General Information of Drug (ID: DM3XYD1)

Drug Name
Tegaserod Drug Info
Synonyms Tegaserod (USAN/INN); 1-[[(Z)-(5-methoxyindol-3-ylidene)methyl]amino]-2-pentylguanidine
Indication
Disease Entry ICD 11 Status REF
Irritable bowel syndrome DD91.0 Approved [1]
Dyspepsia MD92 Withdrawn from market [2]
Gastro-oesophageal reflux DA22 Withdrawn from market [2]
Cross-matching ID
PubChem CID
135409453
ChEBI ID
CHEBI:51043
CAS Number
CAS 145158-71-0
TTD Drug ID
DM3XYD1
VARIDT Drug ID
DR00018
INTEDE Drug ID
DR1541

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
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]
R0-93877 DMM4U9G Constipation DD91.1 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 [6]
YKP-GI DM740LV Constipation DD91.1 Phase 2 [12]
TD-5108 DM6SANW Gastroparesis DA41.00 Phase 2 [8]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [13]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [14]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [15]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [16]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [17]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [18]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [19]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [20]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [21]
Propranolol DM79NTF Angina pectoris BA40 Approved [22]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 1A2 (CYP1A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zolmitriptan DM1IB4Q Migraine 8A80 Approved [23]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [23]
Etoricoxib DM6A4NW Rheumatoid arthritis FA20 Approved [23]
Capsaicin DMGMF6V Back pain ME84.Z Approved [24]
Hesperetin DMKER83 High blood cholesterol level 5C80.00 Approved [25]
Stiripentol DMMSDOY Dravet syndrome 8A61.11 Approved [26]
Nifedipine DMSVOZT Angina pectoris BA40 Approved [27]
Zileuton DMVRIC2 Allergic asthma CA23.0 Approved [28]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [29]
Clonidine DM6RZ9Q Attention deficit hyperactivity disorder 6A05.Z Approved [30]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2D6 (CYP2D6) Main DME DECB0K3 CP2D6_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cytochrome P450 1A2 (CYP1A2) OTLLBX48 CP1A2_HUMAN Gene/Protein Processing [4]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 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: 226).
3 Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
4 In vitro metabolism of tegaserod in human liver and intestine: assessment of drug interactions. Drug Metab Dispos. 2001 Oct;29(10):1269-76.
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 Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
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 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
14 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
15 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
16 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
17 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
18 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
19 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
20 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
21 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
22 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
23 In vitro inhibition of CYP1A2 by model inhibitors, anti-inflammatory analgesics and female sex steroids: predictability of in vivo interactions. Basic Clin Pharmacol Toxicol. 2008 Aug;103(2):157-65.
24 Effects of capsaicin and dihydrocapsaicin on human and rat liver microsomal CYP450 enzyme activities in vitro and in vivo. J Asian Nat Prod Res. 2012;14(4):382-95.
25 Drug interaction study of flavonoids toward CYP3A4 and their quantitative structure activity relationship (QSAR) analysis for predicting potential effects. Toxicol Lett. 2018 Sep 15;294:27-36.
26 Stiripentol. Expert Opin Investig Drugs. 2005 Jul;14(7):905-11.
27 Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):843-52.
28 Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor. Drug Metab Dispos. 2003 Nov;31(11):1352-60.
29 Predictive three-dimensional quantitative structure-activity relationship of cytochrome P450 1A2 inhibitors. J Med Chem. 2005 Jun 2;48(11):3808-15.
30 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.