Lansoprazole

Summary

Lansoprazole (CHEMBL480) is an approved small-molecule EC 3.6.3.10 (H+/K+-exchanging ATPase) inhibitor (ATC A02BC03); 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: A02BC03 (+1 more)
• Indications: 25 conditions
• Clinical trials: 158
• Chemistry: 369.4 Da · C16H14F3N3O2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL480
Name	Lansoprazole
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3883
ChEBI	CHEBI:6375
ATC	A02BC03, A02BC53
Molecular formula	C16H14F3N3O2S
Molecular weight	369.4
InChIKey	MJIHNNLFOKEZEW-UHFFFAOYSA-N

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

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

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

Also known as: A-65006, AG-1749, Agopton, Lansoprazol, Lansoprazole, Lansoprazole component of prevpac, Lansox, Lanzoprazole, Lanzor, Limpidex, NSC-758638, Ogast

Patent coverage: 7,635 distinct patent families (24,317 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 23,447 (96%) 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: 52 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Indoleamine 2,3-dioxygenase 1, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Fructose-bisphosphate aldolase, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], NPC intracellular cholesterol transporter 1.

Bioactivity

ChEMBL activities: 46 potent at pChembl ≥ 5 of 112 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
MAPT	8.6	Ki	2.5	nM	CHEMBL_ACT_12177205
P08482	7.25	Potency	56.2	nM	CHEMBL_ACT_4803410
CYP2C19	7	Potency	100	nM	CHEMBL_ACT_4014665
CYP2C19	7	AC50	100	nM	CHEMBL_ACT_6026387
LMNA	6.9	Potency	125.9	nM	CHEMBL_ACT_3653133
TSHR	6.9	Potency	125.9	nM	CHEMBL_ACT_3935530
TSHR	6.9	Potency	125.9	nM	CHEMBL_ACT_4699401
CYP2C19	6.47	IC50	336.7	nM	CHEMBL_ACT_7755078
P0DTD1	6.41	IC50	390	nM	CHEMBL_ACT_19964199
ATP4A	6.4	IC50	398.1	nM	CHEMBL_ACT_543277
PHOSPHO1	6.36	IC50	434	nM	CHEMBL_ACT_5566604
HSD17B10	6.3	Potency	501.2	nM	CHEMBL_ACT_4829732
PPIA	6.12	IC50	760	nM	CHEMBL_ACT_29171067
CYP2C19	5.9	Potency	1259	nM	CHEMBL_ACT_4015566
P0DTD1	5.8	IC50	1600	nM	CHEMBL_ACT_19964217
FASN	5.77	Ki	1700	nM	CHEMBL_ACT_24721721
HSD17B10	5.7	Potency	1995	nM	CHEMBL_ACT_4833774
DRD4	5.68	AC50	2107	nM	CHEMBL_ACT_25127497
HTR3A	5.64	AC50	2300	nM	CHEMBL_ACT_25149751
RAB9A	5.64	Potency	2311	nM	CHEMBL_ACT_3857597
NPC1	5.64	Potency	2311	nM	CHEMBL_ACT_4752430
NPC1	5.55	Potency	2818	nM	CHEMBL_ACT_4740172
CYP2D6	5.54	IC50	2900	nM	CHEMBL_ACT_15445899
RAB9A	5.5	Potency	3162	nM	CHEMBL_ACT_3860412
TBXA2R	5.46	AC50	3460	nM	CHEMBL_ACT_25155749
OPRM1	5.4	AC50	4000	nM	CHEMBL_ACT_25157830
RAB9A	5.4	Potency	3981	nM	CHEMBL_ACT_3835241
NPC1	5.4	Potency	3981	nM	CHEMBL_ACT_4732275
OPRM1	5.38	AC50	4200	nM	CHEMBL_ACT_25147302
OPRK1	5.31	AC50	4882	nM	CHEMBL_ACT_25130016

Target pathways

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

Indications & clinical

Indications

25 indications (5 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	4	MONDO:0005412	EFO:0004607
gastric ulcer	4	MONDO:0001126	EFO:0009454
peptic esophagitis	3	MONDO:0006896	EFO:1001095
gout	3	MONDO:0005393	EFO:0004274
Helicobacter pylori infectious disease	3	MONDO:0006781	EFO:1000961
lymphoma	3	MONDO:0005062	EFO:0000574
breast neoplasm	3	MONDO:0021100	MONDO:0007254
gastritis	3	MONDO:0004966	EFO:0000217
idiopathic pulmonary fibrosis	3	MONDO:0800504	EFO:0000768
type 1 diabetes mellitus	3	MONDO:0005147	MONDO:0005147
osteoarthritis	3	MONDO:0005178	MONDO:0005178
B-cell chronic lymphocytic leukemia	2	MONDO:0004948	EFO:0000095
eosinophilic esophagitis	2	MONDO:0005361	EFO:0004232
pseudomyxoma peritonei	2	MONDO:0017048	EFO:0007456
rectal cancer	2	MONDO:0006519	EFO:1000657
endometrium neoplasm	2	MONDO:0021251	MONDO:0011962
neoplasm	1	MONDO:0005070	EFO:0000616
cystic fibrosis	1	MONDO:0009061	MONDO:0009061

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

Clinical trials

Total trials: 158.

Phase distribution

Phase	Trials
PHASE4	49
PHASE3	42
PHASE1	26
Not specified	23
PHASE2	13
PHASE2/PHASE3	2
PHASE1/PHASE2	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07533266	PHASE4	NOT_YET_RECRUITING	Study to Evaluate the Efficacy and Safety of Fexuprazan in Prevention of NSAIDs Induced Peptic Ulcer
NCT00204373	PHASE4	COMPLETED	Treatment of Zollinger-Ellison Syndrome With Prevacid
NCT00220909	PHASE4	TERMINATED	Lansoprazole Preventing Gastroduodenal Stress Ulcerations
NCT00230516	PHASE4	COMPLETED	Study of 24-hour Intragastric pH Profiles of Esomeprazole 40 mg and Lansoprazole 30 mg in Healthy Volunteer Subjects
NCT00239551	PHASE4	COMPLETED	Effect of Prevacid on Prostaglandin Levels in Patient With Stress Ulcer
NCT00299845	PHASE4	WITHDRAWN	Randomized Trial for Pharmacogenomics-based Proton Pump Inhibitor Therapy in Children
NCT00352261	PHASE4	COMPLETED	An Open Label pH Comparison of Esomeprazole and Lansoprazole in Barrett’s Esophagus Patients
NCT00369265	PHASE4	TERMINATED	Safety and Efficacy of Lansoprazole 30mg Twice Daily in Treatment of Laryngitis Associated With Gastroesophageal Reflux
NCT00410592	PHASE4	COMPLETED	Evaluation of 24-Hour Intragastric pH Using Esomeprazole, Lansoprazole, and Pantoprazole in Hispanic Patients With GERD
NCT00442013	PHASE4	COMPLETED	Lansoprazole to Treat Children With Asthma
NCT00444145	PHASE4	COMPLETED	Do Laryngeal Tissue Changes in Patients Suspected of Having Laryngopharyngeal Reflux Predict Response to Treatment?
NCT00467571	PHASE4	COMPLETED	Helicobacter Pylori Infection in Children With Chronic Idiopathic Thrombocytopenic Purpura
NCT00472186	PHASE4	TERMINATED	The Effects of Reducing Stomach Acid on Post-tonsillectomy Pain
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
NCT00637416	PHASE4	TERMINATED	Dietary Control Alone Versus Dietary Control Plus Use of Proton Pump Inhibitors to Treat Pediatric Hoarseness
NCT00637845	PHASE4	COMPLETED	Study Comparing Esomeprazole Magnesium 40mg Once Daily Versus Lansoprazole 30 mg Twice Daily in Symptom Control of Subjects With Persistent Gastrooesophageal Reflux Disease (GERD)
NCT00641602	PHASE4	COMPLETED	A Multicenter, Randomized, Double Blind, Double Dummy, Parallel-Group Efficacy Study Comparing 8 Weeks of Treatment With Esomeprazole Magnesium (40mg qd) to Lansoprazole (30mg qd) for the Healing of Erosive Esophagitis in Patients With Moderate or Severe Erosive Esophagitis
NCT00644735	PHASE4	COMPLETED	Multicenter, Randomized, Double-Blind, Double-Dummy, Parallel-Group Comparison of the Remission Rates of Once Daily Treatment With Esomeprazole 20mg and Lansoprazole 15mg for 6 Months in Patients Whose EE Has Been Healed
NCT00663897	PHASE4	COMPLETED	Lansoprazole Versus Mosapride for Functional Dyspepsia
NCT00825630	PHASE4	COMPLETED	13-C Urea Breath Test Using BreathID System and PPIs (Proton Pump Inhibitors)
NCT00903448	PHASE4	COMPLETED	Comparison of Prilosec Over-the-counter (OTC)® Versus Prevacid® for Gastric Acid Suppression
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
NCT01040455	PHASE4	TERMINATED	Lansoprazole for Subgroups of Functional Dyspepsia
NCT01082029	PHASE4	COMPLETED	Study of Anti-reflux Medication as a Potential Treatment for Glue Ear in Children
NCT01123031	PHASE4	WITHDRAWN	Oral vs Intravenous and Proton Pump Inhibitor (PPI）for Peptic Ulcer Bleeding (PUB)
NCT01135368	PHASE4	COMPLETED	Safety and Efficacy of Lansoprazole in Patients With Reflux Disease
NCT01180179	PHASE4	COMPLETED	PPI vs H2RA in Patients With Helicobacter Pylori-Negative Idiopathic Bleeding Ulcers
NCT01506986	PHASE4	COMPLETED	Helicobacter Eradication Aspirin Trial
NCT01512953	PHASE4	UNKNOWN	Effect of Proton Pump Inhibitor on Residual Platelet Reactivity After Clopidogrel in Homogenous Genetic Strata
NCT01667718	PHASE4	COMPLETED	Bismuth Improves the Efficacy of Levofloxacin-containing Triple Therapy for Helicobacter Pylori Treatment
NCT02175901	PHASE4	COMPLETED	Amoxicillin/Metronidazole Based Quadruple Therapy for Helicobacter Pylori Eradication
NCT02175927	PHASE4	COMPLETED	High Dose Amoxicillin Versus Tetracycline as Second-line Treatment of Resistant Helicobacter Pylori Infection
NCT02251184	PHASE4	COMPLETED	Pharmacokinetics of Dipyridamole Administered as Aggrenox® (Dipyridamole Extended Release Plus Aspirin) Capsule Versus Dipyridamole Immediate Release Plus Aspirin Following Alteration of Stomach pH
NCT02278081	PHASE4	UNKNOWN	The Relationship Between Gastroesophageal Reflux and Pediatric Rhinitis: Significance of Pale/Blue Colored Turbinate
NCT02530879	PHASE4	WITHDRAWN	Comparison of Voice Therapy and Antireflex Therapy in LPR
NCT02633930	PHASE4	COMPLETED	Helicobacter Pylori Eradication With Berberine Quadruple Therapy Versus Clarithromycin Quadruple Therapy
NCT02679508	PHASE4	COMPLETED	Vonoprazan Study in Patients With Erosive Esophagitis to Evaluate Long-term Safety
NCT02755753	PHASE4	COMPLETED	A Study to Evaluate REbamiPide as an Adjuvant Regimen to Heal erosIve Reflux Esophagitis
NCT02759393	PHASE4	UNKNOWN	Treatment Effect Between Dexlansoprazole and Double-dose Lansoprazole in Obesity Patients With Reflux Esophagitis
NCT02958046	PHASE4	COMPLETED	The Efficacy of Lansoprazole and Domperidone Combination on Intragastric and Intraesophageal Acidity

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

PharmGKB also curates 4 clinical and 90 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).