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

General Information of Drug (ID: DMHT84I)

Drug Name

A-216546 Drug Info

Synonyms

ABT-546; (2S,3R,4S)-1-[2-(Dibutylamino)-2-oxoethyl]-2-(2,2-dimethylpentyl)-4-(7-methoxy-1,3-benzodioxol-5-yl)tetrahydro-1H-pyrrole-3-carboxylic acid

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[1]

Cross-matching ID

PubChem CID: 71587660
CAS Number: CAS 223756-43-2
TTD Drug ID: DMHT84I

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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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]
Darusentan	DMN8DQH	Hypotension	BA20-BA21	Phase 3	[11]
BQ-123	DM0MO8I	Pulmonary arterial hypertension	BB01.0	Phase 2	[12]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

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

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References

1	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010699)
2	Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor. Eur J Pharmacol. 1999 Feb 5;366(2-3):189-201.
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 ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62.
12	Endothelin in heart failure: a promising therapeutic target Heart. 1997 Feb;77(2):93-4.