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

General Information of Drug (ID: DM3GSB2)

• Drug Name: TPST-1495 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

• Cross-matching ID: TTD Drug ID: DM3GSB2

Molecule-Related Drug Atlas

Drug(s) Targeting Prostaglandin E2 receptor EP4 (PTGER4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
16,16-dimethyl-PGE2	DMNF38S	Stem cell engraftment	QB63.8	Phase 2	[3]
RQ-00000007 (oral)	DMMYTRU	Pain	MG30-MG3Z	Phase 2	[4]
ONO-AE1-437	DMCUGI8	Asthma	CA23	Phase 2	[5]
BGC-20-1531	DMS2MQ5	Migraine	8A80	Phase 2	[6]
IK-007	DMBLFPN	Non-small-cell lung cancer	2C25	Phase 1/2	[7]
E7046	DMFVT43	Rectal adenocarcinoma	2B92	Phase 1	[8]
ONO-4232	DMO4SD2	Acute heart failure	BD10-BD13	Phase 1	[9]
ONO-4578	DME63VK	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
AN0025	DMGSYPY	Aggressive cancer	2A00-2F9Z	Phase 1	[10]
PGF2alpha	DM4XAU7	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[11]

Drug(s) Targeting Prostaglandin E2 receptor EP2 (PTGER2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dinoprostone	DMTYOPD	Medical abortion	JA00.1Z	Approved	[12]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[13]
Alprostadil	DMWH7NQ	Aorta coarctation		Approved	[14]
Iloprost	DMVPZBE	Pulmonary arterial hypertension	BB01.0	Approved	[15]
Omidenepag isopropyl	DMUX7Z8	Glaucoma/ocular hypertension	9C61	Approved	[16]
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[17]
16,16-dimethyl-PGE2	DMNF38S	Stem cell engraftment	QB63.8	Phase 2	[3]
CP-533536	DMZEJLB	Osteoporosis	FB83.0	Phase 2	[18]
Taprenepag	DM1TSHL	Glaucoma/ocular hypertension	9C61	Phase 2	[19]
PF-4418948	DMMETU8	Endometriosis	GA10	Phase 1	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Prostaglandin E2 receptor EP2 (PTGER2)	TT1ZAVI	PE2R2_HUMAN	Antagonist	[2]
Prostaglandin E2 receptor EP4 (PTGER4)	TT79WV3	PE2R4_HUMAN	Antagonist	[2]

References

• [1] ClinicalTrials.gov (NCT04344795) Phase 1a/1b Study of TPST-1495 in Subjects With Solid Tumors. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of Tempest Therapeutics.
• [3] 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.
• [4] Clinical pipeline report, company report or official report of Avarx.
• [5] An EP4 receptor agonist prevents indomethacin-induced closure of rat ductus arteriosus in vivo. Pediatr Res. 2004 Oct;56(4):586-90.
• [6] BGC20-1531, a novel, potent and selective prostanoid EP4 receptor antagonist: a putative new treatment for migraine headache. Br J Pharmacol. 2009 January; 156(2): 316-327.
• [7] Grapiprant: an EP4 prostaglandin receptor antagonist and novel therapy for pain and inflammation. Vet Med Sci. 2015 Dec 21;2(1):3-9.
• [8] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [9] ONO-4232, an EP4-selective Agonist, Improves Left Ventricular Diastolic Dysfunction and Ameliorates Acute and Chronic Heart Failure in Animal Models. Circulation. 2012; 126: A15345.
• [10] AN0025, a novel antagonist of PGE2-receptor E-type 4 (EP4), in combination with total neoadjuvant treatment of advanced rectal cancer. Radiother Oncol. 2023 Aug;185:109669.
• [11] Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes. Eur J Pharmacol. 1997 Dec 11;340(2-3):227-41.
• [12] 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.
• [13] 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: 341).
• [14] Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
• [15] Exploration of prostanoid receptor subtype regulating estradiol and prostaglandin E2 induction of spinophilin in developing preoptic area neurons. Neuroscience. 2007 May 25;146(3):1117-27.
• [16] Clinical pipeline report, company report or official report of Santen Pharmaceutical.
• [17] 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.
• [18] Pfizer. Product Development Pipeline. March 31 2009.
• [19] A phase 2, randomized, dose-response trial of taprenepag isopropyl (PF-04217329) versus latanoprost 0.005% in open-angle glaucoma and ocular hypertension. Curr Eye Res. 2011 Sep;36(9):809-17.