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

General Information of Drug (ID: DMJLV03)

• Drug Name: Vapiprost Drug Info
• Synonyms: Vapiprost hydrochloride; GR-32191; GR-32191B; SN-309

Indication

Disease Entry	ICD 11	Status	REF
Cardiovascular disease	BA00-BE2Z	Terminated	[1]

• Cross-matching ID:
  PubChem CID: 6918030
  CAS Number: CAS 85505-64-2
  TTD Drug ID: DMJLV03

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	[4]
Ridogrel	DMWH9CN	Acute myocardial infarction	BA41	Approved	[5]
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[6]
Ramatroban	DMB8UQ3	Perennial allergic rhinitis	CA08.03	Phase 2/3	[7]
KP-496	DMCO8UZ	Asthma	CA23	Phase 2	[8]
FK-070	DMJSD5W	Angina pectoris	BA40	Phase 2	[9]
TAK-128	DMHPEFS	Diabetic neuropathy	8C0Z	Phase 2	[10]
Ifetroban sodium	DMZP84Y	Thrombosis	DB61-GB90	Phase 2	[11]
Ifetroban	DMEV39E	Aspirin-induced asthma	CA23.20	Phase 2	[12]
YM-57158	DMS31YW	Allergic rhinitis	CA08.0	Phase 1	[13]

Drug(s) Affected By Potassium voltage-gated channel subfamily H member 2 (KCNH2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metoclopramide	DMFA5MY	Nausea	MD90	Approved	[14]
Quinidine	DMLPICK	N. A.	N. A.	Approved	[15]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[16]
Erythromycin	DM4K7GQ	Acne vulgaris	ED80	Approved	[17]
Clarithromycin	DM4M1SG	Acute maxillary sinusitis		Approved	[17]
Disopyramide	DM5SYZP	Long QT syndrome	BC65.0	Approved	[18]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[19]
Amiodarone	DMUTEX3	Tachyarrhythmias	BC71	Approved	[20]
Dofetilide	DMPN1TW	Sinus rhythm disorder	BC9Y	Approved	[21]
Flecainide	DMSQDLE	Tachyarrhythmias	BC71	Approved	[17]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Thromboxane A2 receptor (TBXA2R)	TT2O84V	TA2R_HUMAN	Modulator	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Potassium voltage-gated channel subfamily H member 2 (KCNH2)	OTZX881H	KCNH2_HUMAN	Gene/Protein Processing	[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: 1976).
• [2] Effects of vapiprost, a novel thromboxane receptor antagonist, on thrombus formation and vascular patency after thrombolysis by tissue-type plasminogen activator.. Br J Pharmacol. 1992 July; 106(3): 533-538.
• [3] Why are most phospholipidosis inducers also hERG blockers?. Arch Toxicol. 2017 Dec;91(12):3885-3895. doi: 10.1007/s00204-017-1995-9. Epub 2017 May 27.
• [4] 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.
• [5] Chronic ouabain treatment exacerbates blood pressure elevation in spontaneously hypertensive rats: the role of vascular mechanisms. J Hypertens. 2009 Jun;27(6):1233-42.
• [6] 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.
• [7] Participation in cysteinyl leukotrienes and thromboxane A2 in nasal congestion model in Brown Norway rats. Int Immunopharmacol. 2007 Nov;7(11):1483-7.
• [8] 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.
• [9] 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.
• [10] ClinicalTrials.gov (NCT00229437) Efficacy and Safety Study of TAK-128 in Treating Subjects With Diabetic Peripheral Neuropathy. U.S. National Institutes of Health.
• [11] 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.
• [12] Ifetroban sodium: an effective TxA2/PGH2 receptor antagonist. Cardiovasc Drug Rev. 2001 Summer;19(2):97-115.
• [13] 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.
• [14] Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
• [15] Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
• [16] Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
• [17] Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
• [18] Pharmacology of the short QT syndrome N588K-hERG K+ channel mutation: differential impact on selected class I and class III antiarrhythmic drugs. Br J Pharmacol. 2008 Nov;155(6):957-66. doi: 10.1038/bjp.2008.325. Epub 2008 Aug 25.
• [19] Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. doi: 10.1038/sj.bjp.0706508.
• [20] Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 1999 Mar;359(3):212-9. doi: 10.1007/pl00005344.
• [21] Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. FEBS Lett. 2000 May 26;474(1):111-5. doi: 10.1016/s0014-5793(00)01586-6.