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

General Information of Drug (ID: DMYXD6A)

Drug Name

RWJ-58259 Drug Info

Synonyms

RWJ-58259; CHEMBL7642; SCHEMBL14090275; BDBM50098215; LS-30985

Indication

Disease Entry	ICD 11	Status	REF
Artery stenosis	BD52	Terminated	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Proteinase activated receptor 1 (F2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Vorapaxar	DMA16BR	Myocardial infarction	BA41-BA43	Approved	[2]
E5555	DMQERC6	Acute coronary syndrome	BA41	Phase 2	[3]
PZ-128	DMU5H3A	Peripheral arterial occlusive disorder	BD4Z	Phase 2	[4]
FR-171113	DMIQB9E	Thrombosis	DB61-GB90	Terminated	[5]
SCH-602539	DMRDM9S	Arteriosclerosis	BD40	Investigative	[6]
RWJ-56110	DME07AN	Discovery agent	N.A.	Investigative	[7]
SCH-205831	DM584T6	Thrombosis	DB61-GB90	Investigative	[8]
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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
Proteinase activated receptor 1 (F2R)	TTL935N	PAR1_HUMAN	Modulator	[1]

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References

1	RWJ-58259: a selective antagonist of protease activated receptor-1. Cardiovasc Drug Rev. 2003 Winter;21(4):313-26.
2	In Process Citation. Pharm Unserer Zeit. 2009;38(4):320-8.
3	Safety and tolerability of atopaxar in the treatment of patients with acute coronary syndromes: the lessons from antagonizing the cellular effects of Thrombin-Acute Coronary Syndromes Trial. Circulation. 2011 May 3;123(17):1843-53.
4	PAR1 (Protease-Activated Receptor 1) Pepducin Therapy Targeting Myocardial Necrosis in Coronary Artery Disease and Acute Coronary Syndrome Patients Undergoing Cardiac Catheterization: A Randomized, Placebo-Controlled, Phase 2 Study. Arterioscler Thromb Vasc Biol. 2020 Dec;40(12):2990-3003.
5	In vitro antiplatelet profile of FR171113, a novel non-peptide thrombin receptor antagonist. Eur J Pharmacol. 1999 Nov 19;384(2-3):197-202.
6	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. (Target id: 347).
7	Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. Proc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62.
8	Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4509-13.