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

General Information of Drug (ID: DMN8DQH)

• Drug Name: Darusentan Drug Info
• Synonyms: Endothelin antagonist, BASF; HMR-4005; LU-127043; LU-135252

Indication

Disease Entry	ICD 11	Status	REF
Hypotension	BA20-BA21	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 177236
  CAS Number: CAS 171714-84-4
  TTD Drug ID: DMN8DQH

Molecule-Related Drug Atlas

Drug(s) Targeting Endothelin A receptor (EDNRA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bosentan	DMIOGBU	Pulmonary arterial hypertension	BB01.0	Approved	[3]
Ambrisentan	DMD1QXW	Pulmonary arterial hypertension	BB01.0	Approved	[4]
Macitentan	DMP79A1	Cardiovascular disease	BA00-BE2Z	Approved	[5]
Sparsentan	DMMP51W	IgA nephropathy	MF8Y	Approved	[6]
LU302146	DMMJVXZ	Pulmonary hypertension	BB01	Approved	[7]
Atrasentan	DMM74PK	Diabetic nephropathy	GB61.Z	Phase 3	[8]
Clazosentan	DMQSBX4	Cerebral vasospasm	BA85.Z	Phase 3	[9]
PF-1228305	DMS1EQ7	Pulmonary hypertension	BB01	Phase 3	[10]
BQ-123	DM0MO8I	Pulmonary arterial hypertension	BB01.0	Phase 2	[11]
FR139317	DMEL5SV	Hypertension	BA00-BA04	Phase 2	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Endothelin A receptor (EDNRA)	TTKRD0G	EDNRA_HUMAN	Antagonist	[2]

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: 3508).
• [2] Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [4] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [5] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [6] Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
• [7] Influence of endothelin receptor antagonists on myocardial protein kinase C isoforms in uraemic cardiomyopathy. Clin Sci (Lond). 2002 Aug;103 Suppl 48:276S-279S.
• [8] Effects of a selective ET(A)-receptor antagonist, atrasentan (ABT-627), in murine models of allergic asthma: demonstration of mouse strain specificity. Clin Sci (Lond). 2002 Aug;103 Suppl 48:367S-370S.
• [9] Effects of the selective endothelin A (ET(A)) receptor antagonist Clazosentan on cerebral perfusion and cerebral oxygenation following severe subar... Acta Neurochir (Wien). 2007;149(9):911-8; discussion 918.
• [10] Pfizer. Product Development Pipeline. March 31 2009.
• [11] Endothelin in heart failure: a promising therapeutic target Heart. 1997 Feb;77(2):93-4.
• [12] Reduction of bFGF-induced smooth muscle cell proliferation and endothelin receptor mRNA expression by mevastatin and atorvastatin. Biochem Pharmacol. 2002 Aug 1;64(3):497-505.