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

General Information of Drug (ID: DMB8UQ3)

• Drug Name: Ramatroban Drug Info
• Synonyms: 116649-85-5; Baynas; BAY u3405; Bay u-3405; Bay u 3406; Bay-u-3405; Bay u 3405; BAY-u 3405; UNII-P1ALI72U6C; C21H21FN2O4S; 3-[(3R)-3-[(4-fluorophenyl)sulfonylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]propanoic acid; P1ALI72U6C; 3-(4-Fluorophenylsulfonamido)-1,2,3,4-tetrahydro-9-carbazole propanoic acid; CHEMBL361812; (+)-(3R)-3-(p-Fluorobenzenesulfonamido)-1,2,3,4-tetrahydrocarbazole-9-propionic acid; NCGC00167519-01; EN-137774; DSSTox_RID_81819; Baynas (TN); Ramatroban (JAN/INN); [3H]ramatroban

Indication

Disease Entry	ICD 11	Status	REF
Perennial allergic rhinitis	CA08.03	Phase 2/3	[1]

• Cross-matching ID:
  PubChem CID: 123879
  ChEBI ID: CHEBI:32087
  CAS Number: CAS 116649-85-5
  TTD Drug ID: DMB8UQ3

Molecule-Related Drug Atlas

Drug(s) Targeting Prostaglandin D2 receptor 2 (PTGDR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[4]
Setipiprant	DMZ61IA	Asthma	CA23	Phase 3	[5]
Fevipiprant	DM4NX0C	Asthma	CA23	Phase 3	[6]
AMG 853	DM973N4	Asthma	CA23	Phase 2	[7]
ADC-3680	DM8GHIX	Allergic rhinitis	CA08.0	Phase 2	[8]
ARRY-502	DM17469	Allergic asthma	CA23.0	Phase 2	[9]
QAV-680	DMIZYV1	Allergic rhinitis	CA08.0	Phase 2	[10]
AP-761	DMISQOZ	Asthma	CA23	Phase 2	[11]
AZD1981	DMMCL9F	Chronic obstructive pulmonary disease	CA22	Phase 2	[12]
OC-000459	DM1JBD8	Allergy	4A80-4A85	Phase 2	[13]

Drug(s) Targeting Thromboxane A2 receptor (TBXA2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alprostadil	DMWH7NQ	Aorta coarctation		Approved	[14]
Ridogrel	DMWH9CN	Acute myocardial infarction	BA41	Approved	[15]
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[4]
KP-496	DMCO8UZ	Asthma	CA23	Phase 2	[16]
FK-070	DMJSD5W	Angina pectoris	BA40	Phase 2	[17]
TAK-128	DMHPEFS	Diabetic neuropathy	8C0Z	Phase 2	[18]
Ifetroban sodium	DMZP84Y	Thrombosis	DB61-GB90	Phase 2	[19]
Ifetroban	DMEV39E	Aspirin-induced asthma	CA23.20	Phase 2	[20]
YM-57158	DMS31YW	Allergic rhinitis	CA08.0	Phase 1	[21]
G-619	DM3H6YC	Thrombosis	DB61-GB90	Phase 1	[22]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Prostaglandin D2 receptor 2 (PTGDR2)	TTQDMX5	PD2R2_HUMAN	Antagonist	[2]
Thromboxane A2 receptor (TBXA2R)	TT2O84V	TA2R_HUMAN	Antagonist	[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: 1911).
• [2] CRTH2-specific binding characteristics of [3H]ramatroban and its effects on PGD2-, 15-deoxy-Delta12, 14-PGJ2- and indomethacin-induced agonist resp... Eur J Pharmacol. 2005 Nov 7;524(1-3):30-7.
• [3] Participation in cysteinyl leukotrienes and thromboxane A2 in nasal congestion model in Brown Norway rats. Int Immunopharmacol. 2007 Nov;7(11):1483-7.
• [4] 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.
• [5] Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug;44(8):1044-52.
• [6] Fevipiprant in the treatment of asthma. Expert Opin Investig Drugs. 2018 Feb;27(2):199-207.
• [7] Safety and efficacy of the prostaglandin D2 receptor antagonist AMG 853 in asthmatic patients.J Allergy Clin Immunol.2013 Feb;131(2):339-45.
• [8] Update on the status of DP2 receptor antagonists; from proof of concept through clinical failures to promising new drugs. Expert Opin Investig Drugs. 2014 Jan;23(1):55-66.
• [9] Clinical pipeline report, company report or official report of Array BioPharma (Drug: ARRY-502).
• [10] Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases. Bioorg Med Chem. 2013 Nov 1;21(21):6582-91.
• [11] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028464)
• [12] Clinical pipeline report, company report or official report of AstraZeneca (2009).
• [13] Anti-eosinophil activity and clinical efficacy of the CRTH2 antagonist OC000459 in eosinophilic esophagitis. Allergy. 2013 Mar;68(3):375-85.
• [14] 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.
• [15] Chronic ouabain treatment exacerbates blood pressure elevation in spontaneously hypertensive rats: the role of vascular mechanisms. J Hypertens. 2009 Jun;27(6):1233-42.
• [16] 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.
• [17] 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.
• [18] ClinicalTrials.gov (NCT00229437) Efficacy and Safety Study of TAK-128 in Treating Subjects With Diabetic Peripheral Neuropathy. U.S. National Institutes of Health.
• [19] 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.
• [20] Ifetroban sodium: an effective TxA2/PGH2 receptor antagonist. Cardiovasc Drug Rev. 2001 Summer;19(2):97-115.
• [21] 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.
• [22] G 619, a dual thromboxane synthase inhibitor and thromboxane A2 receptor antagonist, inhibits tumor necrosis factor-alpha biosynthesis. Eur J Pharmacol. 1995 Nov 3;286(1):31-9.