Revanex (revaprazan) / Yuhan Corp - LARVOL DELTA

A Novel UPLC-MS/MS Method for Determining Tegoprazan in Rat Plasma: An Application in a Rat Pharmacokinetic Study. (PubMed, Biomed Chromatogr) - "The internal standard revaprazan (REV) and TEG were analyzed separately on a Waters ACQUITY UPLC BEH column. We finally established a rapid and robust UPLC-MS/MS quantitative analysis of TEG in rat plasma. Rat pharmacokinetics indicated that TEG was absorbed quickly and fast reached the maximum concentration."

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

In vitro combination effects and mechanisms of Revaprazan with Triazole antifungal drugs on Aspergillus. (PubMed, BMC Microbiol) - "This study evaluated REV combined with triazoles (itraconazole, ITR; voriconazole, VOR; posaconazole, POS) against 30 clinical Aspergillus isolates (14 A. fumigatus, 12 A. flavus, 4 A. terreus) using MIC and FICI assays. These in vitro results identify REV + POS as a promising combination against Aspergillus, though in vivo studies and mechanistic validation of transporter inhibition are warranted.Overall, this study shows that the potassium-competitive acid pump antagonist REV exhibits synergistic antifungal activity with triazoles in treating Aspergillus infections. The MFS transporter AF-MFS32 and AF-MFS35 are implicated as possible targets mediating the synergistic interaction between REV and these antifungal drugs."

Journal • Preclinical • Infectious Disease

Clinical pharmacokinetics of potassium competitive acid blockers: a systematic review and meta-analysis. (PubMed, Front Pharmacol) - "The search terms included "Potassium competitive acid blockers" or "P-CABs" or "revaprazan" or "vonoprazan" or "tegoprazan" or "fexuprazan" or "keverprazan" or "zastaprazan" and "pharmacokinetics"...Meta-analysis and qualitative studies indicated that clarithromycin significantly increased vonoprazan and tegoprazan exposure [geometric mean ratio (GMR) (90% confidence interval (CI))] of AUC and Cmax: 1.565 (1.443, 1.687) and 1.538 (1.454, 1.621) for vonoprazan, 2.624 (2.513, 2.735) and 1.876 (1.771, 1.981) for tegoprazan, respectively...It is important to select the appropriate P-CABs by considering the degree of influence on CYP enzymes, the dosage form, and food interactions. Studies on the interaction between P-CABs and antibiotics used to treat H. pylori infections, such as metronidazole, tetracycline, levofloxacin, or rifabutin, as well as non-vitamin K antagonist oral..."

Journal • PK/PD data • Retrospective data • Review • Infectious Disease • CYP2C19

Preliminary Analysis of Drug-Induced Ototoxicity in South Korea: Trends From a National Sample Dataset. (PubMed, J Audiol Otol) - "These correlations and the underlying mechanisms necessitate further investigation, as several medicines have been linked to an increased risk of HL."

Journal • Cardiovascular • Diabetes • Hypertension • Metabolic Disorders • Oncology • Otorhinolaryngology • Pain

Efficacy of Potassium Competitive Acid Blockers (PCABs) vs Proton Pump Inhibitors (PPIs) for Healing of Duodenal Ulcers: A Systematic Review and Meta Analysis (APASL 2025) - "PCABs such as Vonoprazan, Tegoprazan, Soraprazan, Revaprazan, Keverprazan and Linaprazan are reversible, competitive antagonists of the H+/K+ ATPase that is seen to have more sustained acid suppression. PCABs such as Vonoprazan 20mg and Keverprazan 20mg are non inferior to PPIs in the healing of duodenal ulcers. Both classes of drugs had similar tolerability profiles. Table and Figure:Figure 1.Forest plot of PCAB vs PPI on healing of duodenal ulcers at Week 6 Figure 2.Forest plot of PCAB vs PPI on healing of duodenal ulcers at Week 4"

Retrospective data • Review • Chronic Kidney Disease • Musculoskeletal Diseases • Nephrology • Orthopedics • Peptic Ulcer • Renal Disease

FEXUPRAZAN, A NOVEL POTASSIUM-COMPETITIVE ACID BLOCKER, AMELIORATES NSAID-INDUCED SMALL INTESTINAL MUCOSAL INJURY BY RESTORING THE EPITHELIAL BARRIER INTEGRITY IN MICE. (DDW 2024) - "Among other P-CABs revaprazan has demonstrated a reduction in NSAID-induced enteropathy while vonoprazan has not...0189) unlike esomeprazole...The study suggests that indomethacin induces mucosal injury in the small intestine accompanied by elevated inflammatory mediators and a compromised epithelial barrier. Fexuprazan emerges as a potential therapeutic alternative to PPIs demonstrating efficacy in ameliorating indomethacin-induced epithelial injury by restoring the integrity of intestinal epithelial cell junctions. Fexuprazan may serve as a promising option against NSAID-induced enteropathy."

Preclinical • Gastrointestinal Disorder • Inflammation • IL6 • TJP1 • TNFA

TREATMENT OF HELICOBACTER PYLORI WITH POTASSIUM COMPETITIVE ACID BLOCKERS: A SYSTEMATIC REVIEW AND META-ANALYSIS (DDW 2024) - "Methods : This study following PRISMA 0 0 guidelines conducted a systematic review and meta-analysis by searching MEDLINE and SCOPUS libraries for randomized clinical trials (RCTs) or observational studies with the following command: [("Helicobacter pylori" OR "H pylori") AND ("Treatment" OR "Therapy" OR "Eradication") AND ("Vonaprazan" OR "Potassium-Competitive Acid Blocker" OR "P-CAB" OR "PCAB" OR "Revaprazan" OR "Linaprazan" OR "Soraprazan" OR "Tegoprazan")]. Vonoprazan-based triple therapy outperformed conventional PPI-based triple therapy in eradicating H. pylori positioning it as a highly effective first-line regimen. Additionally Tegoprazan-based triple therapy wass non-inferior to classical PPI triple therapy."

Retrospective data • Review • Dyspepsia • Gastric Adenocarcinoma • Gastric Cancer • Gastroenterology • Gastrointestinal Cancer • Gastrointestinal Disorder • Hematological Malignancies • Infectious Disease • Lymphoma • Marginal Zone Lymphoma • Oncology • Peptic Ulcer • Solid Tumor

Treatment of Helicobacter pylori with potassium competitive acid blockers: A systematic review and meta-analysis. (PubMed, World J Gastroenterol) - "VPZ-based triple therapy outperformed conventional PPI-based triple therapy in eradicating H. pylori, positioning it as a highly effective first-line regimen. Additionally, TPZ-based triple therapy was non-inferior to classical PPI triple therapy."

Clinical • Journal • Retrospective data • Review • Dyspepsia • Gastric Adenocarcinoma • Gastric Cancer • Gastroenterology • Gastrointestinal Cancer • Gastrointestinal Disorder • Hematological Malignancies • Infectious Disease • Lymphoma • Marginal Zone Lymphoma • Oncology • Peptic Ulcer • Solid Tumor

Predicting pharmacodynamic effects through early drug discovery with artificial intelligence-physiologically based pharmacokinetic (AI-PBPK) modelling. (PubMed, Front Pharmacol) - "This platform enables researchers to align the PK profile of a drug with desired PD effects at the early drug discovery stage. Case studies are presented to assess and compare five potassium-competitive acid blocker (P-CAB) compounds, after calibration and verification using vonoprazan and revaprazan."

Journal • PK/PD data

Acid-suppressive drugs: A systematic review and network meta-analysis of their nocturnal acid-inhibitory effect. (PubMed, Pharmacotherapy) - "This is the first study to compare the effect of ASDs on inhibiting nocturnal acid breakthrough. Overall, in terms of nocturnal acid-inhibitory effect, vonoprazan and tegoprazan had an advantage against other regimens including H2RAs, isomer PPIs, traditional PPIs, AHB, and new PPIs. Even in some subgroups, such as language classification (English), types of study design (crossover-RCT), age (≤40 years), BMI (18.5-24.9 kg/m ), continent (Asia and North America), disease status (health), the duration of therapy (2 weeks), and time of administration (at daytime or at night-time), the nocturnal acid-inhibitory effect of vonoprazan or tegoprazan were better than most regimens, even AHB and new PPIs."

Journal • Retrospective data • Review

Sodium alginate-based smart gastro-retentive drug delivery system of revaprazan loaded SLNs; Formulation and characterization. (PubMed, Int J Biol Macromol) - "Further assessments in rats confirmed successful gel transformation within the stomach, resulting in the improved bioavailability of REV. Thus, the development of GRS/REV-SLNs significantly improved the delivery and bioavailability of REV within the stomach, and offers a potentially improved method of treating peptic ulcers."

Journal • Gastroenterology • Peptic Ulcer

A cochleate formulation optimized by D-optimal mixture design enhances oral bioavailability of Revaprazan. (PubMed, J Liposome Res) - "Following oral administration in rats, the optimised cochleate improved the relative bioavailability of RVP by approximately 274%, 255%, and 172% compared to RVP suspension, a physical mixture of RVP and the cochleate, and RVP-SUV, respectively. Thus, the optimised cochleate formulation might be a good candidate for the practical development of RVP."

Journal

Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. (PubMed, J Med Chem) - "We show crystal and cryo-EM structures of the gastric proton pump in complex with four different P-CABs, tegoprazan, soraprazan, PF-03716556 and revaprazan, at resolutions reaching 2.8 Å. We reveal that revaprazan has a novel binding mode in which its tetrahydroisoquinoline moiety binds deep in the cation transport conduit. The mechanism of action of these P-CABs can now be evaluated at the molecular level, which will facilitate the rational development and improvement of currently available P-CABs to provide better treatment of acid-related gastrointestinal diseases."

Journal • Gastroenterology • Gastrointestinal Disorder

Enhanced dissolution and bioavailability of revaprazan using self-nanoemulsifying drug delivery system. (PubMed, Pharm Dev Technol) - "This pretreatment barely affected the absorption of raw RVP; however, it greatly influenced the absorption of SNEDDS, resulting in an approximately 40% reduction in both the P value and oral BA representing lymphatic transport. Thus, we suggest that the SNEDDS formulation is a good candidate for improving oral absorption of RVP through enhanced lymphatic uptake."

Journal • Mental Retardation

Development of a Solid Supersaturable Micelle of Revaprazan for Improved Dissolution and Oral Bioavailability Using Box-Behnken Design. (PubMed, Int J Nanomedicine) - "RVP existed in an amorphous state in the optimized SSuM, and the SSuM formed a nanosized dispersion in the aqueous phase, with approximately 71.7% dissolution at 2 h. The optimized SSuM improved the relative bioavailability of RVP in rats by approximately 478%, 276%, and 161% compared to raw RVP, Revanex, and solid micelle, respectively. The optimized SSuM has great potential for the development of solidified formulations of poorly water-soluble drugs with improved oral absorption."

Journal

Pharmacodynamics of tegoprazan and revaprazan after single and multiple oral doses in healthy subjects. (PubMed, Aliment Pharmacol Ther) - "Tegoprazan 50 mg showed stronger gastric acid suppression than revaorazan 200 mg. Both drugs were well tolerated."

Clinical • Journal • PK/PD data • Gastroenterology • Gastroesophageal Reflux Disease • Infectious Disease • GAST

Revaprazan prevented indomethacin-induced intestinal damages by enhancing tight junction related mechanisms. (PubMed, Biochem Pharmacol) - "Here, we investigated the relative changes in indomethacin-induced enteropathy by combining indomethacin with pantoprazole (as PPI) or revaprazan (as PCAB). However, indomethacin and revaprazan combination significantly preserved TJPs and inactivated Rho-GTPase, MLC, and ERK. Hence, revaprazan rather than PPIs should be co-administered with NSAIDs to mitigate NSAID-induced intestinal damage."

Journal • Gastrointestinal Disorder • Immunology • Inflammation • Pain

Identification of Three Antimicrobials Activating Serotonin Receptor 4 in Colon Cells. (PubMed, ACS Synth Biol) - "The 5-HTR assay can be used to screen larger pharmaceutical libraries to identify novel treatments for IBS-C. This work shows that antimicrobials interact not only with the gut microbiota, but also with the human host."

Journal • Constipation • Immunology

A Study to Evaluate Safety, Tolerability, and PD of Tegoprazan on Healthy Male Volunteers (clinicaltrials.gov) - P1; N=16; Recruiting; Sponsor: CJ HealthCare Corporation

New P1 trial • Biosimilar

Revaprazan-loaded surface-modified solid dispersion: Physicochemical characterization and in vivo evaluation. (PubMed, Pharm Dev Technol) - "It had a significantly higher dissolution rate, AUC and C, and a faster T value in comparison to revaprazan powder, with a 5.3-fold improvement in oral bioavailability of revaprazan. Therefore, from an environmental perspective, this SMSD system prepared with water, and without organic solvents, should be recommended as a revaprazan-loaded oral pharmaceutical alternative."

Journal • Preclinical

Novel revaprazan-loaded gelatin microsphere with enhanced drug solubility and oral bioavailability. (PubMed, J Microencapsul) - "Particularly, it gave about 2.3-fold improved oral bioavailability in comparison with revaprazan powder. Therefore, this novel gelatin microsphere system is recommended as an oral pharmaceutical product of poorly water-soluble revaprazan."

Journal