Tegoprazan

Summary

Tegoprazan (CHEMBL4297583) is a phase-3 clinical-stage small molecule (ATC A02BC09) targeting ATP4A; indicated across 7 conditions including helicobacter pylori infectious disease and gastroesophageal reflux disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: A02BC09
• Targets: 1 (ATP4A)
• Indications: 7 conditions
• Clinical trials: 48
• Chemistry: 387.4 Da · C20H19F2N3O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297583
Name	Tegoprazan
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	23582846
ATC	A02BC09
Molecular formula	C20H19F2N3O3
Molecular weight	387.4
InChIKey	CLIQCDHNPDMGSL-HNNXBMFYSA-N

SMILES: CC1=NC2=C(N1)C=C(C=C2O[C@H]3CCOC4=C3C(=CC(=C4)F)F)C(=O)N(C)C

IUPAC name: 7-[[(4S)-5,7-difluoro-3,4-dihydro-2H-chromen-4-yl]oxy]-N,N,2-trimethyl-3H-benzimidazole-5-carboxamide

Also known as: Cj-12420, Lxi-15028, LXI-15028, Tegoprazan, TEGOPRAZAN

Patent coverage: 115 distinct patent families (198 SureChEMBL compound mentions), from 5 matched compound structure(s). One matched structure accounts for 119 (60%) 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
ATP4A	ATP4A	Inhibition	6.28	0.2%	P20648

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): ATP4A.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
Transport of small molecules	1	ATP4A
Ion transport by P-type ATPases	1	ATP4A
Ion channel transport	1	ATP4A

Dominant GO biological processes

GO term	Targets
intracellular sodium ion homeostasis	1
response to xenobiotic stimulus	1
regulation of proton transport	1
intracellular potassium ion homeostasis	1
monoatomic ion transmembrane transport	1
sodium ion export across plasma membrane	1
pH reduction	1
potassium ion transmembrane transport	1
proton transmembrane transport	1
potassium ion import across plasma membrane	1
monoatomic ion transport	1
potassium ion transport	1
establishment or maintenance of transmembrane electrochemical gradient	1

Indications & clinical

Indications

7 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
Helicobacter pylori infectious disease	3	MONDO:0006781	EFO:1000961
gastroesophageal reflux disease	3	MONDO:0007186	EFO:0003948
peptic ulcer disease	3	MONDO:0004247	HP:0004398
duodenal ulcer	3	MONDO:0005412	EFO:0004607
gastric ulcer	3	MONDO:0001126	EFO:0009454
liver disorder	1	MONDO:0005154	EFO:0001421

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

Clinical trials

Total trials: 48.

Phase distribution

Phase	Trials
PHASE1	24
PHASE3	9
PHASE4	8
Not specified	5
PHASE2/PHASE3	1
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06523764	PHASE4	ACTIVE_NOT_RECRUITING	Efficacy and Safety of Tegoprazan and Minocycline Dual Therapy for Helicobacter Pylori Initial Treatment
NCT06743243	PHASE4	ENROLLING_BY_INVITATION	Effect of Tegoprazan for Elective Surgery Patients Under General Anesthesia
NCT06991348	PHASE4	RECRUITING	Clinical Trial for the Comparative Evaluation of Acid Suppression and Symptom Management of Gastroesophageal Reflux Disease With the Administration of Tegoprazan or Pantoprazole
NCT07242443	PHASE4	NOT_YET_RECRUITING	Tegoprazan Plus Amoxicillin BID vs TID Regimens for H. Pylori Eradication（Frequency Adjusted Same-dose Therapy for H. Pylori）
NCT04309916	PHASE4	COMPLETED	Study to Evaluate the Efficacy and Safety of Tegoprazan in ERD Patients With Nighttime Heartburn and Sleep Disturbance
NCT05647278	PHASE4	COMPLETED	Tegoprazan-Amoxicillin Dual Therapy vs. Bismuth Quadruple Therapy for H. Pylori Infection (TATH-1)
NCT05701540	PHASE4	UNKNOWN	A Study to Evaluate the Efficacy and Safety of Tegoprazan in GERD Patients With Nighttime Heartburn
NCT06318104	PHASE4	UNKNOWN	Efficacy and Safety of a Triple Eradication Scheme for Helicobacter Pylori Based on Tegoprazan vs Esomeprazole
NCT07242456	PHASE2/PHASE3	RECRUITING	Head-to-head Study of Tegoprazan 50 mg BID Plus Amoxicillin 1 g TID vs. Vonoprazan 20 mg BID Plus Amoxicillin 1 g TID for H. Pylori Eradication
NCT02556021	PHASE3	COMPLETED	Study to Evaluate the Safety and Efficacy of CJ-12420 in Patients With Non Erosive Reflux Disease
NCT03317223	PHASE3	COMPLETED	A Phase 3 Study to Evaluate the Efficacy and Safety of Triple Therapy With CJ-12420 in H. Pylori Positive Patients
NCT03498456	PHASE3	COMPLETED	Triple Therapy With Tegoprazan in H. Pylori Positive Patients
NCT03591653	PHASE3	COMPLETED	A Multi-center, Randomized, Double-blind, Parallel-group, Placebo Controlled Phase III Study to Evaluate the Efficacy and Safety of LXI-15028 in Non-erosive Reflux Disease in Chinese Patients for 4 Weeks
NCT03615677	PHASE3	COMPLETED	Efficacy and Safety of LXI-15028 Comparing With Esomeprazole in the Treatment of Erosive Esophagitis
NCT04128917	PHASE3	COMPLETED	Triple Therapy With Tegoprazan in H. Pylori Positive Patients_PILOT
NCT04840550	PHASE3	UNKNOWN	Study to Evaluate the Safety, Efficacy of Tegoprazan for the Prevention of PUD in Patients on Treatment With NSAIDs
NCT05577468	PHASE3	COMPLETED	Efficacy and Safety of Tegoprazan Versus Esomeprazole-containing Bismuth Quadruple Therapy for Eradication of Helicobacter Pylori
NCT05871398	PHASE3	COMPLETED	The Efficacy of Potassium-competitive Acid Blocker in Patients With Laryngopharyngeal Reflux Disease
NCT02028663	PHASE2	COMPLETED	Study to Evaluate the Safety and Efficacy of CJ-12420 in Patients With Erosive Esophagitis
NCT06561542	PHASE1	RECRUITING	A Phase I Study of LX22001 for Injection in Healthy Subjects
NCT07277712	PHASE1	NOT_YET_RECRUITING	A Study to Evaluate the Pharmacokinetics and Food-effect of IN-M00002 Tablet in Healthy Adult Volunteers
NCT01473173	PHASE1	COMPLETED	Safety, Tolerability, PK, PD of Escalating Single and Multiple Oral Doses of CJ-12420 in Healthy Male Subjects
NCT01830309	PHASE1	COMPLETED	Food-Effect on PK and PD of Single Oral Dose of CJ-12420 in Healthy Male Subjects
NCT02052336	PHASE1	COMPLETED	Drug-Drug Interaction Study Between CJ-12420 and Clarithromycin in Healthy Male Subjects
NCT03009760	PHASE1	COMPLETED	To Investigate Pharmacokinetics and Pharmacodynamics of CJ-12420 After Single and Multiple Dose Administration
NCT03011996	PHASE1	COMPLETED	To Investigate PK and PD of CJ-12420, Clarithromycin, Amoxicillin After Multiple Dose Administration
NCT03043521	PHASE1	COMPLETED	Pharmacodynamic Properties of CJ-12420 on Evening Dosing
NCT03378284	PHASE1	COMPLETED	A Study to Evaluate Safety, Tolerability, and PD of Tegoprazan on Healthy Male Volunteers
NCT03458650	PHASE1	COMPLETED	A Phase I Study of LuoXin Innovate (LXI-15028) in Healthy Chinese Subjects to Evaluate the Pharmacokinetics, Safety and Tolerability.
NCT03530228	PHASE1	UNKNOWN	A Phase 1 Study of Tegoprazan on Healthy Male Volunteers
NCT03814642	PHASE1	COMPLETED	Effect of Tegoprazan on Pharmacodynamics of Clopidogrel in Healthy Male Participants
NCT03863938	PHASE1	COMPLETED	Food-Effect on PK and PD of Single Oral Dose of Tegoprazan in Healthy Male Subjects
NCT04066257	PHASE1	COMPLETED	Evaluate the PK of Multiple Oral Doses of Tegoprazan, Metronidazole, Tetracycline and Bismuth in Healthy Volunteers
NCT04171687	PHASE1	COMPLETED	Effect of Tegoprazan or RAPA113 on Pharmacodynamics/Pharmacokinetics of Clopidogrel in Healthy Male Volunteers
NCT04221321	PHASE1	COMPLETED	Effect of Tegoprazan or RAPA114 on Pharmacokinetic of Atorvastatin in Healthy Adult Volunteers
NCT04231136	PHASE1	COMPLETED	Study to Evaluate the Pharmacodynamics After Single Oral Dosing of Tegoprazan, EAPA115 and RAPA115 in Healthy Volunteers
NCT04494269	PHASE1	UNKNOWN	A Study to Evaluate Pharmacokinetics and Safety of Tegoprazan in Subjects With Hepatic Impairment and Healthy Controls
NCT04568772	PHASE1	COMPLETED	Study to Evaluate the Influence of Tegoprazan on the Pharmacokinetics of Proguanil in Healthy Volunteers
NCT04639804	PHASE1	COMPLETED	Pharmacokinetic Interaction Between Tegoprazan and NSAIDs After Multiple Oral Dosing in Healthy Male Volunteers
NCT05723510	PHASE1	COMPLETED	PK and PD Interaction Between Tegoprazan and NOACs After Multiple Oral Dosing in Healthy Volunteers

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

5 molecules share ≥1 primary target. Top 5 by shared-target count:

Molecule	Source	Status	Shared targets
CIMETIDINE	ChEMBL + PubChem	Phase 4 (approved)	ATP4A
LANSOPRAZOLE	ChEMBL + PubChem	Phase 4 (approved)	ATP4A
PANTOPRAZOLE	ChEMBL + PubChem	Phase 4 (approved)	ATP4A
OMEPRAZOLE	ChEMBL	Phase 4 (approved)	ATP4A
RANITIDINE	ChEMBL	Phase 4 (approved)	ATP4A