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

General Information of Drug (ID: DM5FW8Y)

• Drug Name: FR-158999 Drug Info
• Synonyms: 4-[4-(4-Amidinophenoxy)butyryl-L-aspartyl-L-valyl]thiomorpholine S,S-dioxide

Indication

Disease Entry	ICD 11	Status	REF
Thrombosis	DB61-GB90	Discontinued in Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 178035
  CAS Number: CAS 160138-41-0
  TTD Drug ID: DM5FW8Y

Molecule-Related Drug Atlas

Drug(s) Targeting Glycoprotein IIb/IIIa receptor (GPIIb/IIIa)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[3]
Eptifibatide	DMQXTJS	Acute cardiac ischemic events	BA40.Z	Approved	[4]
Tirofiban	DMQG17S	Acute coronary syndrome	BA41	Approved	[5]
Abciximab	DMJO6GV	Acute disease		Approved	[5]
DMP-444	DMO7BQS	Coronary artery disease	BA80	Phase 3	[6]
99mTc-rBitistatin	DMFAMNH	Pulmonary embolism	JB42	Phase 1/2	[7]
AjvW2	DM6PN4H	Thrombosis	DB61-GB90	Phase 1	[8]
SDZ-GPI-562	DMU9ZGN	Thrombosis	DB61-GB90	Phase 1	[9]
RGD-891	DMVJMF1	Thrombosis	DB61-GB90	Phase 1	[10]
Lefradafiban	DMKZVLH	Angina pectoris	BA40	Phase 1	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Glycoprotein IIb/IIIa receptor (GPIIb/IIIa)	TT38RM1	ITA2B_HUMAN; ITB3_HUMAN	Antagonist	[2]

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 800011969)
• [2] QSAR study of the peptidic fibrinogen inhibitors FK633, FR158999 and related derivatives, using a novel and useful hydrophobic descriptor (logPmw). Bioorganic & Medicinal Chemistry Letters Volume 8, Issue 18, 22 September 1998, Pages 2483-2488.
• [3] Accutin, a new disintegrin, inhibits angiogenesis in vitro and in vivo by acting as integrin alphavbeta3 antagonist and inducing apoptosis. Blood. 1998 Nov 1;92(9):3268-76.
• [4] Barbourin. A GPIIb-IIIa-specific integrin antagonist from the venom of Sistrurus m. barbouri. J Biol Chem. 1991 May 25;266(15):9359-62.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [6] Evaluation of Tc-99m-labeled glycoprotein IIb/IIIa receptor antagonist DMP444 SPECT in patients with infective endocarditis. Clin Nucl Med. 2003 Jun;28(6):480-4.
• [7] Platelet binding and biodistribution of [99mTc]rBitistatin in animal species and humans. Nucl Med Biol. 2007 Oct;34(7):855-63.
• [8] Novel approaches to the treatment of thrombosis. Trends Pharmacol Sci. 2002 Jan;23(1):25-32.
• [9] Heparin-induced thrombocytopenia: the role of platelet activation and therapeutic implications. Semin Thromb Hemost. 1999;25 Suppl 1:67-75.
• [10] Pharmacokinetics, pharmacodynamics, and safety of a platelet GPIIb/IIIa antagonist, RGD891, following intravenous administration in healthy male volunteers. J Clin Pharmacol. 2000 Nov;40(11):1245-56.
• [11] Pharmacodynamics and safety of lefradafiban, an oral platelet glycoprotein IIb/IIIa receptor antagonist, in patients with stable coronary artery disease undergoing elective angioplasty. Heart. 2001 Apr;85(4):444-50.