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

General Information of DTT (ID: TTQDMX5)

• DTT Name: Prostaglandin D2 receptor 2 (PTGDR2) DTT Info
• Gene Name: PTGDR2

Molecule-Related Drug & Molecule List

1 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[1]

16 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fevipiprant	DM4NX0C	Asthma	CA23	Phase 3	[2]
Setipiprant	DMZ61IA	Asthma	CA23	Phase 3	[3]
Ramatroban	DMB8UQ3	Perennial allergic rhinitis	CA08.03	Phase 2/3	[4]
ADC-3680	DM8GHIX	Allergic rhinitis	CA08.0	Phase 2	[5]
AMG 853	DM973N4	Asthma	CA23	Phase 2	[6]
AP-761	DMISQOZ	Asthma	CA23	Phase 2	[7]
ARRY-502	DM17469	Allergic asthma	CA23.0	Phase 2	[8]
AZD1981	DMMCL9F	Chronic obstructive pulmonary disease	CA22	Phase 2	[9]
BBI-5000	DMR59I4	Alopecia	ED70	Phase 2	[10]
GB001	DM58TGA	Asthma	CA23	Phase 2	[11]
OC-000459	DM1JBD8	Allergy	4A80-4A85	Phase 2	[12]
QAV-680	DMIZYV1	Allergic rhinitis	CA08.0	Phase 2	[13]
AM-211	DMVXRYC	Asthma	CA23	Phase 1	[14]
AM-461	DM7Z8NP	Respiratory disease	CB40	Phase 1	[15]
MK-7246	DMLQOF1	Respiratory disease	CB40	Phase 1	[16]
PGF2alpha	DM4XAU7	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[17]

3 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AZD5985	DMCAKMV	Chronic obstructive pulmonary disease	CA22	Discontinued in Phase 1	[9]
AZD8075	DMKF9U3	Chronic obstructive pulmonary disease	CA22	Discontinued in Phase 1	[9]
RG-7185	DM12VHC	Asthma	CA23	Discontinued in Phase 1	[18]

38 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
13,14-dihydro-15-keto-PGD2	DMZVWCG	Discovery agent	N.A.	Investigative	[4]
13,14-dihydro-15-keto-PGF2alpha	DMNT1XI	Discovery agent	N.A.	Investigative	[19]
15(R)-15-methyl-PGD2	DMY9ZT8	Discovery agent	N.A.	Investigative	[4]
15(S)-15-methyl-PGD2	DMG273T	Discovery agent	N.A.	Investigative	[19]
15-deoxy-Delta12,14-PGD2	DMJ27QT	Discovery agent	N.A.	Investigative	[17]
15-deoxy-Delta12,14-PGJ2	DMNDECA	Discovery agent	N.A.	Investigative	[17]
2-(2,4-diphenylthiazol-5-yl)acetic acid	DMG49N2	Discovery agent	N.A.	Investigative	[20]
2-(2-acetyl-4-bromophenoxy)acetic acid	DMITKZY	Discovery agent	N.A.	Investigative	[21]
2-(2-allyl-4-chlorophenoxy)acetic acid	DMXDGEF	Discovery agent	N.A.	Investigative	[22]
2-(2-benzhydryl-4-phenylthiazol-5-yl)acetic acid	DMN6IV2	Discovery agent	N.A.	Investigative	[23]
2-(2-benzoyl-4-bromophenoxy)acetic acid	DMLOD2Y	Discovery agent	N.A.	Investigative	[21]
2-(2-cyclohexyl-4-fluorophenoxy)acetic acid	DMUN2CS	Discovery agent	N.A.	Investigative	[22]
2-(2-cyclohexyl-4-methoxyphenoxy)acetic acid	DMSI07M	Discovery agent	N.A.	Investigative	[22]
2-(2-cyclohexyl-4-methylphenoxy)acetic acid	DMVCY42	Discovery agent	N.A.	Investigative	[22]
2-(2-cyclohexylphenoxy)acetic acid	DM81WJK	Discovery agent	N.A.	Investigative	[22]
2-(2-formylphenoxy)acetic acid	DMMEBH3	Discovery agent	N.A.	Investigative	[21]
2-(4-bromo-2-(hydroxymethyl)phenoxy)acetic acid	DM7QK5C	Discovery agent	N.A.	Investigative	[21]
2-(4-bromo-2-cyclohexylphenoxy)acetic acid	DM6I1NQ	Discovery agent	N.A.	Investigative	[22]
2-(4-bromo-2-formylphenoxy)acetic acid	DMQVUZP	Discovery agent	N.A.	Investigative	[21]
2-(4-bromo-2-tert-butylphenoxy)acetic acid	DMXAQZ0	Discovery agent	N.A.	Investigative	[21]
2-(4-chloro-2-cycloheptylphenoxy)acetic acid	DM15YM7	Discovery agent	N.A.	Investigative	[24]
2-(4-chloro-2-cyclohexylphenoxy)acetic acid	DMGYZ8D	Discovery agent	N.A.	Investigative	[22]
2-(4-chloro-2-cyclopentylphenoxy)acetic acid	DMA6KQU	Discovery agent	N.A.	Investigative	[22]
2-(4-cyano-2-cyclohexylphenoxy)acetic acid	DM4XFJI	Discovery agent	N.A.	Investigative	[22]
3-(4-chloro-2-cyclohexylphenoxy)propanoic acid	DMQ2D09	Discovery agent	N.A.	Investigative	[22]
4-(4-chloro-2-cyclohexylphenoxy)butanoic acid	DM14I6C	Discovery agent	N.A.	Investigative	[22]
ADC-9971	DMY6PMJ	Allergic rhinitis	CA08.0	Investigative	[25]
AM-156	DMGCOQF	Allergic rhinitis	CA08.0	Investigative	[25]
CAY 10471	DM4O69H	Allergy	4A80-4A85	Investigative	[26]
Delta12-PGJ2	DMB6ADI	Discovery agent	N.A.	Investigative	[19]
IW-1221	DMBTWF0	Asthma	CA23	Investigative	[25]
L-888,291	DMMAIQ2	Discovery agent	N.A.	Investigative	[27]
L-888607	DMJCTWO	Discovery agent	N.A.	Investigative	[28]
Methyl 2-(4-chloro-2-cyclohexylphenoxy)acetate	DMA82IQ	Discovery agent	N.A.	Investigative	[22]
PGD2	DMYDW6J	Discovery agent	N.A.	Investigative	[4]
PGD3	DMWNCLJ	Discovery agent	N.A.	Investigative	[17]
PGJ2	DMR2LTC	Discovery agent	N.A.	Investigative	[19]
U46619	DM13FX4	Discovery agent	N.A.	Investigative	[19]

References

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• [2] Fevipiprant in the treatment of asthma. Expert Opin Investig Drugs. 2018 Feb;27(2):199-207.
• [3] Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug;44(8):1044-52.
• [4] 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.
• [5] 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.
• [6] Safety and efficacy of the prostaglandin D2 receptor antagonist AMG 853 in asthmatic patients.J Allergy Clin Immunol.2013 Feb;131(2):339-45.
• [7] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028464)
• [8] Clinical pipeline report, company report or official report of Array BioPharma (Drug: ARRY-502).
• [9] Clinical pipeline report, company report or official report of AstraZeneca (2009).
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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• [12] Anti-eosinophil activity and clinical efficacy of the CRTH2 antagonist OC000459 in eosinophilic esophagitis. Allergy. 2013 Mar;68(3):375-85.
• [13] 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.
• [14] Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation. J Pharmacol Exp Ther. 2011 Jul;338(1):290-301.
• [15] A novel DP2 receptor antagonist (AM-461): a patent evaluation of WO2011085033. Expert Opin Ther Pat. 2011 Dec;21(12):1931-6.
• [16] Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. Bioorg Med Chem Lett. 2011 Jan 1;21(1):288-93.
• [17] Expression and molecular pharmacology of the mouse CRTH2 receptor. J Pharmacol Exp Ther. 2003 Aug;306(2):463-70.
• [18] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033115)
• [19] Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2. Br J Pharmacol. 2002 Dec;137(8):1163-72.
• [20] Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1177-80.
• [21] Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits. J Med Chem. 2006 Nov 16;49(23):6638-41.
• [22] 2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50.
• [23] Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1181-5.
• [24] 7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8.
• [25] 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. (Target id: 339).
• [26] Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem. 2005 Feb 24;48(4):897-900.
• [27] Identification of a potent and selective synthetic agonist at the CRTH2 receptor. Mol Pharmacol. 2005 Jun;67(6):1834-9.
• [28] Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2. J Med Chem. 2005 Oct 6;48(20):6174-7.