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

General Information of Drug (ID: DMRK8OT)

Drug Name

Candesartan Drug Info

Synonyms

candesartan; 139481-59-7; Blopress; Ratacand; CV-11974; 1-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylic acid; CV 11974; UNII-S8Q36MD2XX; 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic acid; CHEMBL1016; S8Q36MD2XX; 2-Ethoxy-1-(p-(o-1H-tetrazol-5-ylphenyl)benzyl)-7-benzimidazolecarboxylic acid; CHEBI:3347; C24H20N6O3; 2-ethoxy-3-[[4-[2-(1h-tetrazol-5-yl)phenyl]phenyl]methyl]-3h-benzoimidazole-4-carboxylic acid; NCGC00167474-01; AK-57139; Blopress; Candesartan [BAN]; CV11974; Amias (TN); Atacand (TN); Blopress (TN); Candesartan [USAN:INN]; KS-5003; Ratacand (TN); Candesartan (USAN/INN); Atacand, Blopress, Amias, Ratacand,Candesartan; 2-(ethyloxy)-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid; 2-Ethoxy-3-[[4-[2-(1H-tetrazol-5-yl)phenyl]phenyl] methyl]-3H-benzoimidazole-4-carboxylic acid; 2-ethoxy-1-({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl)-1H-benzimidazole-7-carboxylic acid; 2-ethoxy-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid; 2-ethoxy-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4ethyl}-1H-benzimidazole-7-carboxylic acid; 2-ethoxy-7-carboxy-1-(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methylbenzimidazole; [3H]candesartan

Indication

Disease Entry	ICD 11	Status	REF
Chronic heart failure	BD1Z	Approved	[1]
Hypertension	BA00-BA04	Approved	[2]
Malignant essential hypertension	BA00	Approved	[1]

Therapeutic Class

Antihypertensive Agents

Cross-matching ID

PubChem CID: 2541
ChEBI ID: CHEBI:3347
CAS Number: CAS 139481-59-7
TTD Drug ID: DMRK8OT
VARIDT Drug ID: DR00601
INTEDE Drug ID: DR0264

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	[3]

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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	[4]
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Approved	[5]
Prostaglandin G/H synthase 1 (COX-1)	DE073H6	PGH1_HUMAN	Approved	[6]
Carboxylesterase 1 (CES1)	DEB30C5	EST1_HUMAN	Approved	[7]
UDP-glucuronosyltransferase 1A3 (UGT1A3)	DEF2WXN	UD13_HUMAN	Approved	[6]

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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
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
Prostaglandin G/H synthase 1 (COX-1)	DME	PTGS1	6.09	7.747	6.04	7.023

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
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	1.10E-01	-5.91E-02	-3.60E-01
Carboxylesterase 1 (CES1)	DME	CES1	2.02E-01	-7.66E-03	-1.88E-02
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	1.90E-01	-9.81E-03	-5.96E-02
Prostaglandin G/H synthase 1 (COX-1)	DME	PTGS1	3.97E-03	1.56E-01	4.33E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Candesartan 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: 587).
3	Candesartan: widening indications for this angiotensin II receptor blocker Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007.
4	Product Monograph of Atacand.
5	The human UDP-glucuronosyltransferase UGT1A3 is highly selective towards N2 in the tetrazole ring of losartan, candesartan, and zolarsartan. Biochem Pharmacol. 2008 Sep 15;76(6):763-72.
6	Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
7	Different hydrolases involved in bioactivation of prodrug-type angiotensin receptor blockers: carboxymethylenebutenolidase and carboxylesterase 1. Drug Metab Dispos. 2013 Nov;41(11):1888-95.