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

General Information of Drug (ID: DMZR7W6)

• Drug Name: isocarbacyclin Drug Info
• Synonyms: 9-O-methanoprostaglandin I

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 5311244
  CAS Number: CAS 88911-35-7
  TTD Drug ID: DMZR7W6

Molecule-Related Drug Atlas

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	[3]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[4]
Alprostadil	DMWH7NQ	Aorta coarctation		Approved	[5]
Iloprost	DMVPZBE	Pulmonary arterial hypertension	BB01.0	Approved	[6]
Omidenepag isopropyl	DMUX7Z8	Glaucoma/ocular hypertension	9C61	Approved	[7]
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[8]
16,16-dimethyl-PGE2	DMNF38S	Stem cell engraftment	QB63.8	Phase 2	[2]
CP-533536	DMZEJLB	Osteoporosis	FB83.0	Phase 2	[9]
Taprenepag	DM1TSHL	Glaucoma/ocular hypertension	9C61	Phase 2	[10]
TPST-1495	DM3GSB2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]

Drug(s) Targeting Prostaglandin E2 receptor EP3 (PTGER3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
16,16-dimethyl-PGE2	DMNF38S	Stem cell engraftment	QB63.8	Phase 2	[2]
ONO-9054	DM5O6GC	Glaucoma/ocular hypertension	9C61	Phase 2	[12]
PGF2alpha	DM4XAU7	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[2]
BUTAPROST	DMVYNJZ	Discovery agent	N.A.	Patented	[3]
DG041	DMVO9WM	Peripheral vascular disease	BD4Z	Discontinued in Phase 2	[13]
GR-63799X	DM13GK8	Asthma	CA23	Discontinued in Phase 1	[14]
U46619	DM13FX4	Discovery agent	N.A.	Investigative	[15]
carbacyclin	DMMBQYE	Discovery agent	N.A.	Investigative	[2]
PGD2	DMYDW6J	Discovery agent	N.A.	Investigative	[16]
butaprost (free acid form)	DM5MZHP	Discovery agent	N.A.	Investigative	[15]

Drug(s) Targeting Prostacyclin receptor (PTGIR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Treprostinil	DMTIQF3	Pulmonary arterial hypertension	BB01.0	Approved	[17]
Selexipag	DMAHSU0	Pulmonary arterial hypertension	BB01.0	Approved	[18]
Epoprostenol	DMUTYR2	Allergic rhinitis	CA08.0	Approved	[19]
Dinoprost Tromethamine	DMXQKSL	Abortion	JA00	Approved	[20]
Misoprostol	DMHVJFK	Medical abortion	JA00.1Z	Approved	[20]
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[8]
Beraprost	DML634R	Pulmonary hypertension	BB01	Phase 4	[21]
esuberaprost	DMXLGED	Gout	FA25	Phase 3	[22]
Ralinepag	DM7G4Y9	Pulmonary arterial hypertension	BB01.0	Phase 2	[23]
Clinprost	DM6E5VA	Asthma	CA23	Discontinued in Preregistration	[24]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Prostacyclin receptor (PTGIR)	TTOFYT1	PI2R_HUMAN	Agonist	[2]
Prostaglandin E2 receptor EP2 (PTGER2)	TT1ZAVI	PE2R2_HUMAN	Agonist	[2]
Prostaglandin E2 receptor EP3 (PTGER3)	TTPNGDE	PE2R3_HUMAN	Agonist	[2]

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: 1934).
• [2] 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.
• [3] 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.
• [4] 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).
• [5] Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
• [6] 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.
• [7] Clinical pipeline report, company report or official report of Santen Pharmaceutical.
• [8] 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.
• [9] Pfizer. Product Development Pipeline. March 31 2009.
• [10] 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.
• [11] Clinical pipeline report, company report or official report of Tempest Therapeutics.
• [12] IOP-Lowering Effect of ONO-9054, A Novel Dual Agonist of Prostanoid EP3 and FP Receptors, in Monkeys. Invest Ophthalmol Vis Sci. 2015 Apr;56(4):2547-52.
• [13] BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8.
• [14] Effects of the prostanoid EP3-receptor agonists M&B 28767 and GR 63799X on infarct size caused by regional myocardial ischaemia in the anaesthetized rat. Br J Pharmacol. 1999 Feb;126(4):849-58.
• [15] The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93.
• [16] Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes. Eur J Pharmacol. 1997 Dec 11;340(2-3):227-41.
• [17] Dosing considerations in the use of intravenous prostanoids in pulmonary arterial hypertension: an experience-based review. Am Heart J. 2009 Apr;157(4):625-35.
• [18] Selexipag: an oral, selective prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. Eur Respir J. 2012 Oct;40(4):874-80.
• [19] Novel signaling pathways promote a paracrine wave of prostacyclin-induced vascular smooth muscle differentiation. J Mol Cell Cardiol. 2009 May;46(5):682-94.
• [20] Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J Biol Chem. 2003 Feb 28;278(9):6947-58.
• [21] Prostaglandin I2 IP Receptor Agonist, Beraprost, Prevents Transient Global Cerebral Ischemia Induced Hippocampal CA1 Injury in Aging Mice. J Neurol Disord. 2014;2:1000174.
• [22] Specific binding of the new stable epoprostenol analogue beraprost sodium to prostacyclin receptors on human and rat platelets. Arzneimittelforschung. 1989 Apr;39(4):495-9.
• [23] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [24] Protective effect of a prostaglandin I2 analog, TEI-7165, on ischemic neuronal damage in gerbils. Brain Res. 1997 Sep 26;769(2):321-8.