Mucosta ophthalmic suspension (rebamipide ophthalmic) / Otsuka, Kubota - LARVOL DELTA

Effects of Rebamipide for Dry Eye on Optical Quality and Efficacy: A Systematic Review and Meta-Analysis. (PubMed, J Ocul Pharmacol Ther) - "Purpose: To evaluate the effects of rebamipide ophthalmic suspension on optical quality and efficacy of patients with dry eye under different conditions... These results indicate a significant improvement in the efficacy of rebamipide treatment for patients with dry eye, particularly for those wearing SCL. The effect of rebamipide on visual quality was found to correlate with the underlying dry eye status."

Journal • Retrospective data • Review • Dry Eye Disease • Ophthalmology

Comparing two mucin secretagogues for the treatment of dry eye disease: a prospective randomized crossover trial. (PubMed, Sci Rep) - "Thirty patients with DED were randomly treated with either 3% diquafosol or 2% rebamipide ophthalmic solution for 4 weeks, followed by an additional 4-week treatment using the other eye drop after a 2-week washout period. The self-efficacy of both drugs and overall satisfaction scores were comparable. These findings indicate that two mucin secretagogues showed comparable effects in ameliorating symptoms and improving signs (TBUT, corneal and conjunctival staining) in patients with DED."

Clinical • Journal • Dry Eye Disease • Ophthalmology • MMP9

Enhancing Corneal Drug Penetration Using Penetratin for Ophthalmic Suspensions. (PubMed, Biol Pharm Bull) - "In an ex vivo porcine eye model, the addition of 10 µM PNT to rebamipide ophthalmic suspension markedly improved the corneal uptake of rebamipide; however, the addition of 100 µM PNT was ineffective due to potentially increased particle size by aggregation. This article provides basic information on the application of PNT as a penetration enhancer in ophthalmic suspensions, including the in vitro and ex vivo studies mentioned above, as well as the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay and storage stability at different pH values."

Journal • Ophthalmology

The Efficacy and Safety of Rebamipide Ophthalmic Suspension (OPC-12759) in Patients with Dry Eye Disease: A Systematic Review of Randomized Controlled Trials. (PubMed, J Clin Med) - "Adverse events (AEs) were 5.2 ± 7.6% superior in the REB group, with an overall compliance > 95%. Therefore, REB ophthalmic suspension is a safe and effective treatment that could be recommended in patients with DED."

Journal • Review • Anesthesia • Dry Eye Disease • Ophthalmology

Efficacy and safety of topical 2% rebamipide ophthalmic suspension in dry eye disease at tertiary care centre. (PubMed, Indian J Ophthalmol) - "Rebamipide 2% ophthalmic suspension showed significant improvement in symptoms and signs of dry eye. It able to modify epithelial cell function, improve tear stability, and suppress inflammation suggests that it may be a first drug of choice for severe dry eye disease."

Journal • Dry Eye Disease • Inflammation • Ocular Inflammation • Ophthalmology

The Effect of Rebamipide on Refractive Accuracy of Cataract Surgery in Dry Eye Patients (ASCRS-ASOA 2022) - "This study investigated the effect of 2% rebamipide ophthalmic suspension on the predicted refractive accuracy for cataract surgery in patients with dry eye...The degree of improvement of the central part of the cornea and corneal higher-order aberrations showed a significant positive correlation with the degree of improvement in the accuracy of P-SE (p < 0.01). Conclusion Rebamipide significantly improved the corneal surface condition and accuracy of the predicted postoperative refraction in dry eyes._x000D_ Preoperative dry eye treatment with rebamipide may be an option for improving the accuracy of IOL calculation, particularly when using more refractive error-sensitive IOLs, such as trifocal IOLs."

Clinical • Cataract • Dry Eye Disease • Ophthalmology

The Effect of Rebamipide on Refractive Accuracy of Cataract Surgery in Patients with Dry Eye. (PubMed, Ophthalmol Ther) - "Rebamipide significantly improved the corneal surface condition and accuracy of the predicted postoperative refraction in dry eyes."

Journal • Cataract • Dry Eye Disease • Ophthalmology

Benzalkonium Chloride-Induced Corneal Epithelial Injury in Rabbit Reduced by Rebamipide. (PubMed, J Ocul Pharmacol Ther) - "Findings by FL staining were consistent with those by CR; BAK and latanoprost with BAK groups were positive, and eyes with the most severe area and density of corneal epithelial damage (A2D2) were in the saline/BAK group. The rebamipide ophthalmic solution reduces the severity of corneal epithelial injury caused by BAK, an ophthalmic solution preservative."

Journal • Preclinical • Corneal Abrasion • Ophthalmology

Effects of Rebamipide on Differences in Power and Axis of Corneal Astigmatism Between Two Intra-patient Keratometric Measurements in Dry Eyes. (PubMed, Ophthalmol Ther) - "In dry eyes with short TBUTs, rebamipide significantly improved the corneal surface condition and significantly reduced intra-patient discrepancies in astigmatism power and axis measurements. Rebamipide may improve the accuracy of intraocular lens (IOL) power calculations in dry eyes, particularly when toric IOLs are implanted."

Clinical • Journal • Astigmatism • Dry Eye Disease • Ophthalmology

Effect of Rebamipide Ophthalmic Suspension on Deviation of Keratometry Measurements in the Short Break-up Time Type of Dry Eye (ASCRS-ASOA 2021) - "ConclusionIn the short BUT type of dry eyes, rebamipide significantly improved corneal condition and reduced the deviation of the power of astigmatism in two individual measurements. The administration of rebamipide may improve the accuracy of IOL power calculation for short BUT type of dry eye, especially when the implantation of toric IOLs are considered."

Astigmatism • Dry Eye Disease • Ophthalmology

Assessment of mucin-related gene alterations following treatment with rebamipide ophthalmic suspension in Sjögren's syndrome-associated dry eyes. (PubMed, PLoS One) - "MUC16 mRNA levels were significantly decreased from baseline levels at 4 and 8 weeks post-treatment. Ocular surface test using impression cytology is a clinically useful tool for assessing mucous conditions on the ocular surface and can be used to determine the effects of instillation treatment with eye drops that affect mucin production at the ocular surface."

Journal • Dry Eye Disease • Immunology • Ophthalmology • Sjogren's Syndrome

Novel Sustained-Release Drug Delivery System for Dry Eye Therapy by Rebamipide Nanoparticles. (PubMed, Pharmaceutics) - "The commercially available rebamipide ophthalmic suspension (CA-REB) was approved for clinical use in patients with dry eye; however, the residence time on the ocular surface for the traditional formulations is short, since the drug is removed from the ocular surface through the nasolacrimal duct...Moreover, the REB-NPs increased the mucin levels in the lacrimal fluid and healed tear film breakup levels in an N-acetylcysteine-treated rabbit model. The information about this novel DDS route and creation of a nano-formulation can be used to design further studies aimed at therapy for dry eye."

Journal

The Effects of Rebamipide 2% Ophthalmic Solution Application on Murine Subbasal Corneal Nerves After Environmental Dry Eye Stress. (PubMed, Int J Mol Sci) - "In addition, the subbasal nerve fiber density was significantly higher and the DC density was significantly lower in the 2% rebamipide group than in the HA group. Overall, the topical rebamipide ophthalmic solution showed more favorable therapeutic effects when compared to the HA ophthalmic solution in a mouse model of EDES, likely owing to its anti-inflammatory and neuroprotective effects."

Journal • Preclinical

Prevalence of dry eye after cataract surgery: the effect of topical rebamipide treatment (ESCRS 2019) - "Purpose: To investigate the prevalence of dry eye after cataract surgery and the effects of 2% rebamipide ophthalmic solution on postoperative dry eye... Rebamipide has a capability to improve dry eye symptoms after cataract surgery. Subjective dry eye symptoms, which can be easily masked by cataract symptoms before surgery, seemed to become apparent after cataract surgery."

Rebamipide ophthalmic solution modulates the ratio of T helper cell 17/regulatory T cells in dry eye disease mice. (PubMed, Mol Med Rep) - "Furthermore, the increased Th17 and Treg levels were restored following treatment with rebamipide. In conclusion, the anti‑inflammatory and Th17/Treg balance‑preserving effects of rebamipide may contribute to the treatment of DE in mice."

Journal • Preclinical

Retrospective Observational Study on Rebamipide Ophthalmic Suspension on Quality of Life of Dry Eye Disease Patients. (PubMed, J Ophthalmol) - "The DEQS is a useful questionnaire that can assess the severity of the DED symptoms and their impact on the QOL. This trial is registered with UMIN000024405."

HEOR • Journal • Observational data • Retrospective data

The Effect of Rebamipide Ophthalmic Solution on Cytokine and Mucin Secretion in Culture of Conjunctival Epithelial Cells From the Cu, Zn-Superoxide Dismutase-1 (SOD-1) Knock-Down Mouse. (PubMed, Eye Contact Lens) - "Rebamipide seems to increase MUC5AC levels and suppress inflammation by decreasing IL-6 levels in mouse conjunctival epithelial cell cultures. SOD-1 siRNA-treated mouse conjunctival epithelial cell culture is a practical method for investigating changes in mucosa-associated mucins and proinflammatory cytokines in response to therapeutic interventions."

Journal • Preclinical

Severe Dry Eye With Combined Mechanisms is Involved in the Ocular Sequelae of SJS/TEN at the Chronic Stage. (PubMed, Invest Ophthalmol Vis Sci) - "...For the treatment of dry eye in SJS, it is important to suppress chronic inflammation on the ocular surface, and 2% rebamipide ophthalmic solution reportedly helps to obtain ocular surface stabilization. Scleral contact lenses, as well as the newly developed limbal-rigid contact lenses, improve the patients' visual acuity and reduce symptoms related to severe dry eye. Further studies and new therapeutic methods are needed to more effectively treat dry eye in patients afflicted with SJS/TEN."

Journal

Tear Film-Oriented Diagnosis and Tear Film-Oriented Therapy for Dry Eye Based on Tear Film Dynamics. (PubMed, Invest Ophthalmol Vis Sci) - "In December 2010 and January 2012, 3% diquafosol sodium ophthalmic solution and 2% rebamipide ophthalmic suspension, respectively, appeared first in Japan as prescription drugs for the treatment of dry eye (DE). In Japan, TF breakup is regarded as a visible core mechanism for DE, and an abnormal breakup time (i.e., ≤5 seconds) and symptoms are currently used for the diagnosis of DE. Therefore, TFOD and TFOT could be an ideal and practical pathway for clinicians to manage DE."

Journal

Rebamipide promotes lacrimal-duct epithelial cell survival via protecting the barrier function (ARVO 2019) - "...We previously reported that rebamipide ophthalmic suspension, marketed in Japan for the treatment of dry eye, has a protective effect against cultured corneal epithelial cell damage...Immunohistochemical analysis revealed that tight junction protein zonula occludens (ZO)-1, claudin (CLDN)-1, and CLDN-7 were also disrupted in the BAC and the placebo vehicle injected groups, whereas those expressions were expressed in the group injected with BAC and rebamipide. Conclusions Rebamipide protected LDECs via an anti-inflammatory effect and preserved the barrier function, thus suggesting that rebamipide may prevent the death of LDECs due to inflammation."

Dry eye drugs: New approaches to an old problem (Review of Optometry) - "CyclASol is a promising cyclosporine that uses a non-aqueous perfluorobutylpentane technology based on semifluorinated alkanes. This formulation may improve bioavailability of CsA and onset of efficacy. In a Phase II study, CyclASol showed a significant reduction in corneal and conjunctival staining compared with both the vehicle and Restasis with an onset of effect at two weeks."

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