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

General Information of Drug (ID: DMMSFK0)

• Drug Name: Fabesetron Drug Info
• Synonyms: FK-1052

Indication

Disease Entry	ICD 11	Status	REF
Irritable bowel syndrome	DD91.0	Discontinued in Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 208947
  ChEBI ID: CHEBI:31588
  CAS Number: CAS 129300-27-2
  TTD Drug ID: DMMSFK0

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 4 receptor (HTR4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cisapride	DMY7PED	Gastroesophageal reflux disease	DA22.Z	Approved	[3]
Tegaserod	DM3XYD1	Irritable bowel syndrome	DD91.0	Approved	[4]
R0-93877	DMM4U9G	Constipation	DD91.1	Approved	[5]
HTF 919	DM78G6F	Constipation	DD91.1	Approved	[6]
Mosapride	DM2VOQ3	N. A.	N. A.	Phase 4	[7]
Renzapride	DM7HQNX	Irritable bowel syndrome	DD91.0	Phase 3	[8]
Lintopride	DMSHGWN	Nausea	MD90	Phase 2	[9]
TD-8954	DM3C9NV	Gastrointestinal disease	DE2Z	Phase 2	[10]
SB-207266A	DM27KFY	Irritable bowel syndrome	DD91.0	Phase 2	[5]
YKP-GI	DM740LV	Constipation	DD91.1	Phase 2	[11]

Drug(s) Targeting 5-HT 3 receptor (5HT3R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ondansetron	DMOTQ1I	Chemotherapy-induced nausea	MD90	Approved	[12]
Granisetron	DMIUW25	Nausea and vomiting	MD90	Approved	[13]
Ramosetron	DMH7GN8	Nausea and vomiting	MD90	Approved	[14]
Y-25130	DMDPM7R	Nausea and vomiting	MD90	Approved	[15]
Renzapride	DM7HQNX	Irritable bowel syndrome	DD91.0	Phase 3	[8]
Litoxetine	DMKZRBP	Mood disorder	6A60-6E23	Phase 3	[16]
Zatosetron maleate	DMWDEFC	Anxiety disorder	6B00-6B0Z	Phase 3	[17]
Pancopride	DMIRYU9	Nausea	MD90	Phase 3	[18]
Lerisetron	DMOTCIU	Nausea	MD90	Phase 3	[19]
Lintopride	DMSHGWN	Nausea	MD90	Phase 2	[9]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 3 receptor (5HT3R)	TTNXLKE	NOUNIPROTAC	Modulator	[2]
5-HT 4 receptor (HTR4)	TT07C3Y	5HT4R_HUMAN	Modulator	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001434)
• [2] Pharmacological characterization of FK1052, a dihydropyridoindole derivative, as a new serotonin 3 and 4 dual receptor antagonist. J Pharmacol Exp Ther. 1993 May;265(2):752-8.
• [3] Metoclopramide stimulates catecholamine- and granin-derived peptide secretion from pheochromocytoma cells through activation of serotonin type 4 (5... Endocr Relat Cancer. 2009 Mar;16(1):281-90.
• [4] Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
• [5] Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
• [6] 5-Hydroxytryptamine mediated contractions in isolated preparations of equine ileum and pelvic flexure: pharmacological characterization of a new 5-HT(4) agonist. J Vet Pharmacol Ther. 2002 Feb;25(1):49-58.
• [7] The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):125-37.
• [8] Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome. Drugs R D. 2008;9(1):37-63.
• [9] The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.
• [10] The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol. 2011 May 30;2:25.
• [11] A randomized trial of 5-hydroxytryptamine4-receptor agonist, YKP10811, on colonic transit and bowel function in functional constipation. Clin Gastroenterol Hepatol. 2015 Apr;13(4):701-8.e1.
• [12] Treatment of pruritus in chronic liver disease with the 5-hydroxytryptamine receptor type 3 antagonist ondansetron: a randomized, placebo-controlled, double-blind cross-over trial. Eur J Gastroenterol Hepatol. 1998 Oct;10(10):865-70.
• [13] New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations. Cancer J. 2006 Sep-Oct;12(5):341-7.
• [14] Inhibitory effect of YM060 on 5-HT3 receptor-mediated depolarization in colonic myenteric neurons of the guinea pig. Eur J Pharmacol. 1995 Sep 5;283(1-3):107-12.
• [15] The antiemetic profile of Y-25130, a new selective 5-HT3 receptor antagonist. Eur J Pharmacol. 1991 Apr 24;196(3):299-305.
• [16] Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties. Eur J Pharmacol. 1993 Mar 2;232(2-3):139-45.
• [17] Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety. J Clin Psychopharmacol. 1999 Apr;19(2):125-31.
• [18] Pancopride, a potent and long-acting 5-HT3 receptor antagonist, is orally effective against anticancer drug-evoked emesis. Eur J Pharmacol. 1992 Nov 10;222(2-3):257-64.
• [19] Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.