Prucalopride
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Also known as PrucalopridaR-093877R093877ResolorSID174006285SID170466188Prucalopride hydrochlorideÊPrucalopride hydrochlorideÂ
Summary
Prucalopride (CHEMBL117287) is an approved small molecule (ATC A06AX05) targeting HTR4; indicated across 8 conditions including constipation disorder and intestinal pseudo-obstruction.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: A06AX05
- Targets: 1 (HTR4)
- Indications: 8 conditions
- Clinical trials: 63
- Chemistry: 367.9 Da · C18H26ClN3O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL117287 |
| Name | Prucalopride |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 3052762 |
| ATC | A06AX05 |
| Molecular formula | C18H26ClN3O3 |
| Molecular weight | 367.9 |
| InChIKey | ZPMNHBXQOOVQJL-UHFFFAOYSA-N |
SMILES: COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
IUPAC name: 4-amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide
Also known as: Prucaloprida, Prucalopride, R-093877, R093877, Resolor, prucalopride, PRUCALOPRIDE, SID174006285, SID170466188, Prucalopride hydrochlorideÊ, Prucalopride hydrochlorideÂ
Parent form; salt/anhydrous children: CHEMBL2105748, CHEMBL4757628, CHEMBL5199178
Patent coverage: 648 distinct patent families (2,516 SureChEMBL compound mentions), from 1 matched compound structure(s). 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 | Partial agonist | 8.6 | 0% | Q13639 |
Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: 5-hydroxytryptamine receptor 4, 5-hydroxytryptamine receptor 3A, Alpha-2C adrenergic receptor, 5-hydroxytryptamine receptor 1A, Acetylcholinesterase, Prostaglandin G/H synthase 1, Alpha-1A adrenergic receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, 5-hydroxytryptamine receptor 4.
Bioactivity
ChEMBL activities: 14 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HTR4 | 8.6 | Ki | 2.51 | nM | CHEMBL_ACT_2411225 |
| HTR4 | 8.4 | EC50 | 4 | nM | CHEMBL_ACT_29252073 |
| HTR4 | 8.28 | EC50 | 5.2 | nM | CHEMBL_ACT_16400107 |
| HTR4 | 8.28 | EC50 | 5.2 | nM | CHEMBL_ACT_18504166 |
| HTR4 | 8.12 | Ki | 7.5 | nM | CHEMBL_ACT_652616 |
| Q62758 | 7.58 | EC50 | 26 | nM | CHEMBL_ACT_16401322 |
| HTR4 | 7.58 | EC50 | 26 | nM | CHEMBL_ACT_18504543 |
| Q62758 | 7.58 | EC50 | 26 | nM | CHEMBL_ACT_24973825 |
| HTR4 | 7.36 | Ki | 44.1 | nM | CHEMBL_ACT_27216734 |
| HTR4 | 6.96 | Ki | 110 | nM | CHEMBL_ACT_652618 |
| HTR4 | 6.75 | Ki | 180.1 | nM | CHEMBL_ACT_29252151 |
| HTR3A | 5.4 | Ki | 3981 | nM | CHEMBL_ACT_2411224 |
| KCNH2 | 5.39 | IC50 | 4100 | nM | CHEMBL_ACT_29252064 |
| HTR1A | 5.21 | AC50 | 6100 | nM | CHEMBL_ACT_25165019 |
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 (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 |
| intestinal pseudo-obstruction | 3 | MONDO:0002803 | HP:0002590 |
| irritable bowel syndrome | 2 | MONDO:0005052 | EFO:0000555 |
| ileus | 2 | MONDO:0004567 | MONDO:0004567 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
| dyspepsia | 1 | MONDO:0002268 | EFO:0008533 |
| depressive disorder | 0 | MONDO:0002050 | MONDO:0002050 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 63.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 20 |
| PHASE4 | 10 |
| PHASE2 | 9 |
| PHASE1 | 9 |
| Not specified | 9 |
| PHASE1/PHASE2 | 3 |
| PHASE2/PHASE3 | 2 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05455359 | PHASE4 | RECRUITING | Gastrointestinal Dysmotility on Aspiration Risk |
| NCT01424228 | PHASE4 | COMPLETED | Evaluation of Long-term Prucalopride Treatment With Chronic Constipation in Subjects Aged ≥ 18 Years |
| NCT01707667 | PHASE4 | COMPLETED | Study to Investigate Prucalopride vs. Polyethylene Glycol 3350 on Colon Activity |
| NCT02228616 | PHASE4 | COMPLETED | Efficacy and Safety of Prucalopride in Combination With Polyethylene Glycol or Lactulose in Women With Chronic Constipation |
| NCT02425774 | PHASE4 | COMPLETED | Anti-inflammatory Effect of Pre-operative Stimulation of the Cholinergic Anti-Inflammatory Pathway |
| NCT02510976 | PHASE4 | TERMINATED | Prucalopride Versus Placebo in Gastroparesis |
| NCT02806206 | PHASE4 | UNKNOWN | Prucalopride Prior to Small Bowel Capsule Endoscopy |
| NCT03279341 | PHASE4 | COMPLETED | Effect of PEG, Bisacodyl and Prucalopride on Colonic Motility in Healthy Subjects |
| NCT03676374 | PHASE4 | UNKNOWN | Prucalopride Treatment for Refractory Gastro-esophageal Reflux Disease |
| NCT04985669 | PHASE4 | UNKNOWN | Study of Comparative Effectiveness of Prucalopride and Lubiprostone in Constipation Predominant Irritable Bowel Syndrome |
| NCT06816407 | PHASE3 | RECRUITING | Impact of Varying Doses of Prucalopride on Improving Gut Function Recovery After Elective Colorectal Surgery |
| NCT00483886 | PHASE3 | COMPLETED | Efficacy and Safety Study of Prucalopride for the Treatment of Chronic Constipation |
| NCT00485940 | PHASE3 | COMPLETED | Efficacy and Safety Study of Prucalopride for the Treatment of Patients With Chronic Constipation |
| NCT00487422 | PHASE3 | COMPLETED | Efficacy and Safety Study of Prucalopride for the Treatment of Elderly Patients With Chronic Constipation |
| NCT00488137 | PHASE3 | COMPLETED | Efficacy and Safety Study of Prucalopride to Treat Chronic Constipation |
| NCT00577018 | PHASE3 | COMPLETED | Efficacy and Safety Study of the Effect of Dose-Titration of Prucalopride for The Treatment of Chronic Constipation |
| NCT00598338 | PHASE3 | COMPLETED | Efficacy and Safety Study of Prucalopride for the Re-Treatment of Chronic Constipation |
| NCT00987844 | PHASE3 | COMPLETED | Study to Evaluate Long-Term Safety, Tolerability, and Satisfaction With Prucalopride in Chronic Constipation |
| NCT01070615 | PHASE3 | COMPLETED | Study to Evaluate Long-Term Tolerability and Safety of Oral Prucalopride in Chronic Constipation |
| NCT01116206 | PHASE3 | COMPLETED | An Efficacy and Safety Study of Prucalopride in Participants With Chronic Constipation |
| NCT01117051 | PHASE3 | TERMINATED | Prucalopride Effects on Subjects With Chronic Non-cancer Pain Suffering From Opioid Induced Constipation |
| NCT01147926 | PHASE3 | COMPLETED | Evaluation of Prucalopride in Male Subjects With Chronic Constipation. |
| NCT01251822 | PHASE3 | COMPLETED | Comparator Study of PEG 3350 Versus Prucalopride in Females With Chronic Constipation |
| NCT01330381 | PHASE3 | COMPLETED | Prucalopride in Pediatric Subjects With Functional Constipation |
| NCT01655095 | PHASE3 | COMPLETED | Improving Bowel Preparation for the Colon Capsule |
| NCT01864915 | PHASE3 | COMPLETED | Prucalopride + Prucalopride Booster vs. Prucalopride + Picosalax Booster for the Colon Capsule |
| NCT02031081 | PHASE2/PHASE3 | COMPLETED | Prucalopride Versus Placebo in Gastroparesis |
| NCT02947269 | PHASE3 | COMPLETED | Prucalopride in Postoperative Ileus |
| NCT04190173 | PHASE3 | UNKNOWN | Efficacy of PRUcalopride in Critically Ill Patients With Paralytic ILeus |
| NCT04757493 | PHASE2/PHASE3 | UNKNOWN | The Effects of Prucalopride in Patients With Constipation Predominant Irritable Bowel Syndrome |
| NCT04759833 | PHASE3 | TERMINATED | A Study of Prucalopride For Functional Constipation in Children and Teenagers |
| NCT05726097 | PHASE3 | COMPLETED | Bowel Preparation Regimen for Colon Capsule Endoscopy Procedure |
| NCT00575614 | PHASE2 | COMPLETED | Prucalopride in Patients With Chronic Idiopathic Constipation |
| NCT00576511 | PHASE2 | COMPLETED | Effect of Prucalopride in Patients With Severe Chronic Idiopathic Constipation |
| NCT00596596 | PHASE2 | COMPLETED | Trial to Evaluate the Efficacy and Safety of R093877 in Patients With Chronic Idiopathic Constipation |
| NCT00617513 | PHASE2 | COMPLETED | Efficacy and Safety Study of Prucalopride for the Treatment of Chronic Constipation |
| NCT00627692 | PHASE2 | COMPLETED | Evaluation of the Safety and Tolerability of Prucalopride in Constipated Elderly Subjects Living in a Nursing Facility |
| NCT00631813 | PHASE2 | COMPLETED | Efficacy and Safety Study of Prucalopride for the Treatment of Chronic Constipation |
| NCT02004652 | PHASE2 | COMPLETED | Prucalopride for Postoperative Ileus in Patients Undergoing Gastrointestinal Surgery |
| NCT02538367 | PHASE1/PHASE2 | COMPLETED | Phase 1/2a Trial of YH12852 in Healthy Subjects and Patients With Functional 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.
15 molecules share ≥1 primary target. Top 15 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| IMIPRAMINE | 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 |
Related Atlas pages
- Genes: HTR4
- Diseases: constipation disorder, intestinal pseudo-obstruction
- Drugs: Imipramine, Tegaserod, Cisapride, Metoclopramide, Tropisetron, Serotonin, Cyproheptadine, Donepezil, Haloperidol