Mosapride

Summary

Mosapride (CHEMBL60889) is a phase-3 clinical-stage small molecule (ATC A03FA09) targeting HTR4; indicated across 8 conditions including irritable bowel syndrome and constipation disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: A03FA09
• Targets: 1 (HTR4)
• Indications: 8 conditions
• Clinical trials: 23
• Chemistry: 421.9 Da · C21H25ClFN3O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL60889
Name	Mosapride
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	119584
ChEBI	CHEBI:167204
ATC	A03FA09
Molecular formula	C21H25ClFN3O3
Molecular weight	421.9
InChIKey	YPELFRMCRYSPKZ-UHFFFAOYSA-N

SMILES: CCOC1=CC(=C(C=C1C(=O)NCC2CN(CCO2)CC3=CC=C(C=C3)F)Cl)N

IUPAC name: 4-amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide

ChEBI definition: A benzamide resulting from the formal condensation of the carboxy group of 4-amino-5-chloro-2-ethoxybenzoic acid with the amino group of 1-[4-(4-fluorobenzyl)morpholin-2-yl]methanamine.

Also known as: Mosaprida, Mosapride, Mosart, SID29216210, SID50110109, SID174006284, MOSAPRIDE, Mosapride citrate, mosapride

Parent form; salt/anhydrous children: CHEMBL1733174

Patent coverage: 1,123 distinct patent families (3,271 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,243 (99%) 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
HTR4	5-HT4 receptor	Full agonist	6.9	0%	Q13639

Broader ChEMBL bioactivity targets: 19 (assay-derived). Sample: Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2B adrenergic receptor, Menin/Histone-lysine N-methyltransferase MLL, Serotonin 3 (5-HT3) receptor, 5-hydroxytryptamine receptor 1A, 5-hydroxytryptamine receptor 2C, Sodium-dependent serotonin transporter.

Bioactivity

ChEMBL activities: 28 potent at pChembl ≥ 5 of 31 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
O70528	7.16	Ki	69.9	nM	CHEMBL_ACT_1205797
O70528	7.08	Ki	84	nM	CHEMBL_ACT_647860
O70528	6.95	IC50	113	nM	CHEMBL_ACT_846058
SIGMAR1	6.89	Ki	128.4	nM	CHEMBL_ACT_7769232
O70528	6.83	Ki	147	nM	CHEMBL_ACT_7769226
HTR2B	6.72	Ki	188.3	nM	CHEMBL_ACT_7769220
HTR2C	6.68	Ki	207.7	nM	CHEMBL_ACT_7769222
LMNA	6.65	Potency	223.9	nM	CHEMBL_ACT_3623330
HTR2B	6.53	IC50	295.9	nM	CHEMBL_ACT_7769219
SIGMAR1	6.51	IC50	305.6	nM	CHEMBL_ACT_7769231
CYP1A2	6.4	IC50	400	nM	CHEMBL_ACT_7767042
HTR2C	6.4	IC50	396.6	nM	CHEMBL_ACT_7769221
CYP3A4	6.16	IC50	700	nM	CHEMBL_ACT_7767054
ADRA2B	6.06	Ki	871	nM	CHEMBL_ACT_7764998
O70528	6.05	IC50	881.8	nM	CHEMBL_ACT_7769225
CYP2C19	6	IC50	1000	nM	CHEMBL_ACT_7767046
CYP2C9	6	IC50	1000	nM	CHEMBL_ACT_7767048
P35563	5.92	Ki	1189	nM	CHEMBL_ACT_1205796
ADRA2A	5.86	Ki	1380	nM	CHEMBL_ACT_7764996
ADRA2B	5.72	IC50	1908	nM	CHEMBL_ACT_7764997
SLC6A4	5.69	Ki	2025	nM	CHEMBL_ACT_7769230
ADRA2A	5.52	AC50	3009	nM	CHEMBL_ACT_25156271
ADRA2A	5.43	IC50	3679	nM	CHEMBL_ACT_7764995
SLC6A4	5.42	IC50	3812	nM	CHEMBL_ACT_7769229
KCNH2	5.32	IC50	4800	nM	CHEMBL_ACT_2609321
KCNH2	5.32	IC50	4786	nM	CHEMBL_ACT_5219027
HTR1A	5.29	AC50	5180	nM	CHEMBL_ACT_25164866
DRD3	5.16	AC50	6855	nM	CHEMBL_ACT_25194368

Target pathways

Aggregated over 1 target gene(s): HTR4.

Top Reactome pathways

8 total, by targets touching each:

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

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	1
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	1
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
adenylate cyclase-activating serotonin receptor signaling pathway	1
adenylate cyclase-inhibiting serotonin receptor signaling pathway	1
chemical synaptic transmission	1
maintenance of gastrointestinal epithelium	1
regulation of appetite	1
mucus secretion	1
large intestinal transit	1
regulation of postsynapse assembly	1
system process	1
signal transduction	1
G protein-coupled serotonin receptor signaling pathway	1

Indications & clinical

Indications

8 indications (0 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
irritable bowel syndrome	3	MONDO:0005052	EFO:0000555
constipation disorder	3	MONDO:0002203	HP:0002019
dyspepsia	3	MONDO:0002268	EFO:0008533
ileus	3	MONDO:0004567	MONDO:0004567
gastritis	1	MONDO:0004966	EFO:0000217
diarrheal disease	1	MONDO:0001673	HP:0002014
rectal disorder	1	MONDO:0001593	EFO:0000405

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 23.

Phase distribution

Phase	Trials
PHASE4	7
PHASE3	6
Not specified	6
PHASE1/PHASE2	2
PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00663897	PHASE4	COMPLETED	Lansoprazole Versus Mosapride for Functional Dyspepsia
NCT02056405	PHASE4	UNKNOWN	Effect of Mosapride on Postoperative Ileus in Patients Undergoing Colorectal Surgery
NCT02180334	PHASE4	COMPLETED	The Effect of Combination of Mosapride and DPP-4 Inhibitor on Plasma Concentration of Incretin Hormones
NCT02264587	PHASE4	UNKNOWN	Effects and Mechanism of Mosapride Citrate on Diabetic Gastroparesis
NCT02433847	PHASE4	UNKNOWN	Effect of Mosapride on Gut Transit in Patients With Chronic Constipation or Constipated Irritable Bowel Syndrome and Healthy Subjects
NCT02606617	PHASE4	UNKNOWN	A Clinical Trial Analyzing Effects of Prokinetic Drug on the Blood Glucose in Patients With Type 2 Diabetes
NCT02887573	PHASE4	UNKNOWN	Free-residue Nutrients for the Bowel Preparation of Colon Capsule Endoscopy
NCT06826443	PHASE3	NOT_YET_RECRUITING	A Comparative Evaluation of Mosapride Versus Metoclopramide for Enteral Feeding Intolerance in Critically Ill Patients
NCT00742872	PHASE3	TERMINATED	Randomized Trial of Mosapride Versus Placebo in the Treatment of Constipation-Predominant Irritable Bowel Syndrome
NCT01284764	PHASE3	COMPLETED	Efficacy Study of a Low Volume of Water Intake and Mosapride for Endoscopy in Patients With Subtotal Gastrectomy
NCT01411501	PHASE3	COMPLETED	Efficacy and Safety of Acupuncture for Functional Constipation
NCT02831543	PHASE3	UNKNOWN	Clinical Trial to Assess the Efficacy and Safety of Combination Therapy of Motireb 5/100 mg in Functional Dyspepsia Patients.
NCT03477266	PHASE3	COMPLETED	Mouth Dissolving Mosapride Tables Enhance Post Cesarean Gut Recovery
NCT03149393	PHASE1/PHASE2	UNKNOWN	Clinical Study on Post Evaluation After Listing of Qizhi Weitong Granules
NCT05720442	PHASE1/PHASE2	UNKNOWN	Efficacy Assessment of Chinese Herbal Medicine Tangweian Recipe Treating Participants With Diabetic Gastroenteropathy
NCT01781897	PHASE1	UNKNOWN	Electroacupuncture for the Treatment of Functional Constipation
NCT02106130	PHASE1	COMPLETED	A Drug Interaction Study of Mosapride and Rebamipide
NCT06481371	Not specified	NOT_YET_RECRUITING	Zuojin Wan Combined With Rabeprazole or Mosapride for the Treatment of Functional Dyspepsia Combined With Depression
NCT07607249	Not specified	ENROLLING_BY_INVITATION	Clinical Study on the Treatment of Gastrointestinal Dysfunction After Knee Joint Surgery Under General Anesthesia With Floating Needle
NCT03040817	Not specified	UNKNOWN	Cooperative Group for Clinical Research in G-POEM (POP), Jiangsu, China
NCT04493125	Not specified	COMPLETED	Effect of Mosapride Citrate on Gastrointestinal Motility After Laparoscopic Gastrectomy
NCT04905147	Not specified	UNKNOWN	Efficacy of Mosapride on Recovery of Intestinal Motility After Elective Colorectal Cancer Surgery
NCT06156995	Not specified	UNKNOWN	Deep Needling at Zhongliao Point to Stimulate the Sacral Nerve for the Treatment of Slow Transit 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.

16 molecules share ≥1 primary target. Top 16 by shared-target count:

Molecule	Source	Status	Shared targets
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	HTR4
PRUCALOPRIDE	ChEMBL + PubChem	Phase 4 (approved)	HTR4
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	HTR4
CISAPRIDE	ChEMBL	Phase 4 (approved)	HTR4
METOCLOPRAMIDE	ChEMBL	Phase 4 (approved)	HTR4
TROPISETRON	ChEMBL	Phase 4 (approved)	HTR4
SEROTONIN	ChEMBL	Phase 3	HTR4
FELCISETRAG	ChEMBL	Phase 2	HTR4
LITOXETINE	ChEMBL	Phase 2	HTR4
MEBUFOTENIN	ChEMBL	Phase 2	HTR4
PIBOSEROD	ChEMBL	Phase 2	HTR4
PRX-03140	ChEMBL	Phase 2	HTR4
VELUSETRAG	ChEMBL	Phase 2	HTR4
Cyproheptadine	PubChem	Approved	HTR4
Donepezil	PubChem	Approved	HTR4
Haloperidol	PubChem	Approved	HTR4