Tegaserod

Summary

Tegaserod (CHEMBL76370) is an approved small-molecule serotonergic agonist (ATC A06AX06) targeting HTR2B and HTR4; indicated across 3 conditions including constipation disorder and gastroesophageal reflux disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A06AX06
• Targets: 2 (HTR2B, HTR4)
• Indications: 3 conditions
• Clinical trials: 25
• Chemistry: 301.39 Da · C16H23N5O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL76370
Name	Tegaserod
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	135409453
ChEBI	CHEBI:51043
ATC	A06AX06
Molecular formula	C16H23N5O
Molecular weight	301.39
InChIKey	IKBKZGMPCYNSLU-RGVLZGJSSA-N

SMILES: CCCCCN=C(N)N/N=C/C1=CNC2=C1C=C(C=C2)OC

IUPAC name: 1-[(E)-(5-methoxy-1H-indol-3-yl)methylideneamino]-2-pentylguanidine

Pharmacological roles (ChEBI): serotonergic agonist, gastrointestinal drug.

Also known as: HTF 919, HTF919, SDZ-HTF-919, Tegaserod, tegaserod, SID26749090, TEGASEROD, SID144205034, SID170466887

Parent form; salt/anhydrous children: CHEMBL533819, CHEMBL1516474, CHEMBL4303321

Patent coverage: 1,275 distinct patent families (4,580 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 4,574 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
HTR2B	5-HT2B receptor	Antagonist	8.4	0.4%	P41595
HTR4	5-HT4 receptor	Partial agonist	8.4	0%	Q13639

Broader ChEMBL bioactivity targets: 49 (assay-derived). Sample: Vasopressin V2 receptor, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, 5-hydroxytryptamine receptor 4, Vasopressin V1a receptor, 5-hydroxytryptamine receptor 3A, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Amine oxidase [flavin-containing] A, D(1A) dopamine receptor.

Bioactivity

ChEMBL activities: 60 potent at pChembl ≥ 5 of 78 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HTR4	9	EC50	1	nM	CHEMBL_ACT_10952239
HTR4	8.7	EC50	2	nM	CHEMBL_ACT_10952336
HTR4	8.6	EC50	2.51	nM	CHEMBL_ACT_11022002
HTR4	8.6	EC50	2.51	nM	CHEMBL_ACT_13376721
HTR4	8.4	Ki	3.98	nM	CHEMBL_ACT_10952203
HTR4	8.4	Ki	3.98	nM	CHEMBL_ACT_11022001
HTR4	8.4	Ki	3.98	nM	CHEMBL_ACT_13376742
HTR4	8.4	Ki	3.98	nM	CHEMBL_ACT_2411223
O70528	8.2	EC50	6.31	nM	CHEMBL_ACT_10952349
O70528	8.2	EC50	6.31	nM	CHEMBL_ACT_11021998
O70528	7.9	EC50	12.59	nM	CHEMBL_ACT_13375236
HTR4	7.8	EC50	15.85	nM	CHEMBL_ACT_10952342
HTR2B	7.69	AC50	20.6	nM	CHEMBL_ACT_25164216
HTR4	7.51	Ki	31	nM	CHEMBL_ACT_2536460
HTR1A	7.4	AC50	40	nM	CHEMBL_ACT_25165449
HTR1A	6.77	AC50	168.9	nM	CHEMBL_ACT_25164629
HTR2A	6.76	AC50	174.3	nM	CHEMBL_ACT_25173748
HTR5A	6.72	AC50	190	nM	CHEMBL_ACT_25163948
HTR6	6.7	AC50	197.6	nM	CHEMBL_ACT_25119005
SLC6A2	6.58	AC50	260	nM	CHEMBL_ACT_25146425
ADRA1A	6.57	AC50	266.9	nM	CHEMBL_ACT_25138500
ADRA2A	6.51	AC50	310.1	nM	CHEMBL_ACT_25156046
DRD1	6.47	AC50	340	nM	CHEMBL_ACT_25180924
HTR2B	6.46	AC50	342.8	nM	CHEMBL_ACT_25227916
SLC6A2	6.3	AC50	495.1	nM	CHEMBL_ACT_25145406
HTR2C	6.26	AC50	543.4	nM	CHEMBL_ACT_25132206
DRD4	6.18	AC50	656.5	nM	CHEMBL_ACT_25127458
DRD1	6.14	AC50	730	nM	CHEMBL_ACT_25115635
ADRA2C	6.11	AC50	771.1	nM	CHEMBL_ACT_25148299
HTR7	6.1	AC50	802.3	nM	CHEMBL_ACT_25119150

Target pathways

Aggregated over 2 target gene(s): HTR2B, HTR4.

Top Reactome pathways

9 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	2	HTR2B, HTR4
Signaling by GPCR	2	HTR2B, HTR4
Class A/1 (Rhodopsin-like receptors)	2	HTR2B, HTR4
Amine ligand-binding receptors	2	HTR2B, HTR4
GPCR downstream signalling	2	HTR2B, HTR4
Serotonin receptors	2	HTR2B, HTR4
GPCR ligand binding	2	HTR2B, HTR4
G alpha (q) signalling events	1	HTR2B
G alpha (s) signalling events	1	HTR4

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	2
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	2
chemical synaptic transmission	2
G protein-coupled serotonin receptor signaling pathway	2
signal transduction	2
neural crest cell migration	1
positive regulation of cytokine production	1
positive regulation of endothelial cell proliferation	1
heart morphogenesis	1
cardiac muscle hypertrophy	1
intracellular calcium ion homeostasis	1
phospholipase C-activating serotonin receptor signaling pathway	1
serotonin receptor signaling pathway	1
positive regulation of cell population proliferation	1
response to xenobiotic stimulus	1

Indications & clinical

Indications

3 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
constipation disorder	4	MONDO:0002203	HP:0002019
gastroesophageal reflux disease	3	MONDO:0007186	EFO:0003948
dyspepsia	3	MONDO:0002268	EFO:0008533

Clinical trials

Total trials: 25.

Phase distribution

Phase	Trials
PHASE3	13
PHASE4	6
Not specified	3
PHASE2	2
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00142987	PHASE4	COMPLETED	Efficacy of Tegaserod in Relieving the Symptoms of Female Patients With Irritable Bowel Syndrome (IBS), Excluding Those With Predominant Diarrhea IBS
NCT00149877	PHASE4	COMPLETED	Efficacy, Safety and Tolerability of Tegaserod in Patients With Chronic Constipation
NCT00171522	PHASE4	COMPLETED	Preference of Tegaserod vs. PEG 3350 in Patients With Constipation
NCT00277550	PHASE4	WITHDRAWN	The Effects of Tegaserod vs. Placebo on Whole Gut Transit Time in Patients With Chronic Constipation and Dyspepsia
NCT00348634	PHASE4	TERMINATED	Effect of Tegaserod on Orocecal Transit in Elderly Chronic Constipation Patients
NCT00390975	PHASE4	TERMINATED	Effect of Tegaserod on Gastric Emptying in Patients With Diabetic Gastroparesis
NCT00139568	PHASE3	COMPLETED	An Evaluation of the Efficacy and Safety of Tegaserod 6 mg Bid Given Orally to Chinese Patients With Chronic Constipation
NCT00141089	PHASE3	COMPLETED	Assessment of Efficacy and Safety of Tegaserod in Male Patients With Chronic Constipation.
NCT00171418	PHASE3	COMPLETED	Assessment of the Effects of Tegaserod in the Management of Gastroesophageal Reflux Disease (GERD) in Patients With Incomplete Response to Proton Pump Inhibitors (PPIs).
NCT00171431	PHASE3	TERMINATED	The Effect of Tegaserod on Patterns of Flow in the Small Bowel of Patients With Irritable Bowel Syndrome (IBS)
NCT00171457	PHASE3	COMPLETED	The Effects of Tegaserod on Mechanical Sensitivity of the Esophagus and Stomach in Patients With Heartburn and Dyspepsia.
NCT00171470	PHASE3	COMPLETED	The Role of Tegaserod Therapy in the Management of Dyspeptic Symptoms in Female Patients on Proton Pump Inhibitors for the Treatment of Heartburn.
NCT00171483	PHASE3	COMPLETED	Assessment of the Role of Tegaserod Therapy in the Management of Gastroesophageal Reflux Disease (GERD) Symptoms in Patients With Incomplete Response to Proton Pump Inhibitors (PPIs).
NCT00232024	PHASE3	COMPLETED	Assessment of Efficacy and Safety of Tegaserod Treatment and Placebo in Women With Dyspepsia
NCT00232037	PHASE3	COMPLETED	Extension Study to Assess the Long-Term Safety of Tegaserod in Women With Symptoms of Dyspepsia
NCT00232089	PHASE3	COMPLETED	Assessment of Efficacy and Safety of Tegaserod Treatment and Placebo in Women With Dyspepsia
NCT00232102	PHASE3	COMPLETED	Extension Study to Assess the Long-Term Safety of Tegaserod in Women With Symptoms of Dyspepsia
NCT00365820	PHASE2/PHASE3	TERMINATED	Efficacy and Safety of Tegaserod in Opioid-induced Constipation in Patients With Non-cancer Pain
NCT00399659	PHASE3	TERMINATED	Safety and Efficacy of Tegaserod in Opioid-induced Constipation in Patients With Non-cancer Pain.
NCT00414024	PHASE3	TERMINATED	Safety and Efficacy of Tegaserod in Opioid-induced Constipation in Patients With Non-cancer Pain.
NCT00142974	PHASE2	TERMINATED	Assessment of the Effect of Tegaserod (2 mg Tid and 6 mg Tid) on Dyspeptic Symptoms in Diabetic Patients With Symptoms of Diabetic Gastropathy
NCT00149851	PHASE2	COMPLETED	A Study to Assess the Efficacy, Safety and Tolerability of Tegaserod Alone and in Combination With Omeprazole Given Orally in Patients With Symptoms of Symptomatic Gastroesophageal Reflux Disease (sGERD)
NCT00511771	Not specified	NO_LONGER_AVAILABLE	A Treatment Investigational New Drug (tIND) Program of Tegaserod in Women With Irritable Bowel Syndrome With Constipation or With Chronic Idiopathic Constipation
NCT00563615	Not specified	UNKNOWN	Study of Effect of Tegaserod on Small and Large Bowel Transit by Scintigraphic Method
NCT00563758	Not specified	TERMINATED	A Randomized, Double-blind, Placebo-controlled Multicenter Study to Assess the Efficacy, Safety and Tolerability of Tegaserod 2 mg Bid vs Placebo in Patients With Chronic Constipation

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

406 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
CYPROHEPTADINE	ChEMBL + PubChem	Phase 4 (approved)	HTR2B, HTR4
DONEPEZIL	ChEMBL + PubChem	Phase 4 (approved)	HTR2B, HTR4
HALOPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	HTR2B, HTR4
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	HTR2B, HTR4
CISAPRIDE	ChEMBL	Phase 4 (approved)	HTR2B, HTR4
METOCLOPRAMIDE	ChEMBL	Phase 4 (approved)	HTR2B, HTR4
TROPISETRON	ChEMBL	Phase 4 (approved)	HTR2B, HTR4
SEROTONIN	ChEMBL	Phase 3	HTR2B, HTR4
LITOXETINE	ChEMBL	Phase 2	HTR2B, HTR4
MEBUFOTENIN	ChEMBL	Phase 2	HTR2B, HTR4
APREMILAST	ChEMBL + PubChem	Phase 4 (approved)	HTR2B
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	HTR2B
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	HTR2B
OLODATEROL	ChEMBL + PubChem	Phase 4 (approved)	HTR2B
PRUCALOPRIDE	ChEMBL + PubChem	Phase 4 (approved)	HTR4
ABEMACICLIB	ChEMBL	Phase 4 (approved)	HTR2B
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	HTR2B
AGOMELATINE	ChEMBL	Phase 4 (approved)	HTR2B
ALECTINIB	ChEMBL	Phase 4 (approved)	HTR2B
ALMOTRIPTAN	ChEMBL	Phase 4 (approved)	HTR2B
ALOSETRON	ChEMBL	Phase 4 (approved)	HTR2B
AMILORIDE	ChEMBL	Phase 4 (approved)	HTR2B
AMIODARONE	ChEMBL	Phase 4 (approved)	HTR2B
AMISULPRIDE	ChEMBL	Phase 4 (approved)	HTR2B
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	HTR2B
AMLODIPINE	ChEMBL	Phase 4 (approved)	HTR2B
AMODIAQUINE	ChEMBL	Phase 4 (approved)	HTR2B
AMOXAPINE	ChEMBL	Phase 4 (approved)	HTR2B
APOMORPHINE	ChEMBL	Phase 4 (approved)	HTR2B
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	HTR2B
ASENAPINE	ChEMBL	Phase 4 (approved)	HTR2B
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	HTR2B
ATOMOXETINE	ChEMBL	Phase 4 (approved)	HTR2B
AZATADINE	ChEMBL	Phase 4 (approved)	HTR2B
AZELASTINE	ChEMBL	Phase 4 (approved)	HTR2B
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	HTR2B
BENFLUOREX	ChEMBL	Phase 4 (approved)	HTR2B
BENPERIDOL	ChEMBL	Phase 4 (approved)	HTR2B
BENZBROMARONE	ChEMBL	Phase 4 (approved)	HTR2B
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	HTR2B
BENZTROPINE	ChEMBL	Phase 4 (approved)	HTR2B
BEPRIDIL	ChEMBL	Phase 4 (approved)	HTR2B
BITHIONOL	ChEMBL	Phase 4 (approved)	HTR2B
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	HTR2B
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	HTR2B
BROMPERIDOL	ChEMBL	Phase 4 (approved)	HTR2B
BUSPIRONE	ChEMBL	Phase 4 (approved)	HTR2B
CABERGOLINE	ChEMBL	Phase 4 (approved)	HTR2B
CABOZANTINIB	ChEMBL	Phase 4 (approved)	HTR2B
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	HTR2B
CANNABIDIOL	ChEMBL	Phase 4 (approved)	HTR2B
CARBENOXOLONE	ChEMBL	Phase 4 (approved)	HTR2B
CARIPRAZINE	ChEMBL	Phase 4 (approved)	HTR2B
CARVEDILOL	ChEMBL	Phase 4 (approved)	HTR2B
CEPHALEXIN	ChEMBL	Phase 4 (approved)	HTR2B
CETIRIZINE	ChEMBL	Phase 4 (approved)	HTR2B
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	HTR2B
CHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	HTR2B
CHLORPHENTERMINE	ChEMBL	Phase 4 (approved)	HTR2B
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	HTR2B