ilaprazole / Generic mfg. - LARVOL DELTA

Cytochrome P450 Enzymes in the Metabolism of Proton Pump Inhibitors: Implications for the Treatment of Peptic Ulcers. (PubMed, Curr Drug Targets) - "Incorporating CYP2C19 genotyping and pharmacogenomic data into clinical decisionmaking may improve treatment individualization, although evidence remains heterogeneous and context-dependent."

Journal • Gastroenterology • Gastrointestinal Disorder • Infectious Disease • Metabolic Disorders • Peptic Ulcer • CYP2C19 • CYP3A4

Comparative effectiveness of genotype-guided and empirical bismuth-containing quadruple therapy for Helicobacter pylori eradication: a retrospective study. (PubMed, Front Pharmacol) - "All regimens comprised bismuth potassium citrate 2.6 g, a proton pump inhibitor (PPI, esomeprazole 20 mg or ilaprazole 5 mg) or a potassium-competitive acid blocker (P-CAB, keverprazan 20 mg or tegoprazan 50 mg), and antibiotics selected from amoxicillin, clarithromycin, levofloxacin, furazolidone, tetracycline, metronidazole, or doxycycline. Dual clarithromycin and levofloxacin resistance and alcohol consumption remained key determinants of treatment failure even with genotype-guided therapy. However, the precision of estimates for single-drug resistance subgroups was limited by small sample sizes and should be interpreted cautiously."

HEOR • Journal • Retrospective data • Addiction (Opioid and Alcohol) • Infectious Disease

Assessment of Pharmacokinetic Interaction and Clinical Efficacy of Clopidogrel Co-administered with Ilaprazole. (PubMed, Clin Pharmacol Drug Dev) - "Geometric mean ratio (GMR) analysis showed a marked reduction in clopidogrel exposure with pantoprazole (Cmax GMR 0.31, 90% CI 0.18-0.53; AUC GMR 0.24, 90% CI 0.19-0.29), and platelet aggregation was significantly higher at 4 and 10 h (P  .05) Ilaprazole did not affect clopidogrel pharmacokinetics or pharmacodynamics, suggesting it as a safer alternative to pantoprazole in dual antiplatelet therapy."

Clinical • Journal • PK/PD data • Gastroenterology • CYP2C19 • CYP3A4

Rabeprazole exhibits broad-spectrum fusion inhibition against Nipah pseudovirus and authentic HCoV-OC43 and RSV. (PubMed, Bioorg Chem) - "Systematic structure-activity relationship (SAR) profiling among clinically approved PPIs revealed that Ilaprazole and Lansoprazole exhibited stronger anti-NiV potency than Rabeprazole, while Rabeprazole sulfide showed enhanced antiviral activity relative to the parent compound. Rabeprazole also inhibited live RSV and HCoV-229E infection in a dose-dependent manner. Collectively, these findings establish the HR1 groove as a druggable pan-viral target and validate benzimidazole-based PPIs as a versatile scaffold for developing orally available, broad-spectrum antivirals against phylogenetically distinct enveloped viruses that rely on class I fusion machinery."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases • Respiratory Syncytial Virus Infections

An Evaluation of the Inhibitory Effect of Apatinib on Ilaprazole Metabolism: in vitro, in vivo and in silico Study. (PubMed, Drug Des Devel Ther) - "In addition, molecular docking provided structural context for the observed interaction. However, whether the same phenomenon exists in humans remains to be further investigated."

Journal • Preclinical • Gastrointestinal Disorder • Peptic Ulcer • CYP3A4

Ilaprazole Versus Esomeprazole for Artificial Ulcer Healing After Gastric Endoscopic Submucosal Dissection: A Single-Center Retrospective Study. (PubMed, J Clin Med) - "Artificial ulcer size ≥ 30 mm was the principal determinant of delayed healing, whereas the treatment group was not independently associated with healing outcomes. Ilaprazole may be considered a reasonable maintenance PPI option in routine post-ESD management."

Journal • Retrospective data • Gastric Cancer • Oncology • Solid Tumor

Repurposing Ilaprazole as a PP5 TPR Domain Binder with Modulatory Effects on MAPK Signaling. (PubMed, ACS Med Chem Lett) - "While exhibiting minimal single-agent effects, ilaprazole sensitized cells to the MEK inhibitor binimetinib. These results validate the PP5 TPR domain as a druggable site and establish ilaprazole as a lead scaffold for pharmacological modulation of PP5-associated MAPK signaling."

Journal • Colorectal Cancer • Oncology • Solid Tumor • KRAS

Efficacy and safety of ilaprazole for stress ulcer - associated upper gastrointestinal bleeding prophylaxis in critically ill patients: a randomized, double-blind, non-inferiority phase 3 trial. (PubMed, Ann Intensive Care) - "Adverse events were similar between groups, but Ilaprazole had a significantly lower incidence of hepatobiliary disorders (0.9% vs. 5%, p = 0.012). Ilaprazole demonstrated non-inferiority to esomeprazole in preventing UGI bleeding in critically ill patients at high risk of stress ulcer."

Clinical • Head-to-Head • Journal • P3 data • Gastroenterology • Gastrointestinal Disorder • Hepatology • Inflammation • Pneumonia • Stress Ulcer

Assessment of diverse proton pump inhibitor combined with bismuth quadruple regimens and risk factors for Helicobacter pylori eradication in China: A retrospective single-center study. (PubMed, Arab J Gastroenterol) - "The eradication rates across various PPI-based quadruple regimens were comparable; however, the regimen comprising amoxicillin and clarithromycin demonstrated low efficacy and is not advised in settings with high clarithromycin resistance. Among the effective therapeutic regimens, the esomeprazole-based regimen exhibited a slightly higher eradication rate."

Journal • Retrospective data • Infectious Disease

Pharmacokinetics and Bioequivalence of Ilaprazole Enteric-Coated Tablets in Healthy Chinese Volunteers: A Two-Sequence, Four-Period, Fully Replicated Crossover Study. (PubMed, Clin Pharmacol Drug Dev) - "The geometric means and 90% confidence intervals of AUC0-t, AUC0-∞, and Cmax for both fasting and fed conditions were within the 80%-125% bioequivalence range, and the upper limit of the one-sided 95% confidence interval was ≤0. Both formulations demonstrated bioequivalence under these conditions, with no serious adverse reactions observed."

Journal • PK/PD data • Gastroenterology • Gastroesophageal Reflux Disease • CYP2C19

Different Doses of Ilaprazole for Dual Therapy Versus Bismuth-Quadruple Therapy for Helicobacter pylori Infection: A Three-Arm, Randomized Clinical Trial. (PubMed, Helicobacter) - P4 | "The standard- or high-dose dual therapy with ilaprazole demonstrated superior efficacy, safety, and patient compliance compared to quadruple therapy. No significant differences were observed between these dual therapies, which are expected to become promising alternatives for the primary treatment of H. pylori infection."

Clinical • Journal • Infectious Disease

In vitro anti-Helicobacter pylori activity of ilaprazole used alone and in combination with other components of quadruple therapy. (PubMed, Microbiol Spectr) - "The antibacterial activity of ilaprazole was tested on 25 H. pylori strains, including the clinical isolates resistant to clarithromycin (CLA), amoxicillin (AMX), levofloxacin, and/or metronidazole. Importantly, repeated exposure to ilaprazole did not induce resistance, a critical factor for its long-term use. These results provide compelling evidence for ilaprazole's inclusion in clinical treatment strategies, contributing to improved eradication rates and better patient outcomes in H. pylori management."

Journal • Preclinical • Gastroenterology • Gastroesophageal Reflux Disease • Gastrointestinal Disorder • Infectious Disease • Peptic Ulcer

Study to Evaluate the Efficacy and Safety of Ilaprazole 10 mg in Prevention NSAIDs Associated Peptic Ulcer (clinicaltrials.gov) - P3 | N=416 | Recruiting | Sponsor: Il-Yang Pharm. Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • Gastroenterology • Peptic Ulcer

Comparative in vitro assessment of CYP2C19 inhibition by ilaprazole and conventional proton pump inhibitors using a high throughput fluorometric assay. (PubMed, Sci Rep) - "The current study aimed to predict the CYP2C19 inhibitory potential of Ilaprazole versus conventional PPIs (Omeprazole, Lansoprazole, Pantoprazole, and Rabeprazole) on CYP2C19 activity using a high-throughput fluorometric assay. Omeprazole is the most potent CYP2C19 inhibitor, as it exceeded the regulatory threshold guidelines for in vitro study, while other tested PPIs, including Ilaprazole, did not meet this cutoff, suggesting a lower likelihood of clinically significant inhibition. Although previous in vivo studies suggest variable inhibition with other PPIs, current data support the need for further head-to-head in vivo comparisons, particularly between Pantoprazole, Rabeprazole, and Ilaprazole, to determine the most suitable option in clinical scenarios involving CYP2C19 substrate."

Clinical • Journal • Preclinical • CYP2C19

Comparative Analysis of the Efficacy of Esomeprazole and Ilaprazole in Patients With Neurological Disorders Using the Gastroesophageal Reflux Disease Questionnaire. (PubMed, Clin Neuropharmacol) - "Significant differences existed between esomeprazole and ilaprazole users and among ilaprazole users based on aspirin use. Therefore, careful monitoring of PPI use with antiplatelet agents and antacids is recommended in patients with neurological disorders. However, further research is needed to understand these differences and their clinical impact."

Journal • Atrial Fibrillation • Cardiovascular • CNS Disorders • Dyslipidemia • Gastroenterology • Gastroesophageal Reflux Disease • Metabolic Disorders

Medication Safety in Intravenous Therapy: Compatibility of Etoposide with Frequently Drugs Used in Tumour Critical Care During Simulated Y-Site Administration. (PubMed, Drug Des Devel Ther) - "Within 1 h, four medications (cefuroxime sodium, ilaprazole sodium, mycophenolate, and xuebijing) were incompatible. Within 4 h, one medications (ceftazidime) were also found to be incompatible with etoposide under observation. Seven of the 45 common medications in tumor critical care tested with etoposide were incompatible within 4 h. If co administration is inevitable and the drug is infused through a port catheter, a larger volume of saline (NS) or dextrose 5% in water (D5W) should be used to flush the port catheter before and after the etoposide infusion to clean the lumen of the port catheter."

Journal • Critical care • Oncology • Pediatrics

Simultaneous Determination of Multiple Acid-Suppressing Drugs by UPLC-MS/MS Method and Application for Pharmacokinetics Study. (PubMed, Drug Des Devel Ther) - "This study aimed to establish a generic and efficient ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) assay for the determination of five PPIs (esomeprazole, rabeprazole, ilaprazole, lansoprazole, and pantoprazole) and the P-CAB (vonoprazan) in human plasma. The UPLC-MS/MS assay provided an efficient and reliable approach for the simultaneous determination of six acid-suppressing medications in a single analytical run. It has been successfully applied to the pharmacokinetic studies of PPIs and P-CABs, offering a valuable tool for clinical research and therapeutic drug monitoring."

Journal • PK/PD data

Efficacy and safety of high-dose ilaprazole dual therapy for Helicobacter pylori eradication: a multicenter, open-label, randomized controlled clinical trial (ChiCTR) - P4 | N=504 | Sponsor: Shenzhen Hospital of Southern Medical Unversity; Shenzhen Hospital of Southern Medical Unversity

New P4 trial • Infectious Disease

Delineating CYP2C19-Mediated Interactions: Network Pharmacology Investigation of Ilaprazole and Clopidogrel versus Conventional Proton Pump Inhibitors. (PubMed, Curr Drug Discov Technol) - "The application of the network pharmacology technique allows us to consider the potential for different effects of PPIs on clopidogrel and its metabolism via CYP2C19. There is a lower chance of experiencing adverse effects from an interaction between ilaprazole and clopidogrel as ilaprazole has not been linked to CYP2C19. More research is necessary to confirm these results and provide clinical guidance for patients undergoing clopidogrel and PPI combination therapy."

Journal • Cardiovascular • CYP2C19

Biophysical interactions between self-sufficient cytochrome P450 from Tepidiphilus thermophilus and ilaprazole. (PubMed, Dalton Trans) - "This study investigated CYP116B46, a self-sufficient monooxygenase with a reductase domain, to elucidate its interaction with ilaprazole, a PPI. Binding assays and docking simulations indicate that CYP116B46 serves as a suitable model for studying PPI metabolism."

Journal

TREATMENT PATTERNS IN CHINESE PATIENTS WITH HELICOBACTER PYLORI: A MULTICENTER, RETROSPECTIVE, REAL-WORLD STUDY (UEGW 2024) - P=N/A | "Distribution of eradication therapy based upon the type and year of treatment initiation TreatmentType of Eradication therapy (N=13, 234)n (%)aYear of treatment initially prescribed , 2019(N=4492)n (%)aYear of treatment initially prescribed, 2020(N=4125)n (%)aYear of treatment initially prescribed, 2021 (N=4616)n (%)aTotalBismuth quadruple therapyAmoxicillin and ClarithromycinAmoxicillin and FurazolidoneAmoxicillin and LevofloxacinAmoxicillin and MetronidazoleAmoxicillin and TetracyclineFurazolidone and TetracyclineOther Bismuth quadrupleTriple therapycDual therapyc13,234b (-)11,301 (85.39)4376 (38.72)2074 (18.35)2007 (17.76)76 (0.67)9 (0.08)12 (0.11)2747 (24.31)999 (7.55)934 (7.06)4492 (-)4368 (97.24)1800 (41.21)689 (15.77)1021 (23.37)27 (0.62)5 (0.11)1 (0.02)825 (18.89)105 (2.34)19 (0.42)4125 (-)3299 (79.98)1324 (40.13)480 (14.55)516 (15.64)10 (0.30)1 (0.03)0 (0.00)968 (29.34)551 (13.36)275 (6.67)4617 (-)3634 (78.71)1252 (34.45)905 (24.90)470 (12.93)39 (1.07))3..."

Real-world • Real-world evidence • Retrospective data • Gastric Cancer • Gastrointestinal Cancer • Infectious Disease • Oncology • Solid Tumor

Clinical efficacy of ilaprazole combined with somatostatin on severe acute pancreatitis and the effects on oxidative stress and inflammatory response. (PubMed, Pak J Pharm Sci) - "In treatment of SAP, ilaprazole combined with somatostatin can enhance the curative efficacy and decrease the oxidative stress and the inflammatory response in patients. In addition, it cannot increase the adverse reactions, with good safety."

Clinical • Journal • Inflammation • Oncology • Pain • Pancreatitis • CRP • IL6 • TNFA

Efficacy and safety of vonoprazan versus proton pump inhibitors in the treatment of peptic ulcer disease: a systematic review and network meta-analysis for randomized controlled trails. (PubMed, Front Nutr) - "In terms of the healing rate at 2 weeks, lansoprazole 30 mg ranked first, followed by vonoprazan 20 mg and ilaprazole 10 mg. In terms of the healing rate at 4 weeks, pantoprazole 40 mg ranked first, with rabeprazole 10 mg and lansoprazole 30 mg ranking second and third, respectively...Furthermore, lansoprazole 30 mg has shown to be superior in terms of safety outcomes. These findings, derived from a network meta-analysis, necessitate further research for validation."

Journal • Retrospective data • Review • Gastroenterology • Gastrointestinal Disorder • Peptic Ulcer

Comparison of the Efficacy and Safety of Dual and Quadruple Therapy with Ilaprazole in the Eradication of Helicobacter pylori (ChiCTR) - P4 | N=480 | Completed | Sponsor: Beijing Huaxin Hospital (The First Affiliated Hospital of Tsinghua University); China Health Medical Development Foundation

New P4 trial • Infectious Disease

The Impact of a Twice-daily vs Once-daily Proton Pump Inhibitor Dosing Regimen on Laryngopharyngeal Reflux Symptoms: A Prospective Randomized Controlled Trial. (PubMed, J Neurogastroenterol Motil) - "These patients were randomly assigned to receive either a 10 mg twice daily (BID) or a 20 mg once daily (QD) dose of ilaprazole for 12 weeks...Both BID and QD PPI dosing regimens improved subjective symptom scores and objective laryngoscopic findings. There was no significant difference in RSI improvement between the 2 dosing regimens, indicating that either dosing regimen could be considered a viable treatment option."

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