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

General Information of Drug (ID: DMQG17S)

• Drug Name: Tirofiban Drug Info
• Synonyms: AGG; Aggrastat; Agrastat; Tirofibanum; Aggrastat (TN); Agrastat (TN); L-700462; MK-383; Tirofiban (INN); Tirofiban[BAN:INN]; Tirofiban [INN:BAN]; L-700,462; N-(BUTYLSULFONYL)-O-[4-(4-PIPERIDINYL)BUTYL]-L-TYROSINE; N-(Butylsulfonyl)-O-(4-(4-piperidyl)butyl)-L-tyrosine; N-(butylsulfonyl)-O-(4-piperidin-4-ylbutyl)-L-tyrosine; N-(butylsulfonyl)-o-[4-(piperidin-4-yl)butyl]-l-tyrosine; (2S)-2-(butylsulfonylamino)-3-[4-(4-piperidin-4-ylbutoxy)phenyl]propanoic acid

Indication

Disease Entry	ICD 11	Status	REF
Acute coronary syndrome	BA41	Approved	[1]

• Therapeutic Class: Fibrinolytic Agents
• Cross-matching ID:
  PubChem CID: 60947
  ChEBI ID: CHEMBL916
  CAS Number: CAS 144494-65-5
  TTD Drug ID: DMQG17S

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	[4]
Eptifibatide	DMQXTJS	Acute cardiac ischemic events	BA40.Z	Approved	[5]
Abciximab	DMJO6GV	Acute disease		Approved	[2]
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]
XEMILOFIBAN	DMBRYT8	Cardiovascular disease	BA00-BE2Z	Discontinued in Phase 3	[12]

Drug(s) Affected By Integrin alpha-IIb (ITGA2B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[13]
Dactinomycin	DM2YGNW	Adult kidney Wilms tumor		Approved	[14]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[15]
Asasantin	DMCZIHT	Cerebrovascular ischaemia	8B1Z	Approved	[13]
Rosiglitazone	DMILWZR	Chronic kidney disease	GB61	Approved	[16]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[14]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[17]
Nicotine	DMWX5CO	Lung cancer	2C25.0	Approved	[18]
Abciximab	DMJO6GV	Acute disease		Approved	[3]
Eptifibatide	DMQXTJS	Acute cardiac ischemic events	BA40.Z	Approved	[3]

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	Modulator	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Integrin alpha-IIb (ITGA2B)	OT4Y17PY	ITA2B_HUMAN	Drug Response	[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: 6586).
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [3] ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
• [4] 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.
• [5] Barbourin. A GPIIb-IIIa-specific integrin antagonist from the venom of Sistrurus m. barbouri. J Biol Chem. 1991 May 25;266(15):9359-62.
• [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.
• [12] Glycoprotein IIb/IIIa receptor number and occupancy during chronic administration of an oral antagonist. J Pharmacol Exp Ther. 2000 Nov;295(2):670-6.
• [13] Magnitude and time course of platelet inhibition with Aggrenox and Aspirin in patients after ischemic stroke: the AGgrenox versus Aspirin Therapy Evaluation (AGATE) trial. Eur J Pharmacol. 2004 Sep 24;499(3):315-24. doi: 10.1016/j.ejphar.2004.07.114.
• [14] Genomic profiling uncovers a molecular pattern for toxicological characterization of mutagens and promutagens in vitro. Toxicol Sci. 2011 Jul;122(1):185-97.
• [15] Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
• [16] Proteomic analysis of human adipose tissue after rosiglitazone treatment shows coordinated changes to promote glucose uptake. Obesity (Silver Spring). 2010 Jan;18(1):27-34. doi: 10.1038/oby.2009.208. Epub 2009 Jun 25.
• [17] Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
• [18] Cholinergic drugs inhibit in?vitro megakaryopoiesis via the alpha7-nicotinic acetylcholine receptor. Platelets. 2011;22(5):390-5. doi: 10.3109/09537104.2010.551304. Epub 2011 Mar 9.