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omeprazole (Omez Insta)

✓ Approved

Dr.Reddy's Laboratories Ltd. · ATP4A · 小分子

什么是 omeprazole？

omeprazole 是一种小分子，由Dr.Reddy's Laboratories Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Omez Insta
公司Dr.Reddy's Laboratories Ltd.
药物类别小分子
分子靶点ATP4A
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Dr.Reddy's Laboratories Ltd.

作用机制

分子靶点

omeprazole 作用于 1 个分子靶点：

ATP4AATPase H+/K+ transporting subunit alpha (ATP6A)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

omeprazole 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersGastritis✓ Approved

相关研究文献

PubMedPharmaceuticals (Basel, Switzerland)2026-10-27

Old Drugs, New Targets: Molecular Docking Insights into Repurposing Proton Pump Inhibitors for the TLR4/MD-2, NLRP3, and C5aR1 Axes in Autoimmune Liver Diseases.

Yıldız Mehmet M, Şeker Erdi E, Altınkaya Engin E, Poustforoosh Alireza A et al.

Background/Objectives: Autoimmune liver diseases (AILDs), including autoimmune hepatitis, primary biliary cholangitis, and primary sclerosing cholangitis, may include treatment-resistant cases and therefore require new therapeutic strategies. This in silico study evaluated proton pump inhibitors (PPIs) across three pathophysiologically complementary inflammatory targets relevant to hepatic immune injury: TLR4/MD-2, representing upstream innate immune sensing; NLRP3, representing inflammasome-mediated inflammatory amplification; and C5aR1, representing complement-dependent leukocyte recruitment. Methods: The binding profiles of four PPIs (rabeprazole, lansoprazole, omeprazole, and pantoprazole) were analyzed by molecular docking against TLR4/MD-2 (3FXI), NLRP3 (7VTP and 7PZC), and C5aR1 (6C1R and 5O9H). TAK-242, MCC950, and avacopan were included as target-associated reference ligands solely to provide structural and protocol-specific context. Their docking scores were not used as benchmarks of relative binding affinity, inhibitory potency, or pharmacological efficacy. MM-GBSA binding free energy calculations for the best score in all proteins were performed. Molecular docking and molecular dynamics analyses indicated stable interactions for the best docking score. Results: PPIs showed variable but potentially meaningful docking affinities across the evaluated targets. Rabeprazole produced favorable docking scores within the investigated TLR4/MD-2 (-7.85 kcal/mol) and inactive NLRP3 (-9.10 kcal/mol) binding sites under the present docking protocol. The reference ligands TAK-242 and MCC950 were included only to provide structural and protocol-specific context, and their docking scores were not interpreted as measures of relative pharmacological potency. Among the PPIs, lansoprazole showed the most favorable docking score for the C5aR1 allosteric site (-6.93 kcal/mol). Interaction analyses suggested favorable hydrophobic contacts and substantial spatial occupancy within the investigated binding pockets; however, cross-target docking compatibility may partly reflect nonspecific hydrophobic accommodation rather than genuine polypharmacology, and whether these predicted interactions produce target-specific functional effects requires experimental validation. MM-GBSA analysis supported the predicted stability of the rabeprazole-NLRP3 (7PZC) complex (ΔGbind = -56.97 kcal/mol). Conclusions: These findings prioritize rabeprazole and lansoprazole as PPI scaffolds showing favorable predicted interactions across several inflammation-related target structures within the applied computational framework. These results are hypothesis-generating and do not establish target inhibition, target engagement, or therapeutic efficacy. The results are hypothesis-generating and warrant experimental studies to determine whether these predicted interactions translate into target engagement or modulation of inflammatory signaling in AILDs.

PMID 42943278
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PubMedChemistry & biodiversity2026-10-26

Phytochemical Profiling, Molecular Docking Study, and Gastroprotective Effect of Matricaria chamomilla L. Aqueous Extract in Ethanol-Induced Gastric Ulcer in Mice.

Bouhadjar Meroua M, Naimi Dalila D, Cheriet Mouna M, Barros Lillian L et al.

While Matricaria chamomilla L. is renowned for its medicinal properties, most research has focused on its essential oils or organic extracts, neglecting the traditionally used aqueous preparation. This study investigated the chemical composition and the molecular interactions of phenolic compounds in chamomile aqueous extract (CAE), focusing on its unique water-soluble components. CAE, prepared from dried chamomile flowers, was analyzed by UHPLC-DAD-ESI-MS, revealing 19 phenolic constituents dominated by flavonoids and phenolic acids. In silico studies of the major compounds -trans-3,5-di-O-caffeoylquinic acid, myricetin-3-O-glucoside, and 4-O-caffeoylquinic acid, showed high binding affinities (-7.5 to -10.4 kcal/mol) via hydrogen bonding with the catalytic residues of cyclooxygenase-2, metalloproteinase-9, and gastric H+/K+ ATPase, providing a mechanistic of analytical findings. These computational findings were supported by in vitro antioxidant and anti-inflammatory assays and in vivo evaluation in ethanol-induced gastric ulcer mouse models. CAE treatment provided exceptional protection (99% at 500 mg/kg) and reduced the ulcer index from 4.5 to 0.24, significantly outperforming conventional omeprazole treatment. Histopathology confirmed improved mucosal integrity and reduced tissue damage. This work represents the first study combining phytochemical profiling of chamomile aqueous extract with multi-target molecular docking and in vivo validation of its gastro-protective efficacy.

PMID 42928570
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PubMedJournal of xenobiotics2026-10-26

Comparative Reporting Patterns of Rabeprazole and Other Proton Pump Inhibitors in EudraVigilance: A System Organ Class-Level Disproportionality Analysis.

Moleriu Radu Dumitru RD, Cioacă Gabriela Ramona GR, Muntean Călin C, Ilie Adrian-Cosmin AC et al.

Rabeprazole differs from other proton pump inhibitors (PPIs) in its activation and lower dependence on CYP2C19. We compared its System Organ Class (SOC)-level reporting profile with those of esomeprazole, pantoprazole, omeprazole and lansoprazole in EudraVigilance individual case safety reports (ICSRs). Aggregated ICSR counts were retrieved from adrreports.eu (data lock point 4 October 2026). Rabeprazole was compared head-to-head with each comparator using reporting odds ratios (RORs) with 95% confidence intervals across 27 MedDRA SOCs, with Benjamini-Hochberg false discovery rate control over all 108 tests. Bonferroni correction and serious-only analyses were sensitivity analyses; female-only and male-only analyses were exploratory. Of 232,045 ICSRs, 7960 involved rabeprazole. Hepatobiliary disorders were the only SOC reported more often with rabeprazole than with all four comparators (ROR 1.29-1.96); the excess met the Bonferroni threshold and persisted among serious reports (ROR 1.19-1.97) and in both sexes. Skin and subcutaneous tissue disorders were reported more often than with three comparators and, among serious reports, than with all four (ROR 1.14-1.83). Eight SOCs showed consistently lower reporting odds, alongside fewer SOCs per rabeprazole ICSR and a different reporter mix. Rabeprazole showed a consistent hepatobiliary reporting signal within the PPI class, in line with earlier FAERS findings. This is a reporting signal, not a clinical signal: without exposure data, the results describe relative reporting, not incidence, comparative risk or causality, and lower reporting odds do not imply lower clinical risk.

PMID 42931086
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PubMedFrontiers in gastroenterology (Lausanne, Switzerland)2026-10-25

Case Report: When reflux smells like smoke: a case of phantosmia associated with gastroesophageal reflux.

Visak Christopher C, Ketteler Skylar S, Husami Shireen S, Shafqat Imran I

Phantosmia is the perception of an odor without an external stimulus. Gastroesophageal reflux disease (GERD) has been associated with olfactory dysfunction, but phantosmia has rarely been described. A 40-year-old woman with longstanding GERD developed intermittent perceptions of cigarette smoke during a week of worsening heartburn and bloating. Episodes were accompanied by déjà vu, nausea, and chills. A double-contrast barium esophagram demonstrated a small hiatal hernia and reflux to the thoracic inlet. She reported approximately 80% improvement after starting omeprazole, with brief recurrence during a heartburn flare, and complete resolution at later follow-up. Migraine with aura, allergic rhinitis, focal seizures, and psychiatric causes were considered as alternative explanations. The close relationship between reflux activity and olfactory symptoms, together with improvement during reflux-directed treatment, supports a plausible association between GERD and phantosmia. This single case does not establish causation, and neurologic and sinonasal etiologies should remain part of the evaluation.

PMID 42923111
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PubMedBasic & clinical pharmacology & toxicology2026-10-23

Stereoselective Determination of Omeprazole and 5-Hydroxy-Omeprazole in Dried Blood Spots for CYP2C19 Activity Assessment.

Hectors Toon T, Abouir Kenza K, Varesio Emmanuel E, Manson Martijn L ML et al.

We previously proposed stereoselective 5-hydroxy-omeprazole/omeprazole cut-offs for R- and S-omeprazole to differentiate between rapid, normal, and poor CYP2C19 metabolisers. However, the performance of these stereoselective CYP2C19 phenotyping approaches has never been compared with conventional racemic omeprazole phenotyping. Therefore, dried blood spots from healthy, genetically predicted rapid (n = 15), normal (n = 15), and intermediate (n = 14) CYP2C19 metabolisers were stereoselectively reanalysed after administration of omeprazole alone (10 mg) and following CYP2C19 inhibition with voriconazole (400 mg administered prior to omeprazole). Using stereoselective R-, S-, and racemic 5-hydroxy-omeprazole/omeprazole ratios, CYP2C19 phenotyping performance was assessed by genotype-phenotype concordance and phenoconversion patterns relative to prior reports. An adaptive phenotyping strategy using the 3-h metabolic ratio in individuals with delayed absorption and retaining the 2-h ratio otherwise improved agreement with AUC-based CYP2C19 activity measures (Spearman ρ = 0.99 vs. 0.93 and 0.88 for fixed 2- and 3-h ratios, respectively). Across methods, the racemic approach demonstrated the most favourable overall performance, closely followed by the S-enantiomer-based strategy. In conclusion, while racemic omeprazole phenotyping modestly remains the most accurate strategy for assessing CYP2C19 activity, stereoselective assessment of the S-enantiomer provides an alternative that enables CYP2C19 phenotyping in patients treated with esomeprazole without treatment interruption or substitution with omeprazole.

PMID 42919487
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PubMedJournal of agricultural and food chemistry2026-10-23

Yeast Protein-Derived Peptides Protect against Ethanol-Induced Acute Gastric Mucosal Injury: Isolation, Identification, and Potential Mechanisms.

Luo Jin J, Qiao Kaina K, Bi Yongzhao Y, Liu Xialei X et al.

Ethanol-induced gastric mucosal injury (AGMI) is intrinsically linked to oxidative stress, inflammatory responses, and compromised mucosal defense. This study aimed to isolate bioactive peptides from yeast protein (YP) and elucidate these in vitro protective mechanisms against AGMI. Activity-guided multi-technique separation, nanoLC-MS/MS, and bioinformatic screening were used to identify two novel peptides, ISPALLDKL and TAADLRYF. In ethanol-injured GES-1 cells, these peptides (240 and 320 μg/mL) exhibited potent cytoprotective activity comparable to omeprazole. Peptide pre-treatment attenuated reactive oxygen species (from 31.79 to 9.52 and 10.02), restored mitochondrial membrane potential (ΔΨm increased from 0.5 to 2.78 and 2.11), and reduced apoptosis (from 28.55 to 10.52% and 12.58%). Furthermore, these peptides associated with the suppression of pro-inflammatory cytokines, decreasing TNF-α (24.9 and 21.9%), IL-1β (30.1 and 26.3%), and IL-6 (41.9 and 37.6%), while markedly enhancing the anti-inflammatory cytokine IL-10 (110.8 and 91.0%), respectively; these effects were accompanied by inhibition of NF-κB and JAK2-STAT3 phosphorylation. Collectively, ISPALLDKL and TAADLRYF protect against ethanol-induced gastric epithelial cell injury by simultaneously modulating oxidative stress, apoptosis, and inflammation, positioning them as promising natural candidates for gastric mucosal protection.

PMID 42915138
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