Pantoprazole

Summary

Pantoprazole (CHEMBL1502) is an approved small-molecule anti-ulcer drug (ATC A02BC02); indicated across 25 conditions including gastroesophageal reflux disease and peptic ulcer disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A02BC02
• Indications: 25 conditions
• Clinical trials: 146
• Chemistry: 383.4 Da · C16H15F2N3O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1502
Name	Pantoprazole
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	4679
ChEBI	CHEBI:7915
ATC	A02BC02
Molecular formula	C16H15F2N3O4S
Molecular weight	383.4
InChIKey	IQPSEEYGBUAQFF-UHFFFAOYSA-N

SMILES: COC1=C(C(=NC=C1)CS(=O)C2=NC3=C(N2)C=C(C=C3)OC(F)F)OC

IUPAC name: 6-(difluoromethoxy)-2-[(3,4-dimethoxy-2-pyridinyl)methylsulfinyl]-1H-benzimidazole

ChEBI definition: A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2.

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

Other ChEBI roles (chemical / environmental): xenobiotic, environmental contaminant.

Also known as: Altopan, BY 1023, BY-1023, BY1023, NSC-759257, Pantocid, Pantoloc, Pantoprazol, Pantoprazole, Pantozol, Protium, Protium i.v.

Parent form; salt/anhydrous children: CHEMBL3989559

Patent coverage: 4,508 distinct patent families (14,689 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 14,534 (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: 19 (assay-derived). Sample: Microtubule-associated protein tau, Lysine-specific demethylase 4E, Prelamin-A/C, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, Multidrug and toxin extrusion protein 2, Potassium-transporting ATPase, Indoleamine 2,3-dioxygenase 2, Alpha-1A adrenergic receptor.

Bioactivity

ChEMBL activities: 9 potent at pChembl ≥ 5 of 25 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ATP4A	6	IC50	1000	nM	CHEMBL_ACT_516848
LMNA	5.9	Potency	1259	nM	CHEMBL_ACT_3646855
SLC22A2	5.82	IC50	1500	nM	CHEMBL_ACT_12636175
SLC47A1	5.55	IC50	2800	nM	CHEMBL_ACT_12636121
SLC47A1	5.55	IC50	2800	nM	CHEMBL_ACT_12636130
FASN	5.39	Ki	4100	nM	CHEMBL_ACT_15194991
ABCG2	5.26	IC50	5500	nM	CHEMBL_ACT_24777444
P15207	5.14	AC50	7300	nM	CHEMBL_ACT_25187812
ABCG2	5	IC50	10000	nM	CHEMBL_ACT_11000952

Target pathways

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

Indications & clinical

Indications

25 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
gastroesophageal reflux disease	3	MONDO:0007186	EFO:0003948
peptic ulcer disease	3	MONDO:0004247	HP:0004398
diabetes mellitus	3	MONDO:0005015	EFO:0000400
congestive heart failure	3	MONDO:0005009	EFO:0000373
Barrett esophagus	3	MONDO:0013662	EFO:0000280
esophageal disorder	3	MONDO:0003749	EFO:0009544
ulcer disease	3	MONDO:0043839	MONDO:0043839
Zollinger-Ellison syndrome	2	MONDO:0019610	EFO:0007549
Helicobacter pylori infectious disease	2	MONDO:0006781	EFO:1000961
pancreatic gastrin-producing neuroendocrine tumor	2	MONDO:0003525	MONDO:0003523
esophagitis	2	MONDO:0001409	HP:0100633
type 1 diabetes mellitus	2	MONDO:0005147	MONDO:0005147
type 2 diabetes mellitus	2	MONDO:0005148	MONDO:0005148
psychotic disorder	2	MONDO:0005485	EFO:0005407
acute coronary syndrome	1	MONDO:0005542	EFO:0005672
aspergillosis	1	MONDO:0005657	EFO:0007157
bacterial infectious disease	1	MONDO:0005113	EFO:0000771
multiple sclerosis	1	MONDO:0005301	MONDO:0005301
duodenal ulcer	1	MONDO:0005412	EFO:0004607
gastric ulcer	1	MONDO:0001126	EFO:0009454

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

Clinical trials

Total trials: 146.

Phase distribution

Phase	Trials
PHASE4	43
PHASE3	30
PHASE1	29
Not specified	29
PHASE2	12
PHASE2/PHASE3	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04728516	PHASE4	RECRUITING	The Effect of Dual Eradication Therapy vs PPI on Gastrointestinal Bleeding in ACS Patients
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
NCT00133770	PHASE4	COMPLETED	Intravenous (IV) Pantoprazole in Erosive Esophagitis
NCT00206050	PHASE4	COMPLETED	Study of Intragastric pH Profile After 5 Days Pantoprazole 40 mg iv Followed by Oral Esomeprazole 40 mg po or Oral Pantoprazole 40 mg po
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
NCT00246909	PHASE4	COMPLETED	Determination of the Minimal Clinically Important Difference After Treatment With Pantoprazole in Patients With Symptoms of Acid Reflux (Gastroesophageal Reflux Disease) (BY1023/M3-340)
NCT00261339	PHASE4	COMPLETED	Determination of a Questionnaire After Treatment With Pantoprazole at Full Dose and Half Dose in Adult Patients With Symptoms of Acid Reflux (Gastroesophageal Reflux Disease) (BY1023/UK-506)
NCT00279123	PHASE4	COMPLETED	Effects of 2 Different Doses of Pantoprazole on Gastric pH and Recurrent Bleeding in Patients Who Bled From Peptic Ulcers
NCT00304421	PHASE4	COMPLETED	Comparison of the Nighttime Effects of Two Different Drugs on Subjects With GERD
NCT00307944	PHASE4	COMPLETED	Study of Pantoprazole for Sleepiness Associated With Acid Reflux and Sleep Apnea
NCT00325676	PHASE4	COMPLETED	Comparison of the Classical Healing Concept With the Complete Remission Concept After Treatment With Pantoprazole in Adult Patients With Erosive GERD (Gastroesophageal Reflux Disease) (BY1023/M3-342)
NCT00410592	PHASE4	COMPLETED	Evaluation of 24-Hour Intragastric pH Using Esomeprazole, Lansoprazole, and Pantoprazole in Hispanic Patients With GERD
NCT00449813	PHASE4	TERMINATED	The CONQUEST-Study. Evaluation of Clinical Endpoints for Treatment-induced Changes in GERD-related Symptoms (BY1023/NL511)
NCT00625274	PHASE4	COMPLETED	A Randomized, Open-Label, Comparative 3-Way Treatment Crossover Study of 24-Hour Intragastric pH Profile of Once Daily Oral Administration of Esomeprazole 40mg, Lansoprazole 30mg, and Pantoprazole 40mg at Steady State in NSAID-Using Patients
NCT00713947	PHASE4	WITHDRAWN	Effectiveness of the Eradication of Helicobacter Pylori and an Inhibitor of Pump With Proton Versus Control
NCT00731601	PHASE4	COMPLETED	Intravenous Proton Pump Inhibitor for Peptic Ulcer Bleeding
NCT00841854	PHASE4	COMPLETED	Comparison of 7-day and 14-day Bismuth Based Quadruple Therapy for Secondary Helicobacter Pylori Eradication
NCT00881413	PHASE4	WITHDRAWN	Esomeprazole Versus Pantoprazole to Prevent Peptic Ulcer Rebleeding
NCT01016717	PHASE4	WITHDRAWN	Clopidogrel Proton-Pump Inhibitors Study
NCT01112852	PHASE4	COMPLETED	EVL (Endoscopic Variceal Ligation) Plus Vasoconstrictor vs.Ligation Plus PPI( Proton Pump Inhibitor) in the Control of Acute Esophageal Variceal Bleeding
NCT01214408	PHASE4	COMPLETED	Effect of Digene Total (Buffered Pantoprazole) on 24 Hour Gastric Potential Hydrogen (pH) in Patients From Acid Peptic Disorder After Single and Repeated Dosing.
NCT01281501	PHASE4	COMPLETED	Symptomatic Relief of Acute Dyspeptic Pain in Emergency Department With Pantoprazole
NCT01373970	PHASE4	TERMINATED	The Clinical Significance of Acid Rebound in Functional Dyspepsia
NCT01493557	PHASE4	COMPLETED	A Prospective, Open Label Study Evaluating Two Management Strategies on Gastrointestinal Symptoms in Patients Newly on Treatment With Pradaxa for the Prevention of Stroke and Systemic Embolism With Non-valvular Atrial Fibrillation
NCT01608750	PHASE4	UNKNOWN	The Efficacy of Pantoprazole Treatment in Patients With Functional Dyspepsia
NCT01735227	PHASE4	UNKNOWN	Omeprazole and Pantoprazole Antiplatelet Effect of Clopidogrel Clinical Trials(OPEN)
NCT01737840	PHASE4	COMPLETED	Comparison of Pantoprazole and Ranitidine in Dyspepsia
NCT01801280	PHASE4	COMPLETED	Influence of Pantoprazole on the Bioavailability of MMF and EC-MPS
NCT02123498	PHASE4	WITHDRAWN	The Study of Eustachian Tube Dysfunction and Laryngopharyngeal Reflux
NCT02213887	PHASE4	WITHDRAWN	Study of the Effects of Pantoprazole on Levels of Prescribed Psychiatric Medications
NCT02432456	PHASE4	COMPLETED	Ketamine Infusion Therapy for the Management of Acute Pain in Adult Rib Fracture Patients
NCT02466919	PHASE4	COMPLETED	Study of Levofloxacin-based Concomitant Therapy for H. Pylori Eradication in Diabetic Patients
NCT02467621	PHASE4	COMPLETED	Stress Ulcer Prophylaxis in the Intensive Care Unit
NCT02718261	PHASE4	COMPLETED	Sup-Icu RENal (SIREN)
NCT02757703	PHASE4	COMPLETED	Vasoactive Drugs in Real World Practice
NCT02788123	PHASE4	TERMINATED	A Study To Assess The Efficacy And Safety Of Bismuth Tripotassium Dicitrate (De-Nol) In Combination With Pantoprazole And Pantoprazole Monotherapy In Treatment Of Subjects With Nonsteroidal Anti-Inflammatory Drugs (NSAID)-Induced Gastropathy
NCT02987920	PHASE4	TERMINATED	Dextromethorphan Use in Multimodal Analgesia Regimens for Total Knee Arthroplasty
NCT03038009	PHASE4	WITHDRAWN	Proton Pump Inhibitor Prevent Dual Antiplatelet Agents Induced Gastrointestinal Ulcer After Coronary Artery Bypass Graft
NCT03545243	PHASE4	COMPLETED	PPI and Microbiome in Healthy Volunteers and Functional Dyspepsia
NCT03908593	PHASE4	UNKNOWN	Proton Pump Inhibitor Preventing Upper Gastrointestinal Injury In Patients On Dual Antiplatelet Therapy After CABG

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 pantoprazole and CYP2C19	DPWG	CYP2C19	yes	yes
Annotation of CPIC Guideline for lansoprazole, omeprazole, pantoprazol	CPIC	CYP2C19	yes	yes

PharmGKB also curates 3 clinical and 40 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).