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

General Information of Drug (ID: DMZ61IA)

• Drug Name: Setipiprant Drug Info
• Synonyms: ACT-129968

Indication

Disease Entry	ICD 11	Status	REF
Asthma	CA23	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 49843471
  CAS Number: CAS 866460-33-5
  TTD Drug ID: DMZ61IA

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]
Fevipiprant	DM4NX0C	Asthma	CA23	Phase 3	[5]
Ramatroban	DMB8UQ3	Perennial allergic rhinitis	CA08.03	Phase 2/3	[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 Prostaglandin D2 receptor (PTGDR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[4]
QAW-039	DMPCFXN	Asthma	CA23	Phase 3	[14]
AMG 853	DM973N4	Asthma	CA23	Phase 2	[7]
ONO-4053	DMX4MVP	Allergic rhinitis	CA08.0	Phase 2	[15]
TS-022	DMMNXIW	Atopic dermatitis	EA80	Phase 2	[16]
S-555739	DMXDVNZ	Allergy	4A80-4A85	Phase 2	[17]
MK-1029	DM8ZTW7	Asthma	CA23	Phase 2	[8]
SAR-389644	DMA6O9R	Allergic rhinitis	CA08.0	Phase 1	[18]
192C86	DMQ8NTZ	Thrombosis	DB61-GB90	Phase 1	[19]
MK-1092	DMHS79I	Type-1 diabetes	5A10	Phase 1	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Prostaglandin D2 receptor (PTGDR)	TTNVEIR	PD2R_HUMAN	Antagonist	[2]
Prostaglandin D2 receptor 2 (PTGDR2)	TTQDMX5	PD2R2_HUMAN	Antagonist	[3]

References

• [1] ClinicalTrials.gov (NCT01484119) Efficacy, Safety, and Tolerability Study of ACT-129968 in Patients With Seasonal Allergic Rhinitis. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug;44(8):1044-52.
• [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] Fevipiprant in the treatment of asthma. Expert Opin Investig Drugs. 2018 Feb;27(2):199-207.
• [6] 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.
• [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] Effect Of QAW039, An Oral Prostaglandin D2 Receptor (DP2/CRTh2) Antagonist, Upon Sputum And Bronchial Eosinophilic Inflammation And Clinical Outcomes In Treatment-Resistant Asthma: A Phase 2a Randomized Placebo-Controlled Trial. American Thoracic Society Journals. 2015.
• [15] Effect of ONO-4053, a DP1 (prostaglandin D2 receptor) Antagonist, on Prostaglandin D2-Induced Nasal Congestion. Journal of Allergy and Clinical Immunology Volume 135, Issue 2, Supplement, February 2015, Pages AB219.
• [16] Effects of TS-022, a newly developed prostanoid DP1 receptor agonist, on experimental pruritus, cutaneous barrier disruptions and atopic dermatitis... Eur J Pharmacol. 2007 Feb 5;556(1-3):207-14.
• [17] Clinical pipeline report, company report or official report of Shionogi (2011).
• [18] US patent application no. 2008,0300,217, Combination therapy with fumaric acid esters for the treatment of autoimmune and,or inflammatory disorders.
• [19] Prostanoid receptor antagonists: development strategies and therapeutic applications. Br J Pharmacol. 2009 September; 158(1): 104-145.
• [20] The challenge of modulating -cell autoimmunity in type 1 diabetes. Lancet Diabetes Endocrinol. 2019 Jan;7(1):52-64.