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

General Information of Drug (ID: DMM4U9G)

• Drug Name: R0-93877 Drug Info
• Synonyms: Prucalopride; 179474-81-8; UNII-0A09IUW5TP; 4-Amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide; 0A09IUW5TP; C18H26ClN3O3; CHEMBL117287; R-093877; 4-amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide; R 093877; 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide; 4-Amino-5-chloro-2,3-dihydro-N-(1-(3-methoxypropyl)-4-piperidyl)-7-benzofurancarboxamide; R093877; Motegrity; Prucalopride [USAN:INN:BAN]

Indication

Disease Entry	ICD 11	Status	REF
Constipation	DD91.1	Approved	[1]
Irritable bowel syndrome	DD91.0	Approved	[2]

• Cross-matching ID:
  PubChem CID: 3052762
  ChEBI ID: CHEBI:135552
  CAS Number: CAS 179474-81-8
  TTD Drug ID: DMM4U9G
  VARIDT Drug ID: DR00187
  ACDINA Drug ID: D01369

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	[5]
Tegaserod	DM3XYD1	Irritable bowel syndrome	DD91.0	Approved	[6]
HTF 919	DM78G6F	Constipation	DD91.1	Approved	[7]
Mosapride	DM2VOQ3	N. A.	N. A.	Phase 4	[8]
Renzapride	DM7HQNX	Irritable bowel syndrome	DD91.0	Phase 3	[9]
Lintopride	DMSHGWN	Nausea	MD90	Phase 2	[10]
TD-8954	DM3C9NV	Gastrointestinal disease	DE2Z	Phase 2	[11]
SB-207266A	DM27KFY	Irritable bowel syndrome	DD91.0	Phase 2	[3]
YKP-GI	DM740LV	Constipation	DD91.1	Phase 2	[12]
TD-5108	DM6SANW	Gastroparesis	DA41.00	Phase 2	[8]

Drug(s) Transported By P-glycoprotein 1 (ABCB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amoxicillin	DMUYNEI	Acute otitis media	AB00	Approved	[13]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[14]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[15]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[16]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[15]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[15]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[17]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[15]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[18]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 4 receptor (HTR4)	TT07C3Y	5HT4R_HUMAN	Agonist	[3]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[4]

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [2] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [3] Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
• [4] Resolor, INN-prucalopride
• [5] 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.
• [6] Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
• [7] 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.
• [8] 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.
• [9] 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.
• [10] The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.
• [11] 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.
• [12] 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.
• [13] Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
• [14] MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
• [15] Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
• [16] Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
• [17] Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
• [18] Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
• [19] Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.