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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

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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PubMedNeurogastroenterology and motility2026-09-07

Exploring the Mechanism of Medicated Thread Moxibustion of Zhuang Medicine in Diabetic Gastroparesis Rats Based on the Enteric Nervous System.

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

Diabetic gastroparesis (DGP) is a common complication of diabetes mellitus, for which Western medicine treatments are associated with adverse effects and limitations. Enteric nervous system (ENS) injury is a core mechanism underlying this condition. Although Medicated Thread Moxibustion of Zhuang Medicine shows significant therapeutic efficacy, the specific mechanism by which it regulates the ENS to improve DGP remains unclear. A DGP rat model was established by intraperitoneal injection of streptozotocin (STZ) (60 mg/kg). The experimental animals were divided into five groups: control group, model group, mosapride citrate group, non-meridian and non-acupoint group, and Yangming meridian acupoint group. The Yangming meridian acupoint group received Medicated Thread Moxibustion of Zhuang Medicine at bilateral ST21, ST30, ST36, and ST40. Blood glucose, body weight, gastric emptying rate, and small intestinal propulsion rate were measured in each group. Hematoxylin-eosin (HE) staining was used to observe the histomorphology of the antrum and duodenum. Western blotting, immunofluorescence, and immunohistochemistry were performed to detect markers of enteric neurons (PGP9.5, ChAT, and neuronal nitric oxide synthase [nNOS]) and enteric glial cells (EGCs) (S100β, glial fibrillary acidic protein [GFAP], and Glial-cell line-derived neurotrophic factor [GDNF]). Following treatment with Medicated Thread Moxibustion of Zhuang Medicine at the Yangming meridian acupoints, DGP rats exhibited reduced blood glucose levels, restored body weight, increased gastric emptying rate and small intestinal propulsion rate, and ameliorated pathological damage in the gastric antrum and duodenum. Moreover, the expression levels of PGP9.5, ChAT, nNOS, S100β, GFAP, and GDNF were elevated. In addition, the glucose-lowering effect of this therapy was superior to that of mosapride citrate. Medicated Thread Moxibustion of Zhuang Medicine at the Yangming meridian acupoints effectively restores gastrointestinal motility in DGP rats by upregulating the expression of marker proteins of enteric neurons and EGCs, thereby ameliorating the morphological damage to both cell types.

PMID 42702763
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PubMedEuropean journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V2026-09-01

Rebamipide Nanosuspension Loaded In Situ Gel: A Promising Strategy to Improve Ocular Delivery and Treatment of Dry Eye Disease.

Rathod Sayali S, Vaiphei Klaudi K KK, Reddy Akhila A, Sree Amoolya A et al.

Rebamipide (REBA) is used in the treatment of dry eye disease (DED) and is available as Mucosta® ophthalmic suspension that is widely used in Japan. However, certain challenges such as blurred vision, less permeation due to large particle size, frequent administration because of nasolacrimal drainage, and bitter taste were observed after topical instillation. So, in this study, rebamipide nanosuspension (REBA-NS) bearing in-situ gel (REBA-NS gel) was developed for addressing the challenges as well as ease of application. REBA-NS was prepared using the acid-base neutralization method, employing HPMC as a stabilizer and optimized using the quality-by-design approach. Further characterization and evaluation of REBA-NS was carried out, and the optimized REBA-NS was loaded to gel using gellan gum, which has a property of forming an in-situ gel after contact with the simulated tear fluid. Finally, the in-vitro and in-vivo studies of the REBA-NS gel were performed. REBA-NS exhibited nanosized particles (<270 nm) that may help in enhanced permeation, low polydispersity index (<0.25) with high drug content (>80%). Moreover, the REBA-NS gel exhibited mucoadhesiveness, sustained drug release, sterile nature, optimum pH (∼7.2), and osmolality (∼216 mOsm/kg) required for ocular administration, which may aid in the retention of REBA. Finally, REBA-NS gel on the DED-induced rats depicted an increased tear secretion and decreased corneal fluorescein scoring by 1.39-folds and 9.12-folds, respectively, compared to the REBA solution on day 7 of treatment. In a nutshell, REBA-NS gel was found to be a promising approach for treating DED.

PMID 42680015
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PubMedTerapevticheskii arkhiv2026-08-21

[Efficacy and safety of H. pylori eradication therapy in real-world clinical practice: results of the «PAMIR» observational program].

Alexeev N Y NY, Astaf'eva T O TO, Vishnevskaya V V VV, Donchenko N D ND et al.

To evaluate the efficacy, safety and impact on gastrointestinal symptoms of Helicobacter pylori eradication therapy with a ready-to-use set of tablets and capsules [omeprazole 20 mg × 2, clarithromycin 500 mg × 2, amoxicillin 500 mg × 4] (Pylobact® AM) in duodenal ulcer patients within the framework of an observational program. 912 H. pylori-positive patients were included (404 men and 508 women, average age - 43.8 years (43.82±11.39; 18-64 years). Symptoms were assessed using the Gastrointestinal Symptom Rating Scale (GSRS) questionnaire; patients assessed treatment satisfaction, and physicians assessed treatment efficacy and tolerability using a five-point Likert scale. The efficacy of H. pylori eradication was assessed using the results of the 13C-urea breath test, H. pylori antigen stool test, or a rapid urea test with biopsies of the gastric body and antrum obtained during upper endoscopy. A total of 870 patients completed the observational program: 538 patients in the standard triple therapy group (PAM group) and 332 patients in the group enhanced with a bismuth preparation, rebamipide, and/or a probiotic (PAMplus group). A subgroup of patients received triple therapy with bismuth and the synbiotic complex of Floriose with probiotic strains Lactobacillus acidophilus La-14, Lactobacillus rhamnosus Lr-32, Bifidobacterium lactis Bl-04, inulin and B vitamins. H. pylori eradication rates in the PAM, PAMplus, and PAM+Bi+F (ITT) groups were 90.6, 97.03, and 96.82%, respectively. Treatment significantly reduced GSRS abdominal pain scores. Physicians rated the treatment efficacy and tolerability as "very good" or "good" at the end of the program in 93.3% of patients. Patients rated 93.68% as completely or mostly satisfied with the treatment. The effectiveness of H. pylori eradication with a ready-to-use set of capsules and tablets for standard triple therapy is ensured by high patient compliance. The combination of standard triple therapy with bismuth, probiotics, and/or rebamipide increases treatment efficacy.

PMID 42625536
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PubMedInternational immunopharmacology2026-08-13

Retraction notice to "Rebamipide protects against experimentally induced intestinal ischemia/reperfusion-promoted liver damage: Impact on SIRT1/β-catenin/FOXO1and NFκB signaling" [Int. Immunopharmacol. 119 (2023) 110269].

Elwany Nisreen E NE, Salem Amal El AE, Mohamed Noura Mostafa NM, Khalil Sama S SS et al.

PMID 42595644
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PubMedMolecular psychiatry2026-08-02

Mosapride promotes internalization of a TREK1-HTR4 complex and exerts rapid antidepressant-like effects.

Lee Soomin S, Kim Seung Chan SC, Noh Junyeol J, Seo Gyunghwa G et al.

Major depressive disorder (MDD) remains a critical global health burden, and a substantial proportion of patients exhibit insufficient responses to conventional monoaminergic antidepressants. Selective inhibition of the two-pore domain potassium channel TREK1 has emerged as a promising antidepressant strategy; however, the regulatory mechanisms controlling TREK1 trafficking-particularly its functional coupling with G protein-coupled receptors (GPCRs)-remain poorly understood. Here, we established a cell-based screening platform using a biomolecular luminescence complementation (BiLC) assay to monitor agonist-induced changes in membrane-associated TREK1. Using this platform, we identified a TREK1-5-hydroxytryptamine receptor 4 (HTR4) complex in vitro and in native hippocampal tissues using biomolecular fluorescence complementation (BiFC), co-immunoprecipitation (Co-IP), and proximity ligation assays (PLA). Live-cell imaging demonstrated that treatment with the HTR4 agonist mosapride induces redistribution/internalization of a plasma membrane-associated TREK1-HTR4 pool into intracellular compartments. Electrophysiological recordings further confirmed that mosapride reduces TREK1 channel activity in an HTR4-dependent manner. In vivo, oral administration of mosapride for five days ameliorated lipopolysaccharide (LPS)-induced depressive-like behaviors in mice and preserved markers associated with hippocampal neurogenesis. Notably, viral expression of the TREK1 C-terminal interaction domain (C1), which competitively disrupts the TREK1-HTR4 complex, attenuated the neurogenic and behavioral effects of mosapride, supporting a causal role of TREK1 regulation in mediating these antidepressant-like actions. Collectively, our findings reveal a previously unrecognized mechanism in which HTR4 dynamically regulates TREK1 trafficking and function, and they highlight GPCR-based modulation of TREK1 as a potential therapeutic strategy for depressive disorders.

PMID 42542439
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