Details of the Drug

General Information of Drug (ID: DMREUQ6)

Drug Name

Valsartan

Synonyms

valsartan; 137862-53-4; Diovan; Tareg; Provas; L-Valsartan; CGP 48933; Exforge; CGP-48933; (S)-2-(N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid; UNII-80M03YXJ7I; N-(p-(o-1H-Tetrazol-5-ylphenyl)benzyl)-N-valeryl-L-valine; CHEMBL1069; 80M03YXJ7I; CHEBI:9927; C24H29N5O3; (2S)-3-methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid; N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-L-valine; 137863-60-6; AK-58790; Kalpress; Miten; Nisis; Diovan; Vals; Valsarran; Walsartan; Aventis brand of valsartan; CEPA brand of valsartan; Esteve brand of valsartan; Lacer brand of valsartan; Novartis brand of valsartan; Sanol brand of valsartan; Schwarz brand of valsartan; Diovan (TN); Diovan, Valsartan; Valsartan [USAN:INN]; Valtan (TN); Valzaar (TN); Valsartan (JAN/USAN/INN); N-valeryl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)valine; N-pentanoyl-N-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-L-valine; N-pentanoyl-N-{[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-L-valine; L-Valine, N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-(9CI); (S)-N-valeryl-N-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]-methyl}-valine; (s)-2-(n-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)pentanamido)-3-methylbutanoic acid; [3H]valsartan

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): 0

Molecular Weight (mw)

435.5

Topological Polar Surface Area (xlogp)

4.4

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 4: low solubility and low permeability [3]
Clearance: The drug present in the plasma can be removed from the body at the rate of 0.49 mL/min/kg [4]
Elimination: 13% 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 9.5 hours [4]
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 10.5 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 0.22 L/kg [4]
Water Solubility: The ability of drug to dissolve in water is measured as 0.18 mg/mL [3]

Chemical Identifiers

Formula: C24H29N5O3
IUPAC Name: (2S)-3-methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid
Canonical SMILES: CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)[C@@H](C(C)C)C(=O)O
InChI: InChI=1S/C24H29N5O3/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H,31,32)(H,25,26,27,28)/t22-/m0/s1
InChIKey: ACWBQPMHZXGDFX-QFIPXVFZSA-N

Cross-matching ID

PubChem CID: 60846
ChEBI ID: CHEBI:9927
CAS Number: 137862-53-4
DrugBank ID: DB00177
TTD ID: D06UDG
VARIDT ID: DR00071
INTEDE ID: DR1668
ACDINA ID: D00718

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], [7], [8]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Peptide transporter 1 (SLC15A1)	DT9G7XN	S15A1_HUMAN	Substrate	[9]
Multidrug resistance-associated protein 2 (ABCC2)	DTFI42L	MRP2_HUMAN	Substrate	[10]
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DT3D8F0	SO1B1_HUMAN	Substrate	[11]
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DT9C1TS	SO1B3_HUMAN	Substrate	[10]
Organic anion transporter 3 (SLC22A8)	DTVP67E	S22A8_HUMAN	Substrate	[12]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 2C9 (CYP2C9)_{Main DME}	DE5IED8	CP2C9_HUMAN	Substrate	[13]

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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 transporter 3 (SLC22A8)	DTP	OAT3	5.19E-01	-8.88E-03	-2.08E-02
Multidrug resistance-associated protein 2 (ABCC2)	DTP	MRP2	7.16E-01	-1.28E-02	-6.06E-02
Peptide transporter 1 (SLC15A1)	DTP	PEPT1	4.57E-01	2.15E-02	1.72E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	9.69E-01	1.16E-03	3.56E-03
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	8.15E-01	6.20E-03	5.61E-02
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	1.90E-01	-9.81E-03	-5.96E-02

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 Valsartan

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Aliskiren	DM1BV7W	Major	Increased risk of hyperkalemia by the combination of Valsartan and Aliskiren.	Hypertension [BA00-BA04]	[69]
Moexipril	DM26E4B	Major	Increased risk of hyperkalemia by the combination of Valsartan and Moexipril.	Hypertension [BA00-BA04]	[70]
Captopril	DM458UM	Major	Increased risk of hyperkalemia by the combination of Valsartan and Captopril.	Hypertension [BA00-BA04]	[70]
Trandolapril	DM4L6EU	Major	Increased risk of hyperkalemia by the combination of Valsartan and Trandolapril.	Hypertension [BA00-BA04]	[70]
Fosinopril	DM9NJ52	Major	Increased risk of hyperkalemia by the combination of Valsartan and Fosinopril.	Hypertension [BA00-BA04]	[70]
Benazepril	DMH1M9B	Major	Increased risk of hyperkalemia by the combination of Valsartan and Benazepril.	Hypertension [BA00-BA04]	[70]
Enalapril	DMNFUZR	Major	Increased risk of hyperkalemia by the combination of Valsartan and Enalapril.	Hypertension [BA00-BA04]	[70]
Perindopril	DMOPZDT	Major	Increased risk of hyperkalemia by the combination of Valsartan and Perindopril.	Hypertension [BA00-BA04]	[70]
Quinapril	DMR8H31	Major	Increased risk of hyperkalemia by the combination of Valsartan and Quinapril.	Hypertension [BA00-BA04]	[71]
Lisinopril	DMUOK4C	Major	Increased risk of hyperkalemia by the combination of Valsartan and Lisinopril.	Hypertension [BA00-BA04]	[70]
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⏷ Show the Full List of 10 DDI Information of This Drug

Coadministration of a Drug Treating the Disease Different from Valsartan (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Insulin-glulisine	DMQI0FU	Moderate	Increased risk of hypoglycemia by the combination of Valsartan and Insulin-glulisine.	Acute diabete complication [5A2Y]	[72]
Insulin-aspart	DMX7V28	Moderate	Increased risk of hypoglycemia by the combination of Valsartan and Insulin-aspart.	Acute diabete complication [5A2Y]	[73]
Arn-509	DMT81LZ	Moderate	Accelerated clearance of Valsartan due to the transporter induction by Arn-509.	Acute myeloid leukaemia [2A60]	[74]
Promazine	DMZAL7W	Moderate	Additive hypotensive effects by the combination of Valsartan and Promazine.	Appearance/behaviour symptom [MB23]	[75]
Linezolid	DMGFPU2	Moderate	Additive hypotensive effects by the combination of Valsartan and Linezolid.	Bacterial infection [1A00-1C4Z]	[76]
Ag-221	DMS0ZBI	Moderate	Decreased clearance of Valsartan due to the transporter inhibition by Ag-221.	BCR-ABL1-negative chronic myeloid leukaemia [2A41]	[77]
Cariprazine	DMJYDVK	Moderate	Additive hypotensive effects by the combination of Valsartan and Cariprazine.	Bipolar disorder [6A60]	[75]
Olopatadine	DMKMWQG	Moderate	Additive CNS depression effects by the combination of Valsartan and Olopatadine.	Conjunctiva disorder [9A60]	[78]
Drospirenone	DM1A9W3	Moderate	Increased risk of hyperkalemia by the combination of Valsartan and Drospirenone.	Contraceptive management [QA21]	[79]
Ardeparin	DMYRX8B	Moderate	Increased risk of hyperkalemia by the combination of Valsartan and Ardeparin.	Coronary thrombosis [BA43]	[70]
Selegiline	DM6034S	Moderate	Additive hypotensive effects by the combination of Valsartan and Selegiline.	Depression [6A70-6A7Z]	[76]
Isocarboxazid	DMAF1NB	Moderate	Additive hypotensive effects by the combination of Valsartan and Isocarboxazid.	Depression [6A70-6A7Z]	[76]
Tranylcypromine	DMGB5RE	Moderate	Additive hypotensive effects by the combination of Valsartan and Tranylcypromine.	Depression [6A70-6A7Z]	[76]
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of Valsartan and OPC-34712.	Depression [6A70-6A7Z]	[75]
Phenelzine	DMHIDUE	Moderate	Additive hypotensive effects by the combination of Valsartan and Phenelzine.	Depression [6A70-6A7Z]	[76]
Spironolactone	DM2AQ5N	Major	Increased risk of hyperkalemia by the combination of Valsartan and Spironolactone.	Heart failure [BD10-BD1Z]	[80]
Triamterene	DM2HU9I	Major	Increased risk of hyperkalemia by the combination of Valsartan and Triamterene.	Heart failure [BD10-BD1Z]	[80]
Ramipril	DM2R68E	Major	Increased risk of hyperkalemia by the combination of Valsartan and Ramipril.	Heart failure [BD10-BD1Z]	[71]
Eplerenone	DMF0NQR	Moderate	Increased risk of hyperkalemia by the combination of Valsartan and Eplerenone.	Heart failure [BD10-BD1Z]	[81]
Amiloride	DMRTSGP	Major	Increased risk of hyperkalemia by the combination of Valsartan and Amiloride.	Heart failure [BD10-BD1Z]	[80]
Procarbazine	DMIK367	Moderate	Additive hypotensive effects by the combination of Valsartan and Procarbazine.	Hodgkin lymphoma [2B30]	[76]
Potassium chloride	DMMTAJC	Major	Increased risk of hyperkalemia by the combination of Valsartan and Potassium chloride.	Hypo-kalaemia [5C77]	[82]
Tolvaptan	DMIWFRL	Moderate	Increased risk of hyperkalemia by the combination of Valsartan and Tolvaptan.	Hypo-osmolality/hyponatraemia [5C72]	[83]
Propiomazine	DMKY8V1	Moderate	Additive hypotensive effects by the combination of Valsartan and Propiomazine.	Insomnia [7A00-7A0Z]	[75]
ITI-007	DMUQ1DO	Moderate	Additive hypotensive effects by the combination of Valsartan and ITI-007.	Insomnia [7A00-7A0Z]	[75]
Porfimer Sodium	DM7ZWNY	Moderate	Increased risk of photosensitivity reactions by the combination of Valsartan and Porfimer Sodium.	Lung cancer [2C25]	[84]
Ozanimod	DMT6AM2	Moderate	Additive hypotensive effects by the combination of Valsartan and Ozanimod.	Multiple sclerosis [8A40]	[76]
Prochlorperazine	DM53SRA	Moderate	Additive hypotensive effects by the combination of Valsartan and Prochlorperazine.	Nausea/vomiting [MD90]	[75]
Promethazine	DM6I5GR	Moderate	Additive hypotensive effects by the combination of Valsartan and Promethazine.	Nausea/vomiting [MD90]	[75]
Thiethylperazine	DMU3IET	Moderate	Additive hypotensive effects by the combination of Valsartan and Thiethylperazine.	Nausea/vomiting [MD90]	[75]
Olaparib	DM8QB1D	Moderate	Decreased clearance of Valsartan due to the transporter inhibition by Olaparib.	Ovarian cancer [2C73]	[77]
Safinamide	DM0YWJC	Moderate	Additive hypotensive effects by the combination of Valsartan and Safinamide.	Parkinsonism [8A00]	[76]
Rasagiline	DM3WKQ4	Moderate	Additive hypotensive effects by the combination of Valsartan and Rasagiline.	Parkinsonism [8A00]	[76]
Levomepromazine	DMIKFEL	Moderate	Additive hypotensive effects by the combination of Valsartan and Levomepromazine.	Psychotic disorder [6A20-6A25]	[75]
Fluphenazine	DMIT8LX	Moderate	Additive hypotensive effects by the combination of Valsartan and Fluphenazine.	Psychotic disorder [6A20-6A25]	[75]
Triflupromazine	DMKFQJP	Moderate	Additive hypotensive effects by the combination of Valsartan and Triflupromazine.	Psychotic disorder [6A20-6A25]	[75]
Quetiapine	DM1N62C	Moderate	Additive hypotensive effects by the combination of Valsartan and Quetiapine.	Schizophrenia [6A20]	[75]
Mesoridazine	DM2ZGAN	Moderate	Additive hypotensive effects by the combination of Valsartan and Mesoridazine.	Schizophrenia [6A20]	[75]
Thioridazine	DM35M8J	Moderate	Additive hypotensive effects by the combination of Valsartan and Thioridazine.	Schizophrenia [6A20]	[75]
Aripiprazole	DM3NUMH	Moderate	Additive hypotensive effects by the combination of Valsartan and Aripiprazole.	Schizophrenia [6A20]	[75]
Iloperidone	DM6AUFY	Moderate	Additive hypotensive effects by the combination of Valsartan and Iloperidone.	Schizophrenia [6A20]	[75]
Paliperidone	DM7NPJS	Moderate	Additive hypotensive effects by the combination of Valsartan and Paliperidone.	Schizophrenia [6A20]	[75]
Loxapine	DM8AI9U	Moderate	Additive hypotensive effects by the combination of Valsartan and Loxapine.	Schizophrenia [6A20]	[75]
Haloperidol	DM96SE0	Moderate	Additive hypotensive effects by the combination of Valsartan and Haloperidol.	Schizophrenia [6A20]	[75]
Perphenazine	DMA4MRX	Moderate	Additive hypotensive effects by the combination of Valsartan and Perphenazine.	Schizophrenia [6A20]	[75]
Molindone	DMAH70G	Moderate	Additive hypotensive effects by the combination of Valsartan and Molindone.	Schizophrenia [6A20]	[75]
Chlorpromazine	DMBGZI3	Moderate	Additive hypotensive effects by the combination of Valsartan and Chlorpromazine.	Schizophrenia [6A20]	[75]
Thiothixene	DMDINC4	Moderate	Additive hypotensive effects by the combination of Valsartan and Thiothixene.	Schizophrenia [6A20]	[75]
Trifluoperazine	DMKBYWI	Moderate	Additive hypotensive effects by the combination of Valsartan and Trifluoperazine.	Schizophrenia [6A20]	[75]
Ziprasidone	DMM58JY	Moderate	Additive hypotensive effects by the combination of Valsartan and Ziprasidone.	Schizophrenia [6A20]	[75]
Risperidone	DMN6DXL	Moderate	Additive hypotensive effects by the combination of Valsartan and Risperidone.	Schizophrenia [6A20]	[75]
Olanzapine	DMPFN6Y	Moderate	Additive hypotensive effects by the combination of Valsartan and Olanzapine.	Schizophrenia [6A20]	[75]
Amisulpride	DMSJVAM	Moderate	Additive hypotensive effects by the combination of Valsartan and Amisulpride.	Schizophrenia [6A20]	[75]
Asenapine	DMSQZE2	Moderate	Additive hypotensive effects by the combination of Valsartan and Asenapine.	Schizophrenia [6A20]	[75]
Eltrombopag	DMOGFIX	Moderate	Decreased clearance of Valsartan due to the transporter inhibition by Eltrombopag.	Thrombocytopenia [3B64]	[85]
Tacrolimus	DMZ7XNQ	Moderate	Increased risk of hyperkalemia by the combination of Valsartan and Tacrolimus.	Transplant rejection [NE84]	[86]
Insulin-detemir	DMOA4VW	Moderate	Increased risk of hypoglycemia by the combination of Valsartan and Insulin-detemir.	Type-1/2 diabete [5A10-5A11]	[72]
Insulin degludec	DMPL395	Moderate	Increased risk of hypoglycemia by the combination of Valsartan and Insulin degludec.	Type-1/2 diabete [5A10-5A11]	[72]
Trimethoprim	DMM7CHK	Major	Increased risk of hyperkalemia by the combination of Valsartan and Trimethoprim.	Urinary tract infection [GC08]	[87]
Methdilazine	DMAUHQX	Moderate	Additive hypotensive effects by the combination of Valsartan and Methdilazine.	Vasomotor/allergic rhinitis [CA08]	[75]
Trimeprazine	DMEMV9D	Moderate	Additive hypotensive effects by the combination of Valsartan and Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[88]
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⏷ Show the Full List of 61 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
FD&C blue no. 2	E00446	2723854	Colorant
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF	E00255	17730	Colorant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium	E00625	Not Available	Disintegrant
Crospovidone	E00626	Not Available	Disintegrant
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Ferrosoferric oxide	E00231	14789	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Poloxamer 188	E00645	Not Available	Emulsifying agent; Solubilizing agent; Surfactant
Polyethylene glycol 3350	E00652	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 400	E00653	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
Polyvinyl alcohol	E00666	Not Available	Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
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
Vinylpyrrolidone	E00668	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
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⏷ Show the Full List of 23 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Valsartan 80 mg tablet	80 mg	Oral Tablet	Oral
Valsartan 160 mg tablet	160 mg	Oral Tablet	Oral
Valsartan 320 mg tablet	320 mg	Oral Tablet	Oral
Valsartan 40 mg tablet	40 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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