Dexlansoprazole

Summary

Dexlansoprazole (CHEMBL1201863) is an approved small molecule (ATC A02BC06); indicated across 6 conditions including gastroesophageal reflux disease and peptic ulcer disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A02BC06
• Indications: 6 conditions
• Clinical trials: 33
• Chemistry: 369.4 Da · C16H14F3N3O2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201863
Name	Dexlansoprazole
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	9578005
ATC	A02BC06
Molecular formula	C16H14F3N3O2S
Molecular weight	369.4
InChIKey	MJIHNNLFOKEZEW-RUZDIDTESA-N

SMILES: CC1=C(C=CN=C1C[S@@](=O)C2=NC3=CC=CC=C3N2)OCC(F)(F)F

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

Also known as: (r)-lansoprazole, Dexilant, Dexilant solutab, Dexlansoprazol, Dexlansoprazole, Kapidex, Lansoprazole r-form, Lansoprazole, (r)-, NSC-758710, T-168390, TAK-390, DEXLANSOPRAZOLE

Patent coverage: 575 distinct patent families (1,583 SureChEMBL compound mentions), from 5 matched compound structure(s). One matched structure accounts for 1,232 (78%) 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: 3 (assay-derived). Sample: Histone-lysine N-methyltransferase 2A/WDR5, NAD(+) hydrolase SARM1, Cytosolic endo-beta-N-acetylglucosaminidase.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SARM1	5.48	IC50	3300	nM	CHEMBL_ACT_19361228
SARM1	5.46	IC50	3500	nM	CHEMBL_ACT_19361222
WDR5	5.24	IC50	5700	nM	CHEMBL_ACT_22463505

Target pathways

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

Indications & clinical

Indications

6 indications (4 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
esophagitis	4	MONDO:0001409	HP:0100633
peptic esophagitis	3	MONDO:0006896	EFO:1001095
Barrett esophagus	2	MONDO:0013662	EFO:0000280

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

Clinical trials

Total trials: 33.

Phase distribution

Phase	Trials
PHASE1	12
PHASE4	8
PHASE2	5
PHASE3	3
Not specified	3
PHASE1/PHASE2	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01093755	PHASE4	COMPLETED	Does Intensive Acid Suppression Reduce Esophageal Inflammation and Recurrent Barrett’s Esophagus Following Ablation?
NCT01328652	PHASE4	UNKNOWN	Dexlansoprazole to Treat Laryngopharyngeal Reflux and Lingual Tonsil Hypertrophy
NCT01637571	PHASE4	WITHDRAWN	Dexilant Treatment in Gastrointestinal Reflux Disease (GERD Related Non Cardiac Chest Pain
NCT02351960	PHASE4	COMPLETED	Dexlansoprazole in Asian Participants With Gastroesophageal Reflux Disease
NCT02759393	PHASE4	UNKNOWN	Treatment Effect Between Dexlansoprazole and Double-dose Lansoprazole in Obesity Patients With Reflux Esophagitis
NCT03079050	PHASE4	COMPLETED	An Open-Label Trial of Dexlansoprazole 60mg for the Relief of Heartburn During the Fasting Month of Ramadan
NCT03128736	PHASE4	COMPLETED	Comparing Clinical Efficacy of One-Week Dual Delayed-Release Dexlansoprazole and Esomeprazole for GERD Grade A and B
NCT06778395	PHASE4	COMPLETED	Therapeutic Effect of Vonoprazan Versus Dexlansoprazole in Treatment of Gastroesophageal Reflux Disease
NCT00627016	PHASE3	COMPLETED	A Study of Dexlansoprazole Modified Release Formulation to Treat Night Heartburn
NCT02873689	PHASE3	COMPLETED	Efficacy and Safety of Dexlansoprazole on Heartburn Relief in Chinese Patients
NCT02873702	PHASE3	TERMINATED	Efficacy and Safety of Dexlansoprazole in Healing and Maintaining Healing of Erosive Esophagitis
NCT02616302	PHASE2	ACTIVE_NOT_RECRUITING	A Study to Check the Safety of Dexlansoprazole and Learn if it Can Treat Symptomatic Nonerosive Gastroesophageal Reflux Disease in Children 2 to 11 Years Old
NCT01479231	PHASE1/PHASE2	WITHDRAWN	Predictors of Proton Pump Inhibitor (PPI) Response in Eosinophilic Esophagitis
NCT01642602	PHASE2	COMPLETED	Safety and Efficacy of Dexlansoprazole Delayed-Release Capsules in Treating Symptomatic Non-Erosive Gastroesophageal Reflux Disease in Adolescents
NCT01642615	PHASE2	COMPLETED	Safety and Efficacy of Dexlansoprazole Delayed-Release Capsules for Healing of Erosive Esophagitis and Maintenance of Healed Erosive Esophagitis and Relief of Heartburn in Adolescents
NCT02162758	PHASE2	TERMINATED	Effect of Dexlansoprazole 60 mg QD and 60 mg BID on Recurrence of Intestinal Metaplasia in Subjects Who Have Achieved Complete Eradication of Barrett’s Esophagus With Radiofrequency Ablation
NCT02615184	PHASE2	TERMINATED	A Study to Check the Safety of Dexlansoprazole and Learn If it Can Heal Erosive Esophagitis (EE) and Keep it Healed in Children 2 to 11 Years Old
NCT00942175	PHASE1	COMPLETED	A Study of the Effects of Multiple Doses of Dexlansoprazole, Lansoprazole, Omeprazole or Esomeprazole on the Pharmacokinetics and Pharmacodynamics of Clopidogrel in Healthy Participants.
NCT01045096	PHASE1	COMPLETED	Study to Evaluate the Pharmacokinetics and Safety of Dexlansoprazole in Pediatric Subjects With Symptomatic Gastroesophageal Reflux Disease
NCT01149395	PHASE1	COMPLETED	Can E-cadherin Found in Tissue/Blood be Valuable in Identifying & Monitoring Patients With Post-proton Pump Inhibitor (PPI)-Responsive Heartburn
NCT01216293	PHASE1	COMPLETED	Effect of Dexlansoprazole on Bone Homeostasis
NCT02096458	PHASE1	COMPLETED	Sensory Evaluation of Dexlansoprazole Delayed-Release Orally Disintegrating Tablets
NCT02442752	PHASE1	WITHDRAWN	Phase 1 Dexlansoprazole Delayed-Release Capsules for Acid-Related Disorders in Infants Aged 1 to 11 Months
NCT02529787	PHASE1	COMPLETED	A Bioequivalence Study of Dexlansoprazole From Doxirazole 60 mg Capsules (Hikma Pharma,Egypt)and Dexilant 60 mg Delayed Release (DR) Capsules (Takeda Pharmaceuticals America Inc., USA)
NCT03011125	PHASE1	COMPLETED	A Clinical Trial to Evaluate the Safety and Tolerability of Dexlansoprazole Injection in Healthy Chinese Adults (Part 1)
NCT03043521	PHASE1	COMPLETED	Pharmacodynamic Properties of CJ-12420 on Evening Dosing
NCT03120273	PHASE1	UNKNOWN	A Clinical Trial to Evaluate the Safety and Tolerability of Dexlansoprazole Injection in Healthy Chinese Adults（Part 2）
NCT03316976	PHASE1	COMPLETED	A Study to Evaluate the Pharmacokinetics of Dexlansoprazole 30 Milligram (mg) and 60 mg Delayed-release Capsules in Healthy Chinese Participants
NCT04877834	PHASE1	COMPLETED	Bioequivalence Study of DelanzoᵀᴹDR 60mg (Dexlansoprazole) Capsule With Dexilant® 60mg (Dexlansoprazole) Capsule in Healthy Pakistani Subjects.
NCT03202537	EARLY_PHASE1	COMPLETED	Effectiveness of Physiologic Testing in PPI Non-Responders
NCT00928161	Not specified	WITHDRAWN	Reflux Disease in Head and Neck Cancer Patients Undergoing Radiation Therapy
NCT01317472	Not specified	TERMINATED	The Effects of Dexlansoprazole for the Treatment of Throat-Related Reflux
NCT01328392	Not specified	WITHDRAWN	Evaluating Treatment Response in Laryngo-Pharyngeal Reflux

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for dexlansoprazole and CYP2C19	CPIC	CYP2C19	yes	yes

PharmGKB also curates 1 clinical and 4 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).