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PURPOSE To evaluate whether allergic conjunctivitis (AC) could be induced by Acanthamoeba excretory-secretory protein (ESP) and analyze the therapeutic effect of resolvin (Rv) D1 and antiallergic agents. METHODS Human conjunctival epithelial cells (HCVCs) were treated with 10 µg/well of ESP, and Th2 cytokines were measured using real-time PCR. C57BL/6 mice were treated with 10 µg/5 µL of ESP after sensitization, and conjunctivas isolated from the mice were stained with hematoxylin and eosin (H&E) for the analysis of eosinophils and periodic acid-Schiff (PAS) for the analysis of goblet cells. Cytokine levels in the eye-draining lymph nodes (dLNs) and spleens were measured using the enzyme-linked immunosorbent assay (ELISA). Then, the treatment effects of RvD1 and the antiallergic agents (olopatadine, bepotastine, and alcaftadine) on the HCVCs, mouse conjunctivas, dLNs, and spleens were assessed. RESULTS Th2 cytokines were increased in the ESP-treated conjunctival cells. Mouse conjunctivas treated with ESP showed significant infiltration of eosinophils and goblet cells, and the dLN and spleen exhibited increased IL-4, IL-5 and IL-13 levels. All findings were significantly decreased upon treatment with RvD1 and the antiallergic agents. CONCLUSIONS Acanthamoeba could be used to establish an animal model of AC, which could be effectively treated with RvD1 or topical antiallergic agents.

Bepotastine besilate (1, Figure 1, synonymous with bepotastine besylate), is a non-sedative highly selective histamine receptor antagonist, which has a stabilizing effect on mast cells. This antihi...

Introduction: Chronic urticaria is common and distressing dermatosis where the search for newer agents with improved effectiveness and tolerability profile is a felt need. Bepotastine, a second-generation antihistamine, with added effect on suppression of eosinophil migration has a prospect in the management of chronic urticaria. Aims: To assess and compare effectiveness and safety of bepotastine versus levocetirizine in chronic urticaria. Materials and Methods: Single-center, investigator-blind, randomized, active-controlled, parallel-group phase IV trial (CTRI REF/2018/04/019692) conducted on adult patients of chronic urticaria of either sex. Patients were randomized into receiving either bepotastine besilate 10 mg tablet twice daily or levocetirizine 5 mg tablet once daily with fortnightly follow-up for 6 follow-up visits after thebaseline evaluation. The primary outcome measures were Urticaria Activity Score 7 (UAS7) and Urticaria Total Severity Score (TSS). Routine hematological, biochemical tests, treatment-emergent adverse events were monitored for safety. Results: Thirty patients in the bepotastine group and 29 patients in the levocetirizine group were analyzed by modified-intention-to-treat criteria. The study groups were comparable at the baseline with respect to the severity of chronic urticaria. UAS7 and TSS reduced significantly (P < 0.001, Friedman's ANOVA) in both treatment groups from 1st follow-up visit and 2nd follow-up visits (P < 0.05, Post Hoc Dunn's test) At the test-of-cure visit, UAS7 (5.13 ± 8.21 vs 7.48 ± 8.96) and TSS (5.10 ± 4.06 vs 7.07 ± 4.48) were less with bepotastine than levocetirizine although not statistically significant (P = 0.188 and 0.073, respectively, Mann–Whitney U test). Sedation during daytime was found to be significantly more (P < 0.001, Fischer's exact test) with levocetirizine than bepotastine (73.3% vs 17.2%). Conclusion: Bepotastine is comparable to levocetirizine with respect to its effectiveness with an edge in terms of side-effect (sedation during day time); thus, it offers a new therapeutic option in chronic urticaria.

Background To investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents (alcaftadine 0.25%, bepotastine besilate 1.5%, and olopatadine HCL 0.1%) on human corneal epithelial cells (HCECs) and their anti-allergic effects on cultured conjunctival epithelial cells. Methods A Methylthiazolyltetrazolium(MTT)-based calorimetric assay was used to assess cytotoxicities using HCECs at concentrations of 10, 20 or 30% for exposure durations of 30 min, 1 h, 2 h, 12 h or 24 h. Cellular morphologies were evaluated by inverted phase-contrast and electron microscopy. Wound widths were measured 2 h, 18 h, or 24 h after confluent HCECs monolayers were scratched. Realtime PCR was used to quantify anti-allergic effects on cultured human conjunctival cells, in which allergic reactions were induced by treating them with Aspergillus antigen. Results Cell viabilities decreased in time- and concentration-dependent manners. Cells were detached from dishes and showed microvilli loss, cytoplasmic vacuoles, and nuclear condensation when exposed to antiallergic agents; alcaftadine was found to be least cytotoxic. Alcaftadine treated HCECs monolayers showed the best wound healing followed by bepotastine and olopatadine (p p Conclusions Alcaftadine seems to have less side effects and better therapeutic effects than the other two anti-allergic agents tested. It may be more beneficial to use less toxic agents for patients with ocular surface risk factors or presumed symptoms of toxicity.

BACKGROUND The efficacy of rupatadine for the treatment of AR has been confirmed in numerous clinical studies, however there are very few studies on asian patients. OBJECTIVE To assess the safety and efficacy of rupatadine fumarate in the treatment of Korean perennial allergic rhinitis (PAR) patients. METHODS A multicenter, double-blind, randomized, placebo-controlled, comparative study of rupatadine fumarate and bepotastine besilate was conducted. Each group was administered rupatadine, bepotastine or placebo for 4 weeks. Primary parameters for efficacy included morning and evening symptom reduction from baseline at 4 weeks. Treatment safety and tolerability were evaluated according to a self-reported incidence and type of adverse events at each follow up visit. RESULTS Rupatadine showed a significant reduction in symptoms at morning and evening evaluations, in both 5TSS (-5.69, P < 0.0006) and 4NTSS (-4.74, P < 0.0015) compared to placebo. There was a significant reduction from baseline for 5TSS (-65.4%, P = 0.002) and 4NTSS (-63.7%, P = 0.003) with rupatadine compared with placebo. At evening evaluations, there were significant reductions of 5TSS (-63.2%, P = 0.009) and 4NTSS (-61.6%, P = 0.013) for the rupatadine group. Compared with bepotastine, rupatadine showed greater reduction in the morning symptoms at 4 weeks. When individual symptoms were assessed with 12-hour reflective mean daily symptom score, rupatadine showed better efficacy than placebo in sneezing (P = 0.016) and rhinorrhea (P = 0.097). The rate of adverse events showed no statistical significance. CONCLUSIONS Rupatadine is a safe and effective treatment option for Korean PAR patients and possibly a better choice over bepotastine for controlling morning symptom.

INTRODUCTION: Vernal conjunctivitis comprises 0.5% of allergic eye diseases. The study is intended to collate the effectiveness of drugs by observing the reduction in signs and symptoms. OBJECTIVES: The objective of the study is to evaluate the effectiveness and safety of olopatadine 0.1% ophthalmic drops with bepotastine besilate 1.5% ophthalmic drops in patients with vernal keratoconjunctivitis (VKC). MATERIALS AND METHODS: A randomized, open-label, comparative study conducted in Sarojini Devi Eye Hospital, Telangana. The study included 50 patients diagnosed with VKC, of which Group A and Group B were given olopatadine 0.1% ophthalmic drops and bepotastine besilate 1.5% ophthalmic drops, respectively, twice a day for 8 weeks. The reduction in signs and symptoms in both groups was compared. The observations and results were tabulated accordingly, and data were analyzed using the SPSS. The unpaired t-test is used as the test of significance in between two groups. P value is statistically significant when it is less than 0.05. RESULTS: Overall, 50 cases were included in the study, 72% of total patients were in the age group of 5–10 years, and 28% were in the age group of 11–15 years. There were 39 males and 11 females. After 8 weeks of follow-up, the mean reduction in the scoring of symptoms and signs provided better and quicker relief of watering, ocular discomfort, and conjunctival hyperemia with bepotastine 1.5% eye drops. Olopatadine 0.1% eye drops provided faster improvement in papillary hypertrophy. Both drugs were equally effective in reducing itching. Laboratory findings of absolute eosinophil count had no statistical significance in between the two groups. CONCLUSIONS: In this study, based on the evaluation of therapeutic performance, bepotastine eye drops proved quicker relief of symptoms and signs compared to olopatadine eye drops but was not statistically significant which would prove beneficial for the patients.

OBJECTIVES/HYPOTHESIS To evaluate the efficacy and safety of a slow-release form of bepotastine salicylate (HL151, Belion CR) in patients with perennial allergic rhinitis (PAR). STUDY DESIGN Double-blind, placebo-controlled multicenter comparative study. METHODS Two hundred seventy-two PAR patients (aged 19-65 years) were studied to determine the efficacy and safety of HL151 (20 mg once daily administration) relative to those of a placebo in terms of improvements in total and nasal symptom scores. The subjects were randomized to the placebo (n = 138) or HL151 group (n = 134, 20 mg orally once daily for 4 weeks), and reflective and instantaneous total nasal symptom scores (TNSS) were measured daily in comparison with baseline. Among 272 subjects, 229 subjects (119 in the placebo group, 110 in the HL151 group) who completed the study were included for efficacy analysis. RESULTS Instantaneous and reflective TNSS and nasal symptoms such as rhinorrhea, nasal itching, and sneezing at 2 and 4 weeks showed that HL151 was superior to the placebo (all P

Purpose: With increasing environmental pollution, the incidence of allergic conjunctivitis is increasing. Newer anti-allergic medications with combined anti-histaminic and mast cell stabilization action can help reducing the use of topical steroids for milder form of disease. There is no study directly comparing olopatadine (0.1%), bepotastine (1.5%), and alcaftadine (0.25%) for mild to moderate allergic conjunctivitis cases. Hence, we decided to methodically study the efficacy of three topical medications. Methods: Prospective, observer-masked clinical trial enrolled 45 patients with 15 patients in each of the three groups. Patients with mild to moderate allergic conjunctivitis were sequentially assigned to respective groups, and relief of symptoms and signs were noted upto 1-month follow-up. Results: All three topical medications faired almost equally in resolving symptoms of the patients with mild to moderate allergic conjunctivitis, and most of them reported complete relief after 1 week of use of medication. Few cases with limbal or palpebral papillae reported symptomatic relief after use of medication, but the resolution of these signs was not noted in all three groups. Conclusion: We concluded similar efficacy of three medications in relieving symptoms and inefficacy in regressing palpebral and limbal papillae in cases of allergic conjunctivitis.

Bepotastine besilate (BB) is a second-generation H1-antihistamine that, as an ophthalmic solution, is approved in the United States by the Food and Drug Administration (FDA) for the treatment of allergic conjunctivitis. In other countries, the oral presentation of BB is widely used for the improvement of symptoms of allergic rhinitis (AR) as well as urticaria and chronic pruritus with results similar to those by other drugs of the same class. Areas covered: This article was created from a comprehensive literature search with information taken from clinical trials. The articles that have been selected evaluate the clinical and non-clinical pharmacology of BB as well as its use in AR and its efficiency in the improvement of symptoms, its safety, common adverse effects, and overall experiences of its use. Expert opinion: BB is effective and well-tolerated in the treatment of allergic rhinitis. Side effects are infrequent in patients with AR who do not have kidney or liver disease. Clinical trial experience with oral bepotastine outside the United States has confirmed its safety. BB can be useful as a therapeutic option in patients with AR who would like to explore an alternative to the currently available once-daily oral H1-antihistamines.

Significant histamine H1 receptor occupation in the central nervous system (CNS) is associated with sedation. Here we examined the time profiles of the H1 receptor occupancy (RO) in the CNS using sedative (diphenhydramine and ketotifen) and non-sedative (bepotastine and olopatadine) antagonists at their therapeutic doses by integrating in vitro and animal data. A pharmacokinetic model was constructed to associate plasma concentrations and receptor binding in the brain. Dissociation and association rate constants with the H1 receptor and plasma and brain unbound fractions were determined in vitro. Passive and active clearances across the blood–brain barrier (BBB) were estimated based on physicochemical properties and microdialysis studies in mice and monkeys. The estimated RO values were comparable with the reported values determined at time to maximum concentration (Tmax) of plasma by positron-emission tomography in humans. The simulation suggested that the predicted maximum ROs by bepotastine and olopatadine were greater than the reported values. Sensitivity analysis showed that active transport across BBB had a significant impact on the RO duration of the H1 antagonists examined. The present study demonstrated that modeling and simulation permits a reasonable RO estimation in the human CNS. Our findings will facilitate the development of CNS-acting drugs.

Bepotastine (BPT) is a H1-receptor antagonist. It is used as a besilate salt in ophthalmic solution for allergic conjunctivitis and orally for the treatment of allergic rhinitis and urticaria/pruritus. Its systematic forced degradation study is unreported. The same was carried out in different conditions prescribed by International Conference on Harmonisation. The stressed solutions were subjected to reversed phase liquid chromatographic analysis, and BPT was observed to be labile under photobasic condition only, yielding 5 photodegradation products. The structures of the latter were elucidated from data generated by liquid chromatography-high-resolution mass spectrometry and multistage mass spectrometry. Of the 5, 4 products were further isolated and subjected to nuclear magnetic resonance spectroscopy to justify the proposed structures. Two of them, with similar accurate mass, were additionally and unambiguously characterized from their heteronuclear multiple bond correlation data, hydrogen deuterium exchange mass data, and quantum chemical analysis using density functional theory calculations. One degradation product had a structure that could only be explained by unusual rearrangement involving conversions of N-oxide into hydroxylamine, similar to Meisenheimer rearrangement. The physicochemical, as well as absorption, distribution, metabolism, excretion, and toxicity properties of BPT and its characterized photodegradation products were evaluated in silico by ADMET Predictor™ software.

Second-generation antihistamines are widely prescribed for the control of symptoms of allergic inflammation such as itchy hives, coryza, and itchy eyes. In rare circumstances, these drugs might provoke allergic inflammation. Hypersensitivity to bepotastine besilate, a second-generation antihistamine has never been reported. A 17-year-old schoolgirl, whose paroxysmal itchy hives had been controlled with bepotastine, experienced aggravation of the hives. An oral provocation test confirmed her hypersensitivity to bepotastine and cross-reactivity to levocetirizine. She showed no reaction to chlorpheniramine, ketotifen, or olopatadine among the 13 antihistamines tested. While searching for an antihistamine to control her itchy hives, we found that she also exhibited cross-reactivity to various antihistamines with different chemical structures from that of bepotastine, which is not predicted according to the chemical classification of antihistamines. We report a case of hypersensitivity to bepotastine besilate in a patient with chronic spontaneous urticaria.

Purpose: To compare the efficacy and safety of Alcaftadine 0.25%, Olopatadine hydrochloride 0.2%, and Bepotastine besilate 1.5% ophthalmic solutions in the treatment of allergic conjunctivitis. Methods: This is a prospective, observer-masked, comparative study of 180 patients with mild to moderate allergic conjunctivitis, randomized into three groups of 60 patients each. Each group was assigned to be treated with one of the three treatment options namely Alcaftadine 0.25%, Olopatadine hydrochloride 0.2% and Bepotastine besilate 1.5% ophthalmic solutions. Patients were followed-up at regular intervals with relief and resolution of symptoms and signs noted using Total Ocular Scoring System (TOSS) and hyperaemia scale. Results: All three topical medications were effective in resolving symptoms of the patients with mild to moderate allergic conjunctivitis. Baseline mean TOSS scores for Alcaftadine group, Olopatadine group and Bepotastine besilate group were (7.68±2.32), (7.65±2.32) and (7.45±2.27) respectively as compared to the corresponding TOSS scores on 14th Day (4th visit) which were (0.2 ± 0.43), (0.4 ± 0.56) and (0.1 ± 0.36) respectively. The resolution of symptoms in the Bepotastine and Alcaftadine groups was significantly profound as compared to the Olopatadine group (p = 0.008). Bepotastine and Alcaftadine groups significantly reduced allergic conjunctivitis symptoms compared to Olopatadine group (p = 0.008). Conclusion: All three topical ophthalmic medications used in the study are safe and effective in the treatment of allergic conjunctivitis. However, Bepotastine and Alcaftadine appear to outweigh Olopatadine in resolving the symptoms of allergic conjunctivitis.

Background: Vernal keratoconjunctivitis (VKC) is an allergic eye disease that especially affects young boys. Both olopatadine and bepotestine are dual acting drugs that provide rapid symptomatic relief coupled with the long-term disease-modifying benefit. The present study is conducted to compare the efficacy and safety of olopatadine eye drops and bepotastine eye drops in patients of vernal keratoconjunctivitis.Methods: A prospective, randomized, parallel-group, comparative study is conducted over a period of 4 weeks on paediatric patients with VKC. 50 patients are recruited and randomized into two treatment groups. They received the assigned drugs for 4 weeks and are called for follow up at the end of 1st week, 4th week and 12th week. At each follow-up, patients are examined and the clinical parameters are graded.Results: This study shows that both olopatadine and bepotastine are equally efficacious. Bepotastine provided quicker relief to symptoms of watering, ocular discomfort and conjunctival hyperaemia. Number of responders are also more in the bepotastine group. Absolute eosinophilic count improved with both the drugs but there is no statistically significant difference between them. Both drugs showed good safety profile. However, 24% patients reported aversion to bitter taste with bepotastine. There is no treatment related severe adverse effects in both the groups.Conclusions: Both olopatadine and bepotastine are effective in treating vernal keratoconjunctivitis. However, bepotastine performed better in reducing tearing, ocular discomfort and conjunctival hyperaemia.

Objective: To determine the efficacy of the antihistamine bepotastine on treating nasal symptoms in patients with Japanese cedar and cypress pollinosis, based on two previous studies that looked at bepotastine OD’s inhibitory effect on symptom onset after exposure. Design and methods: Randomized double-blind placebo controlled, parallel study. Twenty-eight volunteers with Japanese cedar and cypress pollinosis were randomly assigned into two experimental groups: a bepotastine-treated or a placebo control group. Subjects received either 10 mg bepotastine tablets or placebo tablets 1 day before entering an artificial exposure pollen chamber (OHIO Chamber) and also for three or more consecutive days. They were exposed to Japanese cedar and cypress pollen for 3 h per day for 2 days. Nasal and ocular symptoms were self-rated by each patient at regular intervals in addition to being objectively measured. Possible cognitive impairment was assessed by using the digit cancellation test (D-CAT). Results: In Study 1, under controlled conditions, there were no significant differences (p > .05) between subjects exposed to Japanese cedar pollen and those exposed to cypress pollen in terms of total nasal symptom score (TNSS). In Study 2, in the placebo group, the amount of nasal discharge and the number of sneezes did not diminish before cypress pollen exposure on the second day (p .05). Conclusion: We conclude that bepotastine can suppress allergy-related symptoms without impairing work performance in subjects with seasonal allergic rhinitis caused by Japanese cedar pollen or cypress pollen.

INTRODUCTION To establish the efficacy of bepotastine besilate ophthalmic solution (bepotastine) 1.5%, a dual acting histamine H1 receptor antagonist approved for treatment of ocular itching associated with allergic conjunctivitis, compared to placebo in relieving ocular itching and redness for subjects with active allergic rhinoconjunctivitis. METHODS A randomized, double-masked, placebo-controlled, confirmatory natural exposure study of bepotastine 1.5% and placebo was conducted during allergy season at 12 clinical sites throughout the U.S. Following a 7-day screening period, eligible subjects ≥12 years old were assigned in a 1:1 ratio to dosing OU b.i.d. either bepotastine 1.5% (n = 123) or placebo (n = 122). Subjects recorded instantaneous grades for their ocular symptoms prior to their next dose for 14 consecutive days. Clinically significant reduction in ocular sign or symptom grades between treatment groups required p ≤ 0.05 as determined by ANCOVA analysis. RESULTS Significant clinical effectiveness with bepotastine 1.5% was demonstrated over the 2-week treatment period in comparison to placebo in the intent-to-treat population for reducing mean instantaneous grades for both ocular itching (p = 0.007) and redness (p = 0.001). Investigator rating of efficacy over the 2-week treatment period across response categories was also superior for bepotastine 1.5% compared to placebo (p = 0.024). Only one subject discontinued participation in the study due to an adverse event. CONCLUSIONS These data support bepotastine 1.5% as an effective treatment for allergen-induced signs and symptoms in a clinical study designed to closely resemble the conditions under which patients with allergic rhinoconjunctivitis would require treatment.

Background: Pharmacotherapy is the mainstay of allergic rhinitis and many caregivers use over-the-counter antihistamines. Bepotastine is a novel oral second generation non-sedative antihistamine and an effective treatment option for allergic rhinitis. The objectives of the present study were to evaluate the efficacy and safety of bepotastine versus cetirizine an over the counter drug.Methods: A prospective, randomized, open-label, parallel-group study was conducted among 60 patients fulfilling the inclusion and exclusion criteria. Group A (n=30) received tablet cetirizine 10 mg once daily and Group B (n=30) received tablet bepotastine 10 mg once daily. Efficacy was assessed by mean change in total symptom score (TSS) which is the sum of total nasal symptom score and total ocular symptom score at the end of two weeks from baseline.Results: At the end of two weeks of treatment, both groups showed statistically significant (p