Rabeprazole

Summary

Rabeprazole (CHEMBL1219) is an approved small-molecule EC 3.6.3.10 (H+/K+-exchanging ATPase) inhibitor (ATC A02BC04); indicated across 13 conditions including gastroesophageal reflux disease and peptic ulcer disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A02BC04 (+1 more)
• Indications: 13 conditions
• Clinical trials: 137
• Chemistry: 359.4 Da · C18H21N3O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1219
Name	Rabeprazole
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5029
ChEBI	CHEBI:8768
ATC	A02BC04, A02BC54
Molecular formula	C18H21N3O3S
Molecular weight	359.4
InChIKey	YREYEVIYCVEVJK-UHFFFAOYSA-N

SMILES: CC1=C(C=CN=C1CS(=O)C2=NC3=CC=CC=C3N2)OCCCOC

IUPAC name: 2-[[4-(3-methoxypropoxy)-3-methyl-2-pyridinyl]methylsulfinyl]-1H-benzimidazole

Pharmacological roles (ChEBI): EC 3.6.3.10 (H+/K+-exchanging ATPase) inhibitor, anti-ulcer drug.

Also known as: E-3810 (PPI), E3810, Eraloc, Ly-307640, LY307640, Pariprazole, Rabeprazol, Rabeprazole, SID29215495, rabeprazole, RABEPRAZOLE, SID174007154

Parent form; salt/anhydrous children: CHEMBL1200930, CHEMBL4303515

Patent coverage: 3,764 distinct patent families (12,441 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 12,285 (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

Broader ChEMBL bioactivity targets: 29 (assay-derived). Sample: Microtubule-associated protein tau, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Insulin-degrading enzyme, 5-hydroxytryptamine receptor 2B, 5-hydroxytryptamine receptor 3A, Alpha-2B adrenergic receptor, Thromboxane A2 receptor, 5-hydroxytryptamine receptor 1A.

Bioactivity

ChEMBL activities: 23 potent at pChembl ≥ 5 of 37 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	7.55	Potency	28.2	nM	CHEMBL_ACT_3642314
P14916	6.54	IC50	290	nM	CHEMBL_ACT_19445489
WDR5	6.31	IC50	490	nM	CHEMBL_ACT_22463501
PTGS1	6.15	AC50	710	nM	CHEMBL_ACT_25205504
ADRA2B	6.1	Ki	793	nM	CHEMBL_ACT_7813161
DRD3	6.1	Ki	790	nM	CHEMBL_ACT_7815243
ADRA2B	5.76	IC50	1737	nM	CHEMBL_ACT_7813160
ADORA3	5.74	Ki	1820	nM	CHEMBL_ACT_7813149
ADORA3	5.66	AC50	2200	nM	CHEMBL_ACT_25134418
DRD3	5.63	IC50	2326	nM	CHEMBL_ACT_7815242
SARM1	5.5	IC50	3200	nM	CHEMBL_ACT_19361230
ADORA3	5.49	IC50	3219	nM	CHEMBL_ACT_7813148
SARM1	5.48	IC50	3300	nM	CHEMBL_ACT_19361224
ENGASE	5.35	IC50	4470	nM	CHEMBL_ACT_18160425
ADRA1A	5.3	AC50	4982	nM	CHEMBL_ACT_25138470
KCNH2	5.27	AC50	5329	nM	CHEMBL_ACT_25118165
FASN	5.23	Ki	5900	nM	CHEMBL_ACT_15194993
HTR3A	5.22	AC50	6000	nM	CHEMBL_ACT_25149334
ALDH1A1	5.22	Potency	5967	nM	CHEMBL_ACT_4165599
OPRM1	5.1	AC50	7930	nM	CHEMBL_ACT_25158455
PDE4D	5.1	AC50	8000	nM	CHEMBL_ACT_25185539
ABCG2	5.07	IC50	8500	nM	CHEMBL_ACT_24777443
MAPT	5	Potency	10000	nM	CHEMBL_ACT_4041807

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

13 indications (2 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
gastroesophageal reflux disease	4	MONDO:0007186	EFO:0003948
peptic ulcer disease	4	MONDO:0004247	HP:0004398
duodenal ulcer	3	MONDO:0005412	EFO:0004607
Helicobacter pylori infectious disease	3	MONDO:0006781	EFO:1000961
dyspepsia	2	MONDO:0002268	EFO:0008533
infectious disease	1	MONDO:0005550	EFO:0005741
lymphoid neoplasm	1	MONDO:0005157	EFO:0001642
amyotrophic lateral sclerosis	1	MONDO:0004976	MONDO:0004976
lymphoma	1	MONDO:0005062	EFO:0000574
neoplasm	1	MONDO:0005070	MONDO:0004992
intrahepatic cholangiocarcinoma	1	MONDO:0003210	EFO:1001961

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

Clinical trials

Total trials: 137.

Phase distribution

Phase	Trials
PHASE1	61
PHASE4	32
Not specified	15
PHASE3	14
PHASE2	7
PHASE2/PHASE3	6
PHASE1/PHASE2	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05061732	PHASE4	RECRUITING	Helicobacter Pylori Eradication and Follow-up
NCT07122024	PHASE4	RECRUITING	Efficacy and Safety of Keverprazan-amoxicillin Dual Therapy for Helicobacter Pylori First-line Treatment
NCT07471867	PHASE4	RECRUITING	Effect of ZaStaprazan on Platelet Reactivity of Clopidogrel After PercuTaneous CoronAry InteRvention
NCT00220857	PHASE4	COMPLETED	Rabeprazole Protection of Aspirin Induced Gastric Damage.
NCT00237367	PHASE4	COMPLETED	A Study of Rabeprazole and Pantoprazole on Stomach Acid and Esophageal Acid Exposure in Patients With Gastroesophageal Reflux Disease (GERD) and a History of Nighttime Heartburn
NCT00251732	PHASE4	COMPLETED	Role of Pain Modulation in GERD Patients Who Failed Standard Dose Proton Pump Inhibitors (PPI)
NCT00287391	PHASE4	COMPLETED	Sleep Disorders and Gastroesophageal Reflux Disease (GERD)
NCT00304421	PHASE4	COMPLETED	Comparison of the Nighttime Effects of Two Different Drugs on Subjects With GERD
NCT00354757	PHASE4	COMPLETED	CYP2C19 Genetic Polymorphism on the Accuracy of Proton-Pump Inhibitor Testing
NCT00464308	PHASE4	COMPLETED	A Study to Compare the Number of Patients With Gastro-Oesophageal Reflux Disease (GORD) Achieving Heartburn and Regurgitation Symptom Resolution After Treatment With Either Rabeprazole Sodium 20mg, Esomeprazole 20mg or Esomeprazole 40mg
NCT00838682	PHASE4	TERMINATED	Effect of High-dose Oral Rabeprazole on Recurrent Bleeding After the Endoscopic Treatment of Bleeding Peptic Ulcers
NCT00844675	PHASE4	COMPLETED	Effects of Oral Rabeprazole on the Prevention of Ulcer Bleeding Following Endoscopic Mucosal Resection
NCT00861640	PHASE4	UNKNOWN	Comparison of Oral Rabeprazole vs. iv Omeprazole in Mild to Moderate Nonvariceal Upper Gastrointestinal Bleeding
NCT01008696	PHASE4	COMPLETED	An Efficacy Study to Compare the Treatment Effects of Rabeprazole and Lansoprazole Depending on the Genotyping of CYP2C19 in Treating Reflux Esophagitis
NCT01219764	PHASE4	COMPLETED	A Trial of Standard vs Half Dose Rabeprazole, Clarithromycin, Metronidazole and Amoxicillin in the Treatment of Helicobacter Pylori Infection
NCT01922765	PHASE4	UNKNOWN	Concomitant Therapy of H. Pylori
NCT02638584	PHASE4	COMPLETED	Effects of Ilaprazole on Ulcer Healing Rate and Prevention of Gastrointestinal Bleeding in the Patients Undergone ESD.
NCT02986685	PHASE4	WITHDRAWN	Trimebutine Maleate Combined With Rabeprazole in Patients With Grade A or B Reflux Esophagitis Whose Symptoms Refractory to Rabeprazole
NCT03134378	PHASE4	UNKNOWN	10 vs 14 Days Triple Therapy : H.Pylori Infection Eradication
NCT03521726	PHASE4	COMPLETED	Intraluminal Amoxicillin Powder Monotherapy for Helicobacter Pylori Infection
NCT03616405	PHASE4	UNKNOWN	Pilot Study of a 14-day Modified Sequential Therapy for Helicobacter Pylori Infection
NCT03658733	PHASE4	UNKNOWN	A Pilot Study of a 14-day Modified Sequential Therapy for Helicobacter Pylori Infection
NCT03908619	PHASE4	UNKNOWN	A RCT of Triple Therapy With Proton Pump Inhibitor vs Vonoprazan for Helicobacter Pylori Gastritis
NCT04132479	PHASE4	COMPLETED	The Epidemiology and Optimal Treatment of Helicobacter Pylori in Myanmar
NCT04667299	PHASE4	UNKNOWN	Bismuth-Metronidazole Triple Therapy for H. Pylori First-line Treatment
NCT04697186	PHASE4	COMPLETED	Helicobacter Pylori Eradication With Berberine Plus Amoxicillin Triple Therapy Versus Bismuth-containing Quadruple Therapy
NCT05014334	PHASE4	COMPLETED	Study on The Efficacy and Safety of Berberine-containing Triple Therapy in Helicobacter Pylori First-Line Eradication
NCT05014685	PHASE4	UNKNOWN	PPI-amoxicillin for H. Pylori Treatment
NCT05018923	PHASE4	UNKNOWN	Tetracycline Versus Doxycycline for HP Rescue Therapy
NCT05023577	PHASE4	UNKNOWN	Antibiotic Combination for H. Pylori Eradication in Penicillin-allergic Patients
NCT05419674	PHASE4	UNKNOWN	Efficacy and Safety of Dual Therapy as First-line Treatment for Hp Infection
NCT05718609	PHASE4	UNKNOWN	Efficacy of Therapy Based on Fecal Molecular Antimicrobial Susceptibility Tests for Helicobacter Pylori Infection
NCT07010107	PHASE3	RECRUITING	A Clinical Trial of Anaprazole for Treating Reflux Esophagitis.
NCT07608536	PHASE3	NOT_YET_RECRUITING	Comparison of Rabeprazole and Vonoprazan in the Prevention of Post-endoscopic Variceal Ligation Ulcer in Patients With Cirrhosis
NCT00165646	PHASE3	COMPLETED	A Comparative Study on the Efficacy and Safety of E3810 in Patients With Non-erosive Gastroesophageal Reflux Disease
NCT00197418	PHASE2/PHASE3	UNKNOWN	Second Line Therapy for the Cure of Helicobacter Pylori (H. Pylori) Infection
NCT00214552	PHASE3	COMPLETED	Evaluate the Effects on Asthma Control of Rabeprazole Given Twice Daily in Subjects With Asthma.
NCT00236392	PHASE3	COMPLETED	A Study of Efficacy and Safety of On-demand Maintenance Therapy With Rabeprazole in Patients With Non-erosive Reflux Disease (NERD)
NCT00539240	PHASE2/PHASE3	COMPLETED	Role of Pain Modulation in GERD Patients Who Failed Standard Dose PPI
NCT00553449	PHASE3	COMPLETED	Open Label Study Evaluating Different Dosing Regimens of Rabeprazole in Gastro-esophageal Reflux Disease (GERD) Patients With Night-time Heartburn Symptoms.

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (2) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for rabeprazole and CYP2C19	DPWG	CYP2C19
Annotation of CPIC Guideline for esomeprazole, rabeprazole and CYP2C19	CPIC	CYP2C19

PharmGKB also curates 3 clinical and 86 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).