Drug Database
MO

mosapride + rebamipide (MotiReb / Mucosta + Gasmotin / MR tablet)

✓ Approved

Ildong Pharmaceutical · HTR3A · Small Molecule

What is mosapride + rebamipide?

mosapride + rebamipide is a small molecule developed by Ildong Pharmaceutical. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesMotiReb, Mucosta + Gasmotin, MR tablet
CompanyIldong Pharmaceutical
Drug ClassSmall Molecule
Molecular TargetHTR3A, HTR4
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Ildong Pharmaceutical

Mechanism of Action

Molecular Targets

mosapride + rebamipide acts on 2 molecular targets:

HTR3A5-hydroxytryptamine receptor 3A (5-HT3R, 5-HT-3)
HTR45-hydroxytryptamine receptor 4 (5-HT4, 5-HT4R)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

mosapride + rebamipide is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Gastrointestinal disordersDyspepsia✓ Approved

Related Research Articles

PubMedAnimals : an open access journal from MDPI2026-10-16

Oral Mosapride Attenuates Gastrointestinal Dysmotility During Experimental Endotoxemia in Horses: A Randomized, Blinded Crossover Study.

Varela Diego Duarte DD, Rosa Ana Carolina Ribeiro ACR, Sousa Lara Nunes LN, Luvison Eduarda Zancanaro EZ et al.

Endotoxemia is a major contributor to gastrointestinal hypomotility and postoperative ileus in horses. This study investigated whether oral mosapride retained prokinetic activity during acute lipopolysaccharide (LPS)-induced endotoxemia. Seven healthy adult horses were enrolled in a randomized, blinded, three-period crossover trial and received LPS alone, mosapride alone (MOSA), or LPS plus mosapride (LPS + MOSA), with a 14-day washout interval between periods. Mosapride was administered orally at 2 mg/kg, whereas endotoxemia was induced by an intravenous infusion of Escherichia coli O55:B5 LPS (0.03 µg/kg) over 30 min. Clinical variables, hematologic parameters, abdominal auscultation, and transabdominal ultrasonography were assessed from baseline to 6 h. LPS induced tachycardia, hyperthermia, leukocyte alterations, marked gastrointestinal hypomotility, gastric distension, and increased intestinal wall thickness. Mosapride alone increased gastrointestinal motility without clinically relevant abnormalities. During endotoxemia, mosapride partially restored gastrointestinal motility, reduced intestinal wall thickening and gastric distension, and was associated with a less pronounced hematologic inflammatory response than LPS alone. These findings indicate that oral mosapride retains clinically relevant prokinetic activity during acute experimental endotoxemia and support further investigation of its use as an adjunctive treatment for inflammation-associated gastrointestinal hypomotility in horses.

PMID 42883002
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PubMedZhongguo zhen jiu = Chinese acupuncture & moxibustion2026-10-13

[Effect of medicated-thread moxibustion of Zhuang medicine on autophagy in gastric smooth muscle cells of rats with diabetic gastroparesis via miR-10b-5p/PTEN/PI3K/AKT signaling pathway].

Xu Hui H, He Yujun Y, Wu Yu Y, Wang Zibin Z et al.

To investigate the underlying mechanism of medicated-thread moxibustion of Zhuang medicine in intervention of diabetic gastroparesis (DGP). A total of 63 male SD rats were randomly divided into a blank group (13 rats) and a model preparation group (50 rats). The DGP models were established in the model preparation group by intraperitoneal injection of 1% streptozotocin (55 mg/kg). Forty successfully modeled rats were randomized into a model group, a western medicatione group, a non-meridian and non-point group, and a yangming meridian point group, with 10 rats in each group. In the yangming meridian point group, the medicated-thread moxibustion of Zhuang medicine was operated at bilateral "Liangmen" (ST21), "Qichong" (ST30), "Zusanli" (ST36), and "Fenglong" (ST40), with 3 moxa cones at each point. In the non-meridian and non-point group, the medicated-thread moxibustion of Zhuang medicine was operated at the sites not belonging to either meridian or meridian point, with 3 moxa cones per site. In the western medication group, mosapride citrate suspension was administered via gavage (10 mL/kg). All interventions were performed once daily, and for 3 consecutive weeks. Blood glucose level, gastric emptying rate, and small intestinal propulsion rate were measured in each group. HE staining was used to observe the morphology of gastric smooth muscle in gastric amooth muscle; Western blot was used to detect the protein expression of ubiquitin-bound protein p62 (p62), Beclin1, phosphatase-tensin homolog (PTEN), phosphatidylinositol 3-kinase (PI3K), protein kinase B (AKT), microtubule-associated protein 1 light chain 3 Ⅱ (LC3-Ⅱ) and microtubule-associated protein 1 light chain 3Ⅰ (LC3-Ⅰ) in gastric smooth muscle, and the ratio of LC3-Ⅱ/Ⅰ was calculated. Using the real-time polymerase chain reaction (RT-qPCR), the mRNA expression of microRNA-10b-5p (miR-10b-5p), PTEN, PI3K, and AKT was detected in gastric smooth muscle. With dual-luciferase reporter assay adopted, the targeting relationship between miR-10b-5p and PTEN was verified. Compared with the blank group, the model group showed the increase in blood glucose level (P<0.05), the decrease in gastric emptying rate and small intestinal propulsion rate (P<0.05), disrupted and disorganized gastric smooth muscle cell structure, elevated protein expression of p62 and Beclin1 and LC3-Ⅱ/Ⅰ ratio (P<0.05), reduced mRNA expression of miR-10b-5p (P<0.05), higher protein and mRNA expression of PTEN (P<0.05), and lower protein and mRNA expression of PI3K and AKT (P<0.05). When compared with the model group, the Yangming meridian point group exhibited the decrease in blood glucose level (P<0.05); both the Yangming meridian point group and the western medication group showed the increase in gastric emptying rates and small intestinal propulsion rates (P<0.05), relatively intact gastric smooth muscle cell structure, reduced protein expression of p62 and Beclin1, and LC3-Ⅱ/Ⅰ ratio (P<0.05); higher mRNA expression of miR-10b-5p (P<0.05), lower protein and mRNA expression of PTEN (P<0.05) and higher protein and mRNA expression of PI3K and AKT (P<0.05). Compared with the non-meridian and non-point group, in the Yangming meridian point group, blood glucose decreased (P<0.05), gastric emptying rate and small intestinal propulsion rate increased (P<0.05), the structure of gastric smooth muscle cells was relatively intact, the protein expression of p62 and Beclin1 and LC3-Ⅱ/Ⅰ ratio were reduced (P<0.05); the mRNA expression of miR-10b-5p was elevated (P<0.05), the protein and mRNA expression of PTEN was reduced (P<0.05), and the protein and mRNA expression of PI3K and AKT rose (P<0.05). When the PTEN wild-type (PTEN-WT) fluorescent plasmid was co-transfected with miR-10b-5p mimics, the relative luciferase activity decreased (P<0.001). The medicated-thread moxibustion of Zhuang medicine ameliorates the delayed gastric emptying in DGP rats, which may be related to its regulation of the miR-10b-5p/PTEN/PI3K/AKT signaling pathway, thereby inhibiting autophagy in gastric smooth muscle cells.

PMID 42864291
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PubMedMedical sciences (Basel, Switzerland)2026-09-24

Comparative Efficacy of Rebamipide, Pantoprazole, and Their Combination for Gastroprotection in Patients with Atrial Fibrillation Receiving Direct Oral Anticoagulants: The Randomized REGATA Study.

Vorobyeva Natalya M NM, Malaya Irina P IP, Zakiev Vadim D VD, Masharova Antonina A AA et al.

Background: Patients with atrial fibrillation (AF) receiving direct oral anticoagulants (DOAC) are at an elevated risk of gastrointestinal (GI) mucosal damage and bleeding. Proton pump inhibitors (PPI) are conventional gastroprotectors, but their efficacy in the lower GI tract is limited. This study evaluated the efficacy and safety of rebamipide monotherapy and combination pantoprazole-rebamipide (P + R) therapy compared to pantoprazole monotherapy in this vulnerable population. Methods: In the randomized, parallel-group, open-label, single-center REGATA trial, 210 AF patients receiving DOAC were randomized (1:1:1) to three gastroprotective regimens (n = 70 each) for 24 weeks: pantoprazole monotherapy, rebamipide monotherapy, or their combination. Efficacy analyses were performed in the per-protocol population (n = 118: pantoprazole, n = 36; rebamipide, n = 39; P + R, n = 43). The primary and secondary outcomes included composite clinical GI events (bleeding classified by ISTH/BARC, ulcers/erosions, and severe dyspepsia) and biomarkers of mucosal barrier function (fecal zonulin and calprotectin). Results: The incidence of primary efficacy endpoint events was 13.9% (n = 5; 95% CI: 3.1-25.7) in the pantoprazole group, 10.3% (n = 4; 95% CI: 2.3-21.1) in the rebamipide group, and 9.3% (n = 4; 95% CI: 2.1-18.6) in the P + R group, successfully confirming the non-inferiority hypothesis for both experimental arms within the pre-specified margin of 10% (p < 0.05). Multivariable regression analysis showed that compared with pantoprazole monotherapy, rebamipide monotherapy demonstrated an odds ratio OR of 0.71 (95% CI: 0.18-2.88, p = 0.630), while the P + R therapy was associated with an OR of 0.64 (95% CI: 0.16-2.57, p = 0.525). No major GI bleeding events or fatalities occurred; a single episode of GI bleeding (ISTH minor/BARC Type 2) was recorded in the pantoprazole arm (2.8%). Fecal calprotectin levels significantly decreased in the rebamipide group (by 37.6%, from 139 to 78 µg/g; p < 0.001) and the P + R group (by 50.0%, from 135 to 61 µg/g; p < 0.001), while no significant changes were observed in the pantoprazole group (p = 0.530). Concurrently, fecal zonulin levels, reflecting intestinal epithelial permeability, fell by 45.1% in the rebamipide arm (from 434 to 225 ng/mL; p < 0.001) and by 47.1% in the P + R arm (from 347 to 182 ng/mL; p < 0.001) compared to a minimal 3.0% fluctuation in the pantoprazole group. Conclusions: While demonstrating non-inferiority regarding primary clinical endpoints, both rebamipide monotherapy and combination (P + R) therapy achieved some advantages over pantoprazole monotherapy in decreasing subclinical GI inflammation and restoring intestinal epithelial barrier integrity.

PMID 42783438
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PubMedJournal of ethnopharmacology2026-09-23

Characterization of volatile oil constituents from Aurantii Fructus Immaturus (Zhishi) based on geographical origin, extraction method, and processing differences and its mechanism of ameliorating slow transit constipation via regulation of the PERK/CHOP-autophagy axis.

Zhao Wen-Yuan WY, Lin Gui-Mei GM, Bi Qiu-Ru QR, Li Hong-Ye HY et al.

Aurantii Fructus Immaturus (Zhishi) is traditionally used to treat constipation, and bran-frying moderates its drastic effects. Processing-related changes in volatile oil and their relationship with ER stress and autophagy in slow-transit constipation (STC) remain unclear. To characterize variations in Zhishi volatile oil by origin, extraction method, and bran-processing, and to investigate its effects in STC in relation to the PERK/CHOP-autophagy axis. Volatile oils from raw and bran-processed Zhishi of different origins were analyzed by HS-GC-MS and GC-MS. PCA, OPLS-DA, VIP, and GLM assessed influencing factors. Antioxidant activity was evaluated by DPPH· and ABTS•+ assays. Loperamide-induced STC rats received raw or processed oil, D-limonene, or mosapride. Defecation, intestinal propulsion, colonic histology, and biochemical and molecular markers were evaluated. Seventy-seven constituents were identified, with Jiangxi Zhishi showing the greatest diversity. Bran-frying decreased several monoterpene hydrocarbons, relatively enriched selected oxygenated constituents, and increased the number of detected constituents. Hydrodistillation produced the highest yield and diversity (P < 0.05). Processed oil showed stronger DPPH· scavenging activity than raw oil and D-limonene (P < 0.01); raw and processed oils had comparable ABTS•+ activity, and both outperformed D-limonene (P < 0.01). In STC rats, both oils improved defecation and intestinal propulsion, protected colonic tissue, increased c-kit, ATP, LC3B, 5-HT4R, and SOD, and decreased GRP78, CHOP, p-PERK/PERK, and MDA. Processed oil was more effective than raw oil, whereas D-limonene was weakest. Exploratory Spearman analysis linked selected VIP markers with pharmacodynamic endpoints, while D-limonene showed weak correlations. Origin, processing, and extraction method influence Zhishi volatile oil composition. Bran-frying enhanced antioxidant activity and therapeutic effects against STC, potentially through attenuation of PERK/CHOP-mediated ER stress, modulation of LC3B-associated autophagy-related processes and oxidative stress, protection of interstitial cells of Cajal, and modulation of 5-HT4R signaling.

PMID 42777984
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PubMedBiochemical and biophysical research communications2026-09-17

Transcriptomic analysis of rebamipide-induced gene expression changes toward anti-inflammatory profiles in human conjunctival fibroblasts.

Kinari Gen G, Tagami Mizuki M, Kira Yukimi Y, Haruna Yusuke Y et al.

Excessive conjunctival fibroblast proliferation is a major factor in postoperative scarring following ophthalmic surgery. While Rebamipide is clinically used for dry eye and has anti-inflammatory effects, its direct impact on the transcriptomic profiles and inflammatory signaling of conjunctival fibroblasts remains unclear. We aimed to elucidate the gene expression pathways by which Rebamipide modulates the inflammatory and fibrotic responses of Primary Human Conjunctival Fibroblasts (HCFCs). HCFCs were treated with Rebamipide at 0.054 mM (0.002%) or 0.54 mM (0.02%), which represent 1/1000 and 1/100 of the clinical dose (2%), or control media for 24 h. Global transcriptomic changes were analyzed using RNA-seq. Differential expression analysis (FDR < 0.05 and fold-change ≥ 2) was performed, followed by Ingenuity Pathway Analysis (IPA) to identify enriched pathways and upstream regulators. Key findings were validated at the protein level using immunofluorescence and Western blotting. In the functional assay, Rebamipide significantly and dose-dependently increased the metabolic activity and viability of conjunctival fibroblasts at concentrations between 0.054 mM and 1.08 mM, without inducing cytotoxicity. Concurrently, RNA-seq revealed significant dose-dependent gene alterations, with the 0.54 mM group showing the largest change. Rebamipide strongly inhibited pro-inflammatory pathways (TNF, IL1B, IL6) while activating cell cycle regulatory genes (TP53 at 0.054 mM and CDKN1A at 0.54 mM). Notably, the anti-fibrotic effect was associated with the marked downregulation of CSF3 (G-CSF) and other pro-inflammatory cytokines (CXCL6, CCL2, IL11). Mechanistically, the suppression of CSF3 is likely attributable to Rebamipide's modulation of NF-κB signaling, specifically through blockade of p65 nuclear translocation rather than a change in p65 phosphorylation status. Protein and immunofluorescence analyses supported the RNA-seq data, revealing a statistically significant reduction in Total NF-κB protein and a clear blockade of p65 nuclear translocation, which visually corresponded with the reduction in G-CSF expression. Rebamipide modulates the gene expression profile of HCFCs toward an anti-inflammatory and anti-fibrotic state, primarily through the downregulation of CSF3 and associated pro-inflammatory cytokines. These findings suggest Rebamipide's potential as a novel topical therapeutic strategy for reducing postoperative scarring and complications in transconjunctival surgery.

PMID 42753428
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PubMedKorean journal of ophthalmology : KJO2026-09-10

Comparative Efficacy of Diquafosol, Rebamipide, and Carboxymethylcellulose in Patients with Pre-existing Dry Eye Disease Undergoing Cataract Surgery.

Cho Myung Ho MH, Kim Jae Hyun JH, Lee Jong Soo JS

To compare the clinical efficacy of 3% diquafosol, 2% rebamipide, and 0.5% carboxymethylcellulose (CMC) in patients with pre-existing dry eye disease (DED) undergoing cataract surgery. This retrospective study included 75 eyes of 75 patients with DED undergoing cataract surgery, divided into diquafosol (n=25), rebamipide (n=25), and CMC (n=25, control) groups based on prescribed eye drops, administered four times daily from 2 weeks before surgery to 4 weeks after surgery. Tear film break-up time (TBUT), ocular surface staining, meibomian gland secretion (MGS), lid margin telangiectasia, Schirmer test, and Ocular Surface Disease Index (OSDI) were evaluated preoperatively and at 4 weeks postoperatively. All parameters improved significantly in all groups at 4 weeks (all p<0.001). Diquafosol showed greater improvement than CMC in TBUT and OSDI (p=0.001 and <0.001), and greater TBUT improvement than rebamipide (p=0.017); the difference in corneal staining did not reach significance in the overall three-group comparison (p=0.053). Rebamipide showed greater improvement than CMC in MGS (p=0.018), lid margin telangiectasia (p<0.001), Schirmer test (p=0.005), and OSDI (p=0.001), and greater improvement than diquafosol in lid margin telangiectasia and Schirmer test (p=0.002 and 0.036, respectively). Both diquafosol and rebamipide were more effective than CMC in stabilizing the ocular surface after cataract surgery in patients with pre-existing DED. Diquafosol is advantageous for rapid tear film stabilization, whereas rebamipide is associated with greater improvement in eyelid margin telangiectasia grade and meibomian gland secretory function, suggesting that perioperative eye drop selection should be individualized.

PMID 42717755
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