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

General Information of Drug (ID: DM07K2I)

• Drug Name: Eprosartan Drug Info
• Synonyms: 133040-01-4; Teveten; F-108566; F 108566; UNII-2KH13Z0S0Y; (E)-4-((2-Butyl-5-(2-carboxy-3-(thiophen-2-yl)prop-1-en-1-yl)-1H-imidazol-1-yl)methyl)benzoic acid; (E)-2-Butyl-1-(p-carboxybenzyl)-alpha-2-thenylimidazole-5-acrylic acid; CHEMBL813; SK-108566; 2KH13Z0S0Y; CHEBI:4814; 4-({2-butyl-5-[(1E)-2-carboxy-3-(2-thienyl)prop-1-en-1-yl]-1H-imidazol-1-yl}methyl)benzoic acid; (E)-3-[2-n-butyl-1-{(4-carboxyphenyl)methyl}-1H-imidazol-5-yl]-2-(2-thienyl)methyl-2-propenoic acid; SK&F 108566; SKF-108566; Teveten (TN); Eprosartan (USAN/INN); Eprosartan [USAN:BAN:INN]; SK&F-108566; (4-carboxybenzyl)imidazole-5-acrylic acid; (E)-alpha{[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazole-5-yl]methylene}-2-thiopheneproprionic acid; 4-({2-butyl-5-[(1E)-2-carboxy-3-(thiophen-2-yl)prop-1-en-1-yl]-1H-imidazol-1-yl}methyl)benzoic acid; 4-[[2-butyl-5-[(E)-3-hydroxy-3-oxo-2-(thiophen-2-ylmethyl)prop-1-enyl]imidazol-1-yl]methyl]benzoic acid; [3H]eprosartan

Indication

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

• Therapeutic Class: Antihypertensive Agents
• Cross-matching ID:
  PubChem CID: 5281037
  ChEBI ID: CHEBI:4814
  CAS Number: CAS 133040-01-4
  TTD Drug ID: DM07K2I
  VARIDT Drug ID: DR01208
  ACDINA Drug ID: D00236

Molecule-Related Drug Atlas

Drug(s) Targeting Angiotensin II receptor type-1 (AGTR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Losartan	DM72JXH	Diabetic kidney disease	GB61.Z	Approved	[4]
Olmesartan medoxomil	DMWBHRY	High blood pressure	BA00	Approved	[5]
Irbesartan	DMTP1DC	Diabetic kidney disease	GB61.Z	Approved	[4]
Valsartan	DMREUQ6	Chronic heart failure	BD1Z	Approved	[4]
Candesartan	DMRK8OT	Chronic heart failure	BD1Z	Approved	[6]
Telmisartan	DMS3GX2	Hypertension	BA00-BA04	Approved	[7]
ANGIOTENSIN II	DMLWQ27	Increase blood pressure	BA04	Approved	[8]
SARALASIN	DMKS1DV	Hypertension	BA00-BA04	Approved	[9]
Tasosartan	DMM13DI	Hypertension	BA00-BA04	Approved	[10]
Sparsentan	DMMP51W	IgA nephropathy	MF8Y	Approved	[11]

Drug(s) Transported By Peptide transporter 1 (SLC15A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amoxicillin	DMUYNEI	Acute otitis media	AB00	Approved	[12]
Sulfasalazine	DMICA9H	Irritable bowel syndrome	DD91.0	Approved	[13]
Ampicillin	DMHWE7P	Acute epiglottitis		Approved	[14]
Losartan	DM72JXH	Diabetic kidney disease	GB61.Z	Approved	[3]
Enalapril	DMNFUZR	Congestive heart failure	BD10	Approved	[15]
Cefazolin	DMPDYFR	Bacteremia	1A73	Approved	[16]
Ceftriaxone	DMCEW64	Acute gonococcal cervicitis		Approved	[17]
Dexamethasone	DMMWZET	Acute adrenal insufficiency		Approved	[13]
Cefadroxil	DMMC345	Bacterial infection	1A00-1C4Z	Approved	[3]
Irbesartan	DMTP1DC	Diabetic kidney disease	GB61.Z	Approved	[3]

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	[2]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Peptide transporter 1 (SLC15A1)	DT9G7XN	S15A1_HUMAN	Substrate	[3]

References

• [1] 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: 588).
• [2] Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7.
• [3] High-affinity interaction of sartans with H+/peptide transporters. Drug Metab Dispos. 2009 Jan;37(1):143-9.
• [4] Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41.
• [5] Mechanism of diastolic stiffening of the failing myocardium and its prevention by angiotensin receptor and calcium channel blockers. J Cardiovasc Pharmacol. 2009 Jul;54(1):47-56.
• [6] Candesartan: widening indications for this angiotensin II receptor blocker Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007.
• [7] Deletion of angiotensin II type I receptor reduces hepatic steatosis. J Hepatol. 2009 Jun;50(6):1226-35.
• [8] The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1. J Med Chem. 2010 Mar 11;53(5):2063-75.
• [9] Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.
• [10] Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54.
• [11] Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
• [12] Interactions of amoxicillin and cefaclor with human renal organic anion and peptide transporters. Drug Metab Dispos. 2006 Apr;34(4):547-55.
• [13] Peptide transporter substrate identification during permeability screening in drug discovery: comparison of transfected MDCK-hPepT1 cells to Caco-2 cells. Arch Pharm Res. 2007 Apr;30(4):507-18.
• [14] Several hPepT1-transported drugs are substrates of the Escherichia coli proton-coupled oligopeptide transporter YdgR. Res Microbiol. 2017 Jun;168(5):443-449.
• [15] The intestinal H+/peptide symporter PEPT1: structure-affinity relationships. Eur J Pharm Sci. 2004 Jan;21(1):53-60.
• [16] Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1. J Med Chem. 2005 Jun 30;48(13):4410-9.
• [17] Intestinal transport of beta-lactam antibiotics: analysis of the affinity at the H+/peptide symporter (PEPT1), the uptake into Caco-2 cell monolayers and the transepithelial flux. Pharm Res. 1999 Jan;16(1):55-61.