Details of the Drug

General Information of Drug (ID: DMS3GX2)

Drug Name

Telmisartan

Synonyms

Kinzal; Kinzalmono; Micardis; Pritor; Abbott brand of telmisartan; Boehringer Ingelheim brand of telmisartan; Glaxo Wellcome brand of telmisartan; GlaxoSmithKline brand of telmisartan; BIBR 277; BIBR 277SE; BIBR-277; BIBR-277SE; Bay 68-9291; Micardis (TN); Telmisartan [USAN:INN]; YM-086; BIBR-277-SE; Telmisartan (JAN/USAN/INN); Micardis, Targit, Temax, BIBR277, Telmisartan; 2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid; 4'-((1,4'-dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-(1,1'-biphenyl)-2-carboxylic acid; 4'-((4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic acid; 4'-((4-mehtyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimmidazolyl)methyl)-2-biphenylcarboxylic acid; 4'-[(1,4'-dimethyl-2'propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid; 4'-[(1,7'-dimethyl-2'-propyl-1H,3'H-2,5'-bibenzimidazol-3'-yl)methyl][1,1'-biphenyl]-2-carboxylic acid; 4'-[(1,7'-dimethyl-2'-propyl-1H,3'H-2,5'-bibenzimidazol-3'-yl)methyl]biphenyl-2-carboxylic acid

Indication

Disease Entry	ICD 11	Status	REF
Hypertension	BA00-BA04	Approved	[1], [2]

Therapeutic Class

Antihypertensive Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 2

Molecular Weight (mw)

514.6

Topological Polar Surface Area (xlogp)

6.9

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Clearance: The drug present in the plasma can be removed from the body at the rate of 8.4 mL/min/kg [4]
Elimination: 0.5% 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 20 hours [4]
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 2.2207 micromolar/kg/day [5]
Unbound Fraction: The unbound fraction of drug in plasma is 0.004% [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 5.3 L/kg [4]

Chemical Identifiers

Formula: C33H30N4O2
IUPAC Name: 2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid
Canonical SMILES: CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C
InChI: InChI=1S/C33H30N4O2/c1-4-9-30-35-31-21(2)18-24(32-34-27-12-7-8-13-28(27)36(32)3)19-29(31)37(30)20-22-14-16-23(17-15-22)25-10-5-6-11-26(25)33(38)39/h5-8,10-19H,4,9,20H2,1-3H3,(H,38,39)
InChIKey: RMMXLENWKUUMAY-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 65999
ChEBI ID: CHEBI:9434
CAS Number: 144701-48-4
DrugBank ID: DB00966
TTD ID: D0N6RF
VARIDT ID: DR00248
INTEDE ID: DR1545
ACDINA ID: D00657

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiotensin II receptor type-1 (AGTR1)	TT8DBY3	AGTR1_HUMAN	Antagonist	[6]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Organic anion transporting polypeptide 2B1 (SLCO2B1)	DTPFTEQ	SO2B1_HUMAN	Substrate	[7]
Organic anion transporting polypeptide 1A2 (SLCO1A2)	DTE2B1D	SO1A2_HUMAN	Substrate	[8]
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DT9C1TS	SO1B3_HUMAN	Substrate	[8]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Substrate	[9]
UDP-glucuronosyltransferase 1A3 (UGT1A3)	DEF2WXN	UD13_HUMAN	Substrate	[10]

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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

Hypertension

ICD Disease Classification

BA00-BA04

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Angiotensin II receptor type-1 (AGTR1)	DTT	AGTR1	8.95E-01	1.34E-02	0.07
Organic anion transporting polypeptide 2B1 (SLCO2B1)	DTP	OATP2B1	6.30E-05	2.52E-01	5.88E-01
Organic anion transporting polypeptide 1A2 (SLCO1A2)	DTP	OATP1A2	1.16E-03	4.00E-01	4.43E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	9.69E-01	1.16E-03	3.56E-03
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	1.10E-01	-5.91E-02	-3.60E-01

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 Telmisartan

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Aliskiren	DM1BV7W	Major	Increased risk of hyperkalemia by the combination of Telmisartan and Aliskiren.	Hypertension [BA00-BA04]	[65]
Captopril	DM458UM	Major	Increased risk of hyperkalemia by the combination of Telmisartan and Captopril.	Hypertension [BA00-BA04]	[66]
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Coadministration of a Drug Treating the Disease Different from Telmisartan (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Insulin-glulisine	DMQI0FU	Moderate	Increased risk of hypoglycemia by the combination of Telmisartan and Insulin-glulisine.	Acute diabete complication [5A2Y]	[67]
Insulin-aspart	DMX7V28	Moderate	Increased risk of hypoglycemia by the combination of Telmisartan and Insulin-aspart.	Acute diabete complication [5A2Y]	[68]
Cariprazine	DMJYDVK	Moderate	Additive hypotensive effects by the combination of Telmisartan and Cariprazine.	Bipolar disorder [6A60]	[69]
Drospirenone	DM1A9W3	Moderate	Increased risk of hyperkalemia by the combination of Telmisartan and Drospirenone.	Contraceptive management [QA21]	[70]
Ardeparin	DMYRX8B	Moderate	Increased risk of hyperkalemia by the combination of Telmisartan and Ardeparin.	Coronary thrombosis [BA43]	[66]
Mycophenolic acid	DMU65NK	Moderate	Increased metabolism of Telmisartan caused by Mycophenolic acid mediated induction of UGT.	Crohn disease [DD70]	[71]
Selegiline	DM6034S	Moderate	Additive hypotensive effects by the combination of Telmisartan and Selegiline.	Depression [6A70-6A7Z]	[72]
Isocarboxazid	DMAF1NB	Moderate	Additive hypotensive effects by the combination of Telmisartan and Isocarboxazid.	Depression [6A70-6A7Z]	[72]
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of Telmisartan and OPC-34712.	Depression [6A70-6A7Z]	[69]
Procarbazine	DMIK367	Moderate	Additive hypotensive effects by the combination of Telmisartan and Procarbazine.	Hodgkin lymphoma [2B30]	[72]
Tolvaptan	DMIWFRL	Moderate	Increased risk of hyperkalemia by the combination of Telmisartan and Tolvaptan.	Hypo-osmolality/hyponatraemia [5C72]	[73]
ITI-007	DMUQ1DO	Moderate	Additive hypotensive effects by the combination of Telmisartan and ITI-007.	Insomnia [7A00-7A0Z]	[69]
Ozanimod	DMT6AM2	Moderate	Additive hypotensive effects by the combination of Telmisartan and Ozanimod.	Multiple sclerosis [8A40]	[72]
Promethazine	DM6I5GR	Moderate	Additive hypotensive effects by the combination of Telmisartan and Promethazine.	Nausea/vomiting [MD90]	[69]
Safinamide	DM0YWJC	Moderate	Additive hypotensive effects by the combination of Telmisartan and Safinamide.	Parkinsonism [8A00]	[72]
Rasagiline	DM3WKQ4	Moderate	Additive hypotensive effects by the combination of Telmisartan and Rasagiline.	Parkinsonism [8A00]	[72]
Levomepromazine	DMIKFEL	Moderate	Additive hypotensive effects by the combination of Telmisartan and Levomepromazine.	Psychotic disorder [6A20-6A25]	[69]
Quetiapine	DM1N62C	Moderate	Additive hypotensive effects by the combination of Telmisartan and Quetiapine.	Schizophrenia [6A20]	[69]
Aripiprazole	DM3NUMH	Moderate	Additive hypotensive effects by the combination of Telmisartan and Aripiprazole.	Schizophrenia [6A20]	[69]
Iloperidone	DM6AUFY	Moderate	Additive hypotensive effects by the combination of Telmisartan and Iloperidone.	Schizophrenia [6A20]	[69]
Paliperidone	DM7NPJS	Moderate	Additive hypotensive effects by the combination of Telmisartan and Paliperidone.	Schizophrenia [6A20]	[69]
Molindone	DMAH70G	Moderate	Additive hypotensive effects by the combination of Telmisartan and Molindone.	Schizophrenia [6A20]	[69]
Thiothixene	DMDINC4	Moderate	Additive hypotensive effects by the combination of Telmisartan and Thiothixene.	Schizophrenia [6A20]	[69]
Amisulpride	DMSJVAM	Moderate	Additive hypotensive effects by the combination of Telmisartan and Amisulpride.	Schizophrenia [6A20]	[69]
Asenapine	DMSQZE2	Moderate	Additive hypotensive effects by the combination of Telmisartan and Asenapine.	Schizophrenia [6A20]	[69]
Insulin-detemir	DMOA4VW	Moderate	Increased risk of hypoglycemia by the combination of Telmisartan and Insulin-detemir.	Type-1/2 diabete [5A10-5A11]	[67]
Insulin degludec	DMPL395	Moderate	Increased risk of hypoglycemia by the combination of Telmisartan and Insulin degludec.	Type-1/2 diabete [5A10-5A11]	[67]
Trimeprazine	DMEMV9D	Moderate	Additive hypotensive effects by the combination of Telmisartan and Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[74]
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⏷ Show the Full List of 28 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
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Meglumine	E00181	8567	Buffering agent
Sodium stearyl fumarate	E00545	23665634	lubricant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Crospovidone	E00626	Not Available	Disintegrant
Eisenoxyd	E00585	56841934	Colorant
Hexahydric alcohol	E00083	5780	Diluent; Flavoring agent; Humectant; Plasticizing agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	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
Sodium hydroxide	E00234	14798	Alkalizing agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
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⏷ Show the Full List of 13 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Telmisartan 20 mg tablet	20 mg	Oral Tablet	Oral
Telmisartan 40 mg tablet	40 mg	Oral Tablet	Oral
Telmisartan 80 mg tablet	80 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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