Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMREUQ6)

Drug Name

Valsartan Drug Info

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
Chronic heart failure	BD1Z	Approved	[1]
Hypertension	BA00-BA04	Approved	[2]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Phase 3	[3]
Nephropathy	GC2Z	Investigative	[1]

Therapeutic Class

Antihypertensive Agents

Cross-matching ID

PubChem CID: 60846
ChEBI ID: CHEBI:9927
CAS Number: CAS 137862-53-4
TTD Drug ID: DMREUQ6
VARIDT Drug ID: DR00071
INTEDE Drug ID: DR1668
ACDINA Drug ID: D00718

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiotensin II receptor type-1 (AGTR1)	TT8DBY3	AGTR1_HUMAN	Antagonist	[4]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Peptide transporter 1 (SLC15A1)	DT9G7XN	S15A1_HUMAN	Approved	[5]
Multidrug resistance-associated protein 2 (ABCC2)	DTFI42L	MRP2_HUMAN	Approved	[6]
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DT3D8F0	SO1B1_HUMAN	Approved	[7]
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DT9C1TS	SO1B3_HUMAN	Approved	[6]
Organic anion transporter 3 (SLC22A8)	DTVP67E	S22A8_HUMAN	Approved	[8]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[9]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Angiotensin II receptor type-1 (AGTR1)	DTT	AGTR1	9.315	6.241	6.761	5.625
Organic anion transporter 3 (SLC22A8)	DTP	OAT3	2.722	2.07	8.103	3.597
Multidrug resistance-associated protein 2 (ABCC2)	DTP	MRP2	7.751	4.17	6.425	6.282
Peptide transporter 1 (SLC15A1)	DTP	PEPT1	3.807	4.52	5.285	7.133
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	8.873	2.17	2.485	3.322
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	9.79	0.485	3.511	2.07
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Chronic heart failure

ICD Disease Classification

BD1Z

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 between Disease Section and Healthy Individual Tissue

References

1	Valsartan FDA Label
2	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: 3937).
3	Valsartan for Prevention of Acute Respiratory Distress Syndrome in Hospitalized Patients With SARS-COV-2 (COVID-19) Infection Disease
4	Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41.
5	High-affinity interaction of sartans with H+/peptide transporters. Drug Metab Dispos. 2009 Jan;37(1):143-9.
6	Involvement of transporters in the hepatic uptake and biliary excretion of valsartan, a selective antagonist of the angiotensin II AT1-receptor, in humans. Drug Metab Dispos. 2006 Jul;34(7):1247-54.
7	Regulation of Organic Anion Transporting Polypeptides (OATP) 1B1- and OATP1B3-Mediated Transport: An Updated Review in the Context of OATP-Mediated Drug-Drug Interactions. Int J Mol Sci. 2018 Mar 14;19(3). pii: E855.
8	Prediction of the overall renal tubular secretion and hepatic clearance of anionic drugs and a renal drug-drug interaction involving organic anion transporter 3 in humans by in vitro uptake experiments. Drug Metab Dispos. 2011 Jun;39(6):1031-8.
9	In vitro inhibition screening of human hepatic P450 enzymes by five angiotensin-II receptor antagonists. Eur J Clin Pharmacol. 2000 May;56(2):135-40.