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

General Information of Drug (ID: DMIYJ2M)

• Drug Name: STA2 Drug Info
• Synonyms: 11alpha-carba-9alpha,11beta-thia-Txa2

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 5311453
  TTD Drug ID: DMIYJ2M

Molecule-Related Drug Atlas

Drug(s) Targeting Thromboxane A2 receptor (TBXA2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alprostadil	DMWH7NQ	Aorta coarctation		Approved	[3]
Ridogrel	DMWH9CN	Acute myocardial infarction	BA41	Approved	[4]
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[5]
Ramatroban	DMB8UQ3	Perennial allergic rhinitis	CA08.03	Phase 2/3	[6]
KP-496	DMCO8UZ	Asthma	CA23	Phase 2	[7]
FK-070	DMJSD5W	Angina pectoris	BA40	Phase 2	[8]
TAK-128	DMHPEFS	Diabetic neuropathy	8C0Z	Phase 2	[9]
Ifetroban sodium	DMZP84Y	Thrombosis	DB61-GB90	Phase 2	[10]
Ifetroban	DMEV39E	Aspirin-induced asthma	CA23.20	Phase 2	[11]
YM-57158	DMS31YW	Allergic rhinitis	CA08.0	Phase 1	[12]

Drug(s) Targeting Prostaglandin E2 receptor EP3 (PTGER3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
16,16-dimethyl-PGE2	DMNF38S	Stem cell engraftment	QB63.8	Phase 2	[2]
ONO-9054	DM5O6GC	Glaucoma/ocular hypertension	9C61	Phase 2	[13]
PGF2alpha	DM4XAU7	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[2]
BUTAPROST	DMVYNJZ	Discovery agent	N.A.	Patented	[14]
DG041	DMVO9WM	Peripheral vascular disease	BD4Z	Discontinued in Phase 2	[15]
GR-63799X	DM13GK8	Asthma	CA23	Discontinued in Phase 1	[16]
U46619	DM13FX4	Discovery agent	N.A.	Investigative	[17]
carbacyclin	DMMBQYE	Discovery agent	N.A.	Investigative	[2]
PGD2	DMYDW6J	Discovery agent	N.A.	Investigative	[18]
butaprost (free acid form)	DM5MZHP	Discovery agent	N.A.	Investigative	[17]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Prostaglandin E2 receptor EP3 (PTGER3)	TTPNGDE	PE2R3_HUMAN	Agonist	[2]
Thromboxane A2 receptor (TBXA2R)	TT2O84V	TA2R_HUMAN	Agonist	[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: 1939).
• [2] Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24.
• [3] Flow after prostaglandin E1 is mediated by receptor-coupled adenylyl cyclase in human anterior segments. Invest Ophthalmol Vis Sci. 1999 Oct;40(11):2622-6.
• [4] Chronic ouabain treatment exacerbates blood pressure elevation in spontaneously hypertensive rats: the role of vascular mechanisms. J Hypertens. 2009 Jun;27(6):1233-42.
• [5] Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806.
• [6] Participation in cysteinyl leukotrienes and thromboxane A2 in nasal congestion model in Brown Norway rats. Int Immunopharmacol. 2007 Nov;7(11):1483-7.
• [7] Effects of KP-496, a novel dual antagonist for leukotriene D4 and thromboxane A2 receptors, on contractions induced by various agonists in the guinea pig trachea. Allergol Int. 2006 Dec;55(4):403-10.
• [8] Pharmacokinetic and pharmacodynamic properties of FK070 (KDI-792), a novel thromboxane receptor antagonist/thromboxane synthetase inhibitor, after single and multiple oral administrations to healthy volunteers. J Pharm Pharmacol. 1996 Apr;48(4):380-5.
• [9] ClinicalTrials.gov (NCT00229437) Efficacy and Safety Study of TAK-128 in Treating Subjects With Diabetic Peripheral Neuropathy. U.S. National Institutes of Health.
• [10] AT-1 receptor antagonism modifies the mediation of endothelin-1, thromboxane A2, and catecholamines in the renal constrictor response to angiotensin II. Kidney Int Suppl. 2005 Jan;(93):S3-9.
• [11] Ifetroban sodium: an effective TxA2/PGH2 receptor antagonist. Cardiovasc Drug Rev. 2001 Summer;19(2):97-115.
• [12] In vitro pharmacologic profile of YM158, a new dual antagonist for LTD4 and TXA2 receptors. J Pharmacol Exp Ther. 1998 Nov;287(2):633-9.
• [13] IOP-Lowering Effect of ONO-9054, A Novel Dual Agonist of Prostanoid EP3 and FP Receptors, in Monkeys. Invest Ophthalmol Vis Sci. 2015 Apr;56(4):2547-52.
• [14] Evaluation of WO 2012/177618 A1 and US-2014/0179750 A1: novel small molecule antagonists of prostaglandin-E2 receptor EP2.Expert Opin Ther Pat. 2015 Jul;25(7):837-44.
• [15] BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8.
• [16] Effects of the prostanoid EP3-receptor agonists M&B 28767 and GR 63799X on infarct size caused by regional myocardial ischaemia in the anaesthetized rat. Br J Pharmacol. 1999 Feb;126(4):849-58.
• [17] The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93.
• [18] Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes. Eur J Pharmacol. 1997 Dec 11;340(2-3):227-41.