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

✓ Approved

Ildong Pharmaceutical · HTR3A · 小分子

什么是 mosapride + rebamipide？

mosapride + rebamipide 是一种小分子，由Ildong Pharmaceutical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MotiReb, Mucosta + Gasmotin, MR tablet
公司Ildong Pharmaceutical
药物类别小分子
分子靶点HTR3A, HTR4
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Ildong Pharmaceutical

作用机制

分子靶点

mosapride + rebamipide 作用于 2 个分子靶点：

HTR3A5-hydroxytryptamine receptor 3A (5-HT3R, 5-HT-3)
HTR45-hydroxytryptamine receptor 4 (5-HT4, 5-HT4R)
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

mosapride + rebamipide 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 disordersDyspepsia✓ Approved

相关研究文献

PubMedRevista espanola de enfermedades digestivas2026-10-26

Partial regression of a refractory gastric ulcer following abdominal radiotherapy during a sofalcone-containing combination regimen.

Guo Zhong-Wei ZW, Zhang Jin-Xuan JX, Li Han-Chuan HC, Chang Xin-Yao XY et al.

Radiation-induced gastric ulcer is uncommon but can be persistent and difficult to heal, particularly in patients receiving ongoing multimodality cancer treatment. We report a 68-year-old man with pancreatic ductal adenocarcinoma who developed a refractory antral ulceration after upper abdominal radiotherapy during intermittent chemotherapy. High-dose pantoprazole, rebamipide, Kangfuxin liquid, and subsequent vonoprazan achieved bleeding control but failed to induce healing. After sofalcone was added, postprandial pain improved substantially, and serial endoscopy showed regression of the ulcer from 2.0×1.8 cm to 0.6×0.8 cm. This case highlights the therapeutic challenge of post-radiation gastric ulceration and supports further study of repair-directed therapy.

PMID 42929252
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PubMedCureus2026-10-25

Comparative Effectiveness and Safety of Rebamipide Versus Diquafosol in the Treatment of Dry Eye Disease: A Systematic Review and Meta-Analysis.

Iqbal Mehreen M, Rehman Huzaifa H, Bhurgri Allah Rakhio AR, Abera Daniel D et al.

This systematic review and meta-analysis aimed to compare the efficacy and tolerability of rebamipide (REB) and diquafosol (DQS), two widely used mucin secretagogues, in the treatment of dry eye disease. A comprehensive search of PubMed, Embase, Web of Science, Cochrane CENTRAL, and Scopus was conducted following Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines, identifying six comparative studies enrolling 277 patients across South Korea and Japan. Pooled analyses were performed using random-effects models, standardized mean differences (SMDs) for continuous outcomes and risk ratios (RRs) for dichotomous outcomes with 95% confidence intervals (CIs). Tear break-up time showed no significant difference between REB and DQS (SMD = -0.21 seconds, 95% CI: -0.52 to 0.11, p=0.20). Subjective symptom scores were also comparable (SMD=0.11, 95% CI: -0.16 to 0.38, p=0.40). Corneal staining scores were nearly identical (SMD=-0.002, 95% CI: -0.324 to 0.321, p=0.993), while conjunctival staining showed a nonsignificant trend favoring REB (SMD=-0.403, 95% CI: -1.508 to 0.702, p=0.475, I²=87.6%). These findings suggest comparable efficacy between both agents as first-line mucin secretagogues in the available studies, though formal equivalence cannot be established from this evidence base, and more large-scale trials are required to validate the findings.

PMID 42927075
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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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