Delving into the Latest Updates on Revaprazan Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Revanex, Revaprazan, Revaprazan hydrochloride (USAN)

+ [8]

Target

H+/K+ ATPase x Proton pump

Mechanism

P-CAB(Potassium-competitive acid blockers), Proton pump inhibitors

Therapeutic Areas

Digestive System Disorders

Active Indication

Duodenal UlcerGastritisStomach Ulcer

Inactive Indication

Non-erosive gastro-esophageal reflux diseaseNon-erosive reflux disease

Originator Organization

Yuhan Corp.

Active Organization

Yuhan Corp.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

KR (15 Sep 2005),

Duodenal UlcerGastritisStomach Ulcer

Regulation-

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Structure

Molecular FormulaC22H23FN4

InChIKeyLECZXZOBEZITCL-UHFFFAOYSA-N

CAS Registry199463-33-7

View All Structures (2)

AbstractBackground and AimsAcid‐suppressive drugs (ASDs) are widely used in many gastric acid‐associated diseases. Nocturnal acid breakthrough has been a common problem of many ASDs, such as proton‐pump inhibitors (PPIs) and H2‐receptor antagonists (H2RAs). Potassium‐competitive acid blockers (P‐CABs) are expected to solve this continuing conundrum. This article examined major ASDs and compared them with placebo in terms of nocturnal acid‐inhibitory effects, using a network meta‐analysis of randomized controlled trials (RCTs).MethodsTo compare the effectiveness of major ASDs, a Bayesian network meta‐analysis (NMA) was applied to process data extracted from RCTs. The plausible ranking for each regimen and some subgroups were assessed by surface under the cumulative ranking curves (SUCRA).ResultsFifty‐five RCTs were conducted with 2015 participants. In terms of nocturnal acid‐inhibitory effects, the overall results showed that tegoprazan (SUCRA 91.8%) and vonoprazan (SUCRA 91.0%) had the best performance, followed by new PPIs (including tenatoprazole and ilaprazole) (SUCRA 76.6%), additional H2RAs once at bedtime (AHB) (SUCRA 61.3%), isomer PPIs (including esomeprazole and dexlansoprazole) (SUCRA 38.6%), revaprazan (SUCRA 34.7%), traditional PPIs (including omeprazole, rabeprazole, pantoprazole, lansoprazole) (SUCRA 32.6%), H2RAs (SUCRA 23.1%), and placebo (SUCRA 0.3%). In some subgroups, the nocturnal acid‐inhibitory effect of vonoprazan or tegoprazan was better than most of the other regimens, even new PPIs and AHB.ConclusionsThis 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/m2), 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.

02 Jan 2024·Journal of Liposome Research

A cochleate formulation optimized by D-optimal mixture design enhances oral bioavailability of Revaprazan

Article

Author: Kim, Min Song ; Sin, Gi Hyeong ; Choi, Young Wook ; Choi, Ji Yeh ; Goo, Yoon Tae ; Hong, Sun Ho ; Kim, Chang Hyun

A cochleate formulation was developed to enhance the oral bioavailability of revaprazan (RVP). Dimyristoyl phosphatidylcholine (DMPC) liposome containing dicetyl phosphate (DCP) successfully formed a cochleate after treatment with CaCl₂, whereas that containing sodium deoxycholate did not. Cochleate was optimised using a D-optimal mixture design with three independent variables-DMPC (X₁, 70.58 mol%), cholesterol (X₂, 22.54 mol%), and DCP (X₃, 6.88 mol%)-and three response variables: encapsulation efficiency (Y_1, 76.92%), released amount of free fatty acid at 2 h (Y₂, 39.82%), and released amount of RVP at 6 h (Y₃, 73.72%). The desirability function was 0.616, showing an excellent agreement between the predicted and experimental values. The cylindrical morphology of the optimised cochleate was visualised, and laurdan spectroscopy confirmed the dehydrated membrane interface, showing an increased generalised polarisation value (approximately 0.5) over small unilamellar vesicle of RVP (RVP-SUV; approximately 0.1). The optimised cochleate showed greater resistance to pancreatic enzyme than RVP-SUV. RVP was released in a controlled manner, achieving approximately 94% release in 12 h. 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.

01 Dec 2023·International Journal of Biological Macromolecules

Sodium alginate-based smart gastro-retentive drug delivery system of revaprazan loaded SLNs; Formulation and characterization

Article

Author: Raja, Hadiqa Nazish ; Al Awadh, Ahmed Abdullah ; Alasiri, Ali ; Khan, Salman ; Alamri, Ali H ; Shabbir, Kanwal ; Lahiq, Ahmed A ; Din, Fakhar Ud

Revaprazan (REV), a novel reversible Proton Pump Inhibitor (PPI) used to treat peptic ulcers, faces challenges in therapeutic efficacy due to its poor dissolution properties and a short half-life. Solid lipid nanoparticles (SLNs) have emerged as a drug delivery system capable of enhancing dissolution and bioavailability of lipid soluble drugs. Here, we report on the development and optimization of a smart gastro-retentive raft system of REV-loaded SLNs (GRS/REV-SLNs) to enhance drug bioavailability and gastric retention. The optimized REV-SLNs had a particle size of 120 nm, a Polydispersity Index (PDI) of 0.313, a zeta potential of -20.7 mV, and efficient drug incorporation of 88 %. Transmission Electron Microscopy (TEM) affirmed the spherical morphology of these REV-SLNs, while Fourier Transform Infrared Spectroscopy (FTIR) revealed no chemical interactions among components. In-vitro assessment of the final GRS/REV-SLNs demonstrated sustained gelation and buoyancy for over 12 h, which would significantly enhance REV retention and its release within the stomach. 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.

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