolism of Tiagabine caused by Dasatinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[76]
Apraclonidine	DMO4PVE	Moderate	Additive CNS depression effects by the combination of Tiagabine and Apraclonidine.	Optic nerve disorder [9C40]	[77]
Rucaparib	DM9PVX8	Moderate	Decreased metabolism of Tiagabine caused by Rucaparib mediated inhibition of CYP450 enzyme.	Ovarian cancer [2C73]	[78]
Buprenorphine	DMPRI8G	Major	Additive CNS depression effects by the combination of Tiagabine and Buprenorphine.	Pain [MG30-MG3Z]	[79]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Tiagabine caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[80]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Tiagabine caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[81]
Lonafarnib	DMGM2Z6	Moderate	Decreased metabolism of Tiagabine caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[82]
Enzalutamide	DMGL19D	Moderate	Increased metabolism of Tiagabine caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[83]
Temsirolimus	DMS104F	Moderate	Increased plasma concentrations of Tiagabine and Temsirolimus due to competitive inhibition of the same metabolic pathway.	Renal cell carcinoma [2C90]	[84]
Voxelotor	DMCS6M5	Moderate	Decreased metabolism of Tiagabine caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[85]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Tiagabine caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[47]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Tiagabine caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[55]
Armodafinil	DMGB035	Minor	Increased metabolism of Tiagabine caused by Armodafinil mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[86]
LEE011	DMMX75K	Moderate	Decreased metabolism of Tiagabine caused by LEE011 mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[87]
Pitolisant	DM8RFNJ	Moderate	Increased metabolism of Tiagabine caused by Pitolisant mediated induction of CYP450 enzyme.	Somnolence [MG42]	[47]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Tiagabine caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[88]
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⏷ 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
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⏷ 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

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