The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Jon I Williams - One of the best experts on this subject based on the ideXlab platform.
-
Bepotastine besilate ophthalmic solution 1.5% for alleviating nasal symptoms in patients with allergic conjunctivitis.
Journal of asthma and allergy, 2018Co-Authors: Megan E. Cavet, Paul J Gomes, Warner Carr, Jon I WilliamsAbstract:Background Bepotastine besilate ophthalmic solution (BBOS) 1.5% is a topical antihistamine for the treatment of ocular itching associated with allergic conjunctivitis (AC). Allergic rhinitis and AC are common comorbid conditions. We explored the efficacy of BBOS 1.5% in alleviating nasal symptoms in an integrated analysis of two Phase III conjunctival allergen challenge (CAC) studies and a Phase IV environmental allergen study. Methods In the Phase III trials, a CAC was performed 15 minutes, 8 hours, and 16 hours following ocular instillation of BBOS 1.5% (n=78) or placebo (n=79), and subjects evaluated nasal symptoms. In the environmental study, subjects instilled BBOS 1.5% (n=123) or placebo (n=122) twice daily and nasal symptoms were evaluated over 2 weeks. Results In the Phase III trials, BBOS 1.5% had reduced CAC-induced nasal congestion and pruritus at 15 minutes and 8 hours postdosing and rhinorrhea and a non-ocular composite-symptom score (sum of nasal scores plus ear or palate pruritus) at all time points postdosing (all P≤0.01 vs placebo). In the Phase IV environmental study, BBOS 1.5% reduced sneezing and nasal pruritus over 2 weeks and median number of days to improvement of nasal pruritus and total nasal symptom score (sum for rhinorrhea, sneezing, nasal pruritus, and nasal congestion; P≤0.04 vs placebo). Additionally, investigator-reported improvement in overall ocular (pruritus, hyperemia, tearing) and nasal symptoms was greater with BBOS 1.5% vs placebo (P≤0.03). Conclusion Results of these exploratory analyses indicate that topical ocular BBOS 1.5% reduced nasal symptoms, supporting its use for alleviating rhinitis symptoms associated with AC.
-
Treatment of allergic conjunctivitis with Bepotastine besilate ophthalmic solution 1.5
Clinical ophthalmology (Auckland N.Z.), 2014Co-Authors: M T Bergmann, Jon I Williams, Paul J GomesAbstract:Purpose: To examine the pooled per-protocol ocular end points from two conjunctival allergen challenge (CAC) clinical trials of the dual-action antihistamine Bepotastine besilate ophthalmic solution (BBOS) 1.5%. Methods: Two Phase III, placebo-controlled, double-masked, randomized clinical trials were conducted at a total of six separate centers using the CAC model of allergic conjunctivitis. The same study design was employed for both clinical trials, with subjects randomly assigned to either BBOS 1.5% (n=78) or placebo (n=79) treatment. Each subject received one eye drop of the test agent bilaterally at different study visits 15 minutes, 8 hours, or 16 hours prior to a CAC. Primary ocular end points included changes in ocular itching reported at 3, 5, and 7 minutes and conjunctival hyperemia assessed at 7, 15, and 20 minutes following each CAC. Secondary ocular end points included chemosis as well as episcleral and ciliary hyperemia judged by investigators, and tearing (scored as either absent or present) and eyelid swelling judged by subjects. Results: A statistically significant reduction in ocular itching was observed for BBOS 1.5% treatment compared to placebo at all time points (P0.0001), while measures for onset and 8-hour persistence of action also reached clinical significance (ie, 1.0 unit difference) at a majority of time points. In addition, a significant reduction in conjunctival hyperemia was achieved at a majority of time points during the onset of action CAC test. Secondary end points were also significantly improved compared to placebo, most prominently for reduced tearing at all study visits and reduced eyelid swelling at the onset of action and 8-hour study visits. Adverse events were generally mild and transient. Conclusion: BBOS 1.5% rapidly reduced CAC-induced ocular itching with duration of effectiveness of at least 8 hours after dosing. Certain secondary signs of inflammation were also significantly reduced.
-
efficacy of Bepotastine besilate ophthalmic solution 1 5 for seasonal allergic conjunctivitis a randomized placebo controlled natural exposure clinical trial
Allergy and Asthma Proceedings, 2013Co-Authors: W Carr, Timothy R. Mcnamara, Anjuli Nayak, Paul H Ratner, Jon I WilliamsAbstract:: Allergic conjunctivitis (AC) affects an estimated 20% of the population in the Western world, with a large fraction suffering due to seasonal or perennial allergen exposures. Bepotastine besilate ophthalmic solution (BBOS) 1.5%, a dual-acting histamine (H(1)) receptor antagonist and mast cell stabilizer, is indicated for itching associated with AC. This study was designed to evaluate the efficacy and safety of BBOS 1.5% for reducing ocular itching associated with AC in subjects enrolled in a natural exposure trial. Eligible subjects in a multicenter, double-masked, randomized, parallel-group, placebo-controlled, natural exposure clinical trial were randomly assigned to either BBOS 1.5% or placebo eyedrops on a 1:1 basis and instilled 1 drop of the test agent into both eyes twice daily for 2 weeks. The mean change from baseline in instantaneous and reflective ocular itching scores at the end of 2 weeks of treatment were evaluated based on subject-assessed severity of instantaneous and reflective itching. Subject-reported adverse events (AEs) were also recorded for safety. Treatment with BBOS 1.5% significantly reduced instantaneous and reflective ocular itching scores from baseline compared with placebo over the 2-week study period(p = 0.007 and p = 0.005, respectively). BBOS 1.5% was well tolerated, and AEs were generally transient and mild. This clinical study indicates BBOS 1.5% effectively and safely treated ocular itching in a natural exposure allergy study and is a useful treatment option for the management of ocular itching associated with AC. (ClinicalTrials.gov identifier number: NCT01174823.)
-
Integrated phase III trials of Bepotastine besilate ophthalmic solution 1.5% for ocular itching associated with allergic conjunctivitis.
Allergy and asthma proceedings, 2012Co-Authors: Edward J Meier, James A. Gow, Timothy R. Mcnamara, Paul J Gomes, Gail Torkildsen, Jon I WilliamsAbstract:Allergic conjunctivitis is a clinical reaction to environmental allergens and is manifested by ocular itching caused by IgE-induced mast cell degranulation. Bepotastine besilate is a selective H(1)-antagonist with mast cell stabilizing properties. This report examines the reduction of ocular itching integrated from two conjunctival allergen challenge (CAC) clinical trials comparing Bepotastine besilate ophthalmic solution (BBOS) 1.5% to placebo in subjects with a history of allergic conjunctivitis. Two phase III, double-masked, placebo-controlled, parallel-group, CAC clinical trials evaluated BBOS 1.5% versus placebo to reduce ocular itching. Eligible subjects were randomly assigned 1:1 to either BBOS 1.5% (n = 78) or placebo (n = 79). Ocular itching was graded by subjects using a standardized scale (0–4 U). Adverse events and ophthalmic clinical findings were recorded for safety. BBOS 1.5% was superior to placebo for reducing CAC-induced ocular itching (p < 0.0001) as early as 3 minutes post-CAC and for at least 8 hours after dosing. Post hoc analyses examining several populations also showed a significant improvement (p < 0.0001) for subjects with more severe itching response at screening and for the proportion of subjects with complete or nearly complete resolution of CAC-induced itching, both outcomes supporting the clinical benefit of BBOS 1.5%. Adverse events were generally transient and mild. BBOS 1.5% is safe and effective in the treatment of ocular itching associated with allergic conjunctivitis within 3 minutes of a CAC and with a sustained duration of action of at least 8 hours. (ClinicalTrials.gov numbers: NCT00424398 and NCT00586664).
-
multicenter clinical evaluation of Bepotastine besilate ophthalmic solutions 1 0 and 1 5 to treat allergic conjunctivitis
American Journal of Ophthalmology, 2010Co-Authors: T T Macejko, M T Bergmann, Jon I Williams, Paul J Gomes, T R Mcnamara, Mark B AbelsonAbstract:Purpose To evaluate the effectiveness of Bepotastine besilate ophthalmic solutions 1.0% and 1.5% compared with placebo at reducing ocular itching and conjunctival hyperemia in the conjunctival allergen challenge (CAC) model of allergic conjunctivitis. Design Prospective, double-masked, randomized, placebo-controlled, phase 3 CAC clinical trial. Methods This multicenter trial enrolled 130 subjects with a clinical history of allergic conjunctivitis who were randomized to Bepotastine besilate ophthalmic solution 1.0%, 1.5%, or 0.0% (placebo). One drop of test agent was instilled bilaterally before a CAC test evaluating responses at 15 minutes, 8 hours, or 16 hours after test agent instillation. Primary efficacy outcomes were unit improvements relative to placebo in mean scores for ocular itching and conjunctival hyperemia, each graded on 0- to 4-unit scales. Results Reductions of 1.2 units or more in mean ocular itching scores at all time points for both Bepotastine besilate ophthalmic solutions 1.0% and 1.5% were observed at onset of action and 8-hour duration-of-action CAC tests ( P P ≤ .0125) were observed for Bepotastine besilate ophthalmic formulations only at the onset of action CAC test. Conclusions Bepotastine besilate ophthalmic solutions 1.0% and 1.5% both substantially decreased CAC-induced ocular itching for at least 8 hours after dosing. Reductions in conjunctival hyperemia after a CAC, although statistically significant for Bepotastine besilate ophthalmic solutions 1.0% and 1.5% compared with placebo when assessed at 15 minutes after dosing, were modest.
Kimihiro Okubo - One of the best experts on this subject based on the ideXlab platform.
-
Histamine antagonist Bepotastine suppresses nasal symptoms caused by Japanese cedar and cypress pollen exposure
Journal of drug assessment, 2016Co-Authors: Sho Kanzaki, Kazuhiro Hashiguchi, Kiyochika Suematsu, Kenichiro Wakabayashi, Kimihiro OkuboAbstract: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.
-
Double-blind placebo-controlled study of Bepotastine besilate in pediatric patients with perennial allergic rhinitis
Expert opinion on pharmacotherapy, 2015Co-Authors: Kimihiro Okubo, Masahiko Ichimura, Tomoya Koyama, Yutaka Susuta, Hitoshi IzakiAbstract:Background: Although second-generation antihistamines, such as Bepotastine besilate, are recommended as a first-line treatment option for adult perennial allergic rhinitis (PAR), few non-sedating second-generation antihistamines are safe for children.Objective: A double-blind, placebo-controlled, comparative study of 473 pediatric PAR patients (7 – 15 years old) to determine the superiority and safety of Bepotastine besilate (10 mg twice daily) relative to placebo for improved total and individual nasal symptom scores compared with baseline.Research design and methods: Subjects were randomized to placebo (n = 233) or Bepotastine besilate (n = 240, 10 mg orally twice daily for 2 weeks). Interference of daily life by PAR was assessed by measuring change in individual nasal symptom scores from baseline.Results: Bepotastine besilate was superior to placebo in terms of total nasal symptom scores, with improved overall nasal symptoms of PAR compared with baseline values. Subgroup analyses demonstrated bepotasti...
-
Effectiveness of Second-Generation Antihistamine for the Treatment of MorningSymptoms Observed in Patients with Perennial Allergic Rhinitis: ComparisonStudy of Bepotastine Besilate versus Olopatadine Hydrochloride
otolaryngology, 2015Co-Authors: Terumichi Fujikura, Kimihiro OkuboAbstract:Objective: The aim of the present study was to examine circadian rhythm-based treatment strategies with the intension of improving the pharmacotherapy for morning symptoms with perennial allergic rhinitis. We investigated the effects of two second generation antihistamines, with different pharmacokinetic parameters, Bepotastine besilate and olopatadine hydrochloride, for the treatment of morning symptoms. Methods: Twenty-four subjects with perennial allergic rhinitis were recruited for this study. They were randomly allocated to either a Bepotastine group (n=10) or an olopatadine group (n=14). During the 1-hour period after waking up in the morning, the patients counted and recorded the number of sneezes and nose blowing. PNIF was also measured. The study participants took the allocated medicine twice a day. They continued recording their nasal symptoms and PNIF after awakening for 10 to 14 days. Results: In both group, taking Bepotastine and olopatadine, the mean sneezing count and the mean nose blowing count were well suppressed. However, a significant change in the nasal congestion score was not observed throughout the study. Especially in olopatadine group, PNIF increased from day 2 onward and a significant increase was observed for the following 10 days. Conclusion: The worsening of nasal symptoms after awakening that is associated with perennial allergic rhinitis has a significant impact on the quality of life of patients. Two second-generation antihistamines, Bepotastine besilate and olopatadine hydrochloride, were effective for the treatment of these morning symptoms. The measurement of Peak Nasal Inspiratory Flow (PNIF) value might lead to a favorable self-evaluation of nasal symptom and treatment effects. Some guidance regarding the taking of medicine from Powered by Editorial Manager® and ProduXion Manager® from Aries Systems Corporation the viewpoint of chronotherapy might improve the satisfaction of patients with the results of pharmacotherapy.
-
Bepotastine besilate OD tablets suppress nasal symptoms caused by Japanese cedar pollen exposure in an artificial exposure chamber (OHIO Chamber).
Expert opinion on pharmacotherapy, 2009Co-Authors: Kazuhiro Hashiguchi, Huaipeng Tang, Toshio Fujita, Kiyochika Suematsu, Minoru Gotoh, Kimihiro OkuboAbstract:Objective: To investigate the efficacy and safety of Bepotastine, we conducted a randomized, investigator-blind, placebo-controlled and parallel study to evaluate the allergic symptoms and the cognitive function of the subjects with Japanese cedar (JC) pollinosis in response to JC pollen exposure in an artificial exposure chamber. Methods: Twenty-four volunteers with JC pollinosis were enrolled in this study. The subjects were randomly divided into two groups: a Bepotastine group and a placebo group (12 subjects each). Subjects received either a 10-mg Bepotastine OD (orally disintegrating) tablet or a placebo 10 min before entering the chamber for a 3-h exposure. The nasal and ocular symptoms were evaluated by each patient at regular intervals. The amount of nasal discharge was measured and the number of sneezes recorded. To evaluate the cognitive function, a digit cancellation test (D-CAT), in which the subjects have to eliminate certain numbers within a fixed time, was conducted. Results: Twelve subject...
-
BepotastinebesilateODtablets suppressnasalsymptoms causedbyJapanesecedarpollen exposureinanartificialexposure chamber(OHIOChamber)
2009Co-Authors: Kazuhiro Hashiguchi, Huaipeng Tang, Toshio Fujita, Kiyochika Suematsu, Minoru Gotoh, Kimihiro OkuboAbstract:Objective: To investigate the efficacy and safety of Bepotastine, we conducted a randomized, investigator-blind, placebo-controlled and parallel study to evaluate the allergic symptoms and the cognitive function of the subjects with Japanese cedar (JC) pollinosis in response to JC pollen exposure in an artificial exposure chamber. Methods: Twenty-four volunteers with JC pollinosis were enrolled in this study. The subjects were randomly divided into two groups: a Bepotastine group and a placebo group (12 subjects each). Subjects received either a 10-mg Bepotastine OD (orally disintegrating) tablet or a placebo 10 min before entering the chamber for a 3-h exposure. The nasal and ocular symptoms were evaluated by each patient at regular intervals. The amount of nasal discharge was measured and the number of sneezes recorded. To evaluate the cognitive function, a digit cancellation test (D-CAT), in which the subjects have to eliminate certain numbers within a fixed time, was conducted. Results: Twelve subjects in the placebo group developed nasal and/or ocular symptoms, whereas six subjects in the Bepotastine group showed none of the symptoms during exposure. Mean secretion weights and number of sneezes were significantly lower in the Bepotastine group than in the placebo group. In D-CAT, no deterioration of work performance was observed in the Bepotastine group. No adverse effects were observed in either group. Conclusion: Bepotastine treatment is effective and well tolerated in patients with allergen-induced symptoms exposed to JC pollen in an exposure chamber.
Paul J Gomes - One of the best experts on this subject based on the ideXlab platform.
-
Bepotastine besilate ophthalmic solution 1.5% for alleviating nasal symptoms in patients with allergic conjunctivitis.
Journal of asthma and allergy, 2018Co-Authors: Megan E. Cavet, Paul J Gomes, Warner Carr, Jon I WilliamsAbstract:Background Bepotastine besilate ophthalmic solution (BBOS) 1.5% is a topical antihistamine for the treatment of ocular itching associated with allergic conjunctivitis (AC). Allergic rhinitis and AC are common comorbid conditions. We explored the efficacy of BBOS 1.5% in alleviating nasal symptoms in an integrated analysis of two Phase III conjunctival allergen challenge (CAC) studies and a Phase IV environmental allergen study. Methods In the Phase III trials, a CAC was performed 15 minutes, 8 hours, and 16 hours following ocular instillation of BBOS 1.5% (n=78) or placebo (n=79), and subjects evaluated nasal symptoms. In the environmental study, subjects instilled BBOS 1.5% (n=123) or placebo (n=122) twice daily and nasal symptoms were evaluated over 2 weeks. Results In the Phase III trials, BBOS 1.5% had reduced CAC-induced nasal congestion and pruritus at 15 minutes and 8 hours postdosing and rhinorrhea and a non-ocular composite-symptom score (sum of nasal scores plus ear or palate pruritus) at all time points postdosing (all P≤0.01 vs placebo). In the Phase IV environmental study, BBOS 1.5% reduced sneezing and nasal pruritus over 2 weeks and median number of days to improvement of nasal pruritus and total nasal symptom score (sum for rhinorrhea, sneezing, nasal pruritus, and nasal congestion; P≤0.04 vs placebo). Additionally, investigator-reported improvement in overall ocular (pruritus, hyperemia, tearing) and nasal symptoms was greater with BBOS 1.5% vs placebo (P≤0.03). Conclusion Results of these exploratory analyses indicate that topical ocular BBOS 1.5% reduced nasal symptoms, supporting its use for alleviating rhinitis symptoms associated with AC.
-
Treatment of allergic conjunctivitis with Bepotastine besilate ophthalmic solution 1.5
Clinical ophthalmology (Auckland N.Z.), 2014Co-Authors: M T Bergmann, Jon I Williams, Paul J GomesAbstract:Purpose: To examine the pooled per-protocol ocular end points from two conjunctival allergen challenge (CAC) clinical trials of the dual-action antihistamine Bepotastine besilate ophthalmic solution (BBOS) 1.5%. Methods: Two Phase III, placebo-controlled, double-masked, randomized clinical trials were conducted at a total of six separate centers using the CAC model of allergic conjunctivitis. The same study design was employed for both clinical trials, with subjects randomly assigned to either BBOS 1.5% (n=78) or placebo (n=79) treatment. Each subject received one eye drop of the test agent bilaterally at different study visits 15 minutes, 8 hours, or 16 hours prior to a CAC. Primary ocular end points included changes in ocular itching reported at 3, 5, and 7 minutes and conjunctival hyperemia assessed at 7, 15, and 20 minutes following each CAC. Secondary ocular end points included chemosis as well as episcleral and ciliary hyperemia judged by investigators, and tearing (scored as either absent or present) and eyelid swelling judged by subjects. Results: A statistically significant reduction in ocular itching was observed for BBOS 1.5% treatment compared to placebo at all time points (P0.0001), while measures for onset and 8-hour persistence of action also reached clinical significance (ie, 1.0 unit difference) at a majority of time points. In addition, a significant reduction in conjunctival hyperemia was achieved at a majority of time points during the onset of action CAC test. Secondary end points were also significantly improved compared to placebo, most prominently for reduced tearing at all study visits and reduced eyelid swelling at the onset of action and 8-hour study visits. Adverse events were generally mild and transient. Conclusion: BBOS 1.5% rapidly reduced CAC-induced ocular itching with duration of effectiveness of at least 8 hours after dosing. Certain secondary signs of inflammation were also significantly reduced.
-
Integrated phase III trials of Bepotastine besilate ophthalmic solution 1.5% for ocular itching associated with allergic conjunctivitis.
Allergy and asthma proceedings, 2012Co-Authors: Edward J Meier, James A. Gow, Timothy R. Mcnamara, Paul J Gomes, Gail Torkildsen, Jon I WilliamsAbstract:Allergic conjunctivitis is a clinical reaction to environmental allergens and is manifested by ocular itching caused by IgE-induced mast cell degranulation. Bepotastine besilate is a selective H(1)-antagonist with mast cell stabilizing properties. This report examines the reduction of ocular itching integrated from two conjunctival allergen challenge (CAC) clinical trials comparing Bepotastine besilate ophthalmic solution (BBOS) 1.5% to placebo in subjects with a history of allergic conjunctivitis. Two phase III, double-masked, placebo-controlled, parallel-group, CAC clinical trials evaluated BBOS 1.5% versus placebo to reduce ocular itching. Eligible subjects were randomly assigned 1:1 to either BBOS 1.5% (n = 78) or placebo (n = 79). Ocular itching was graded by subjects using a standardized scale (0–4 U). Adverse events and ophthalmic clinical findings were recorded for safety. BBOS 1.5% was superior to placebo for reducing CAC-induced ocular itching (p < 0.0001) as early as 3 minutes post-CAC and for at least 8 hours after dosing. Post hoc analyses examining several populations also showed a significant improvement (p < 0.0001) for subjects with more severe itching response at screening and for the proportion of subjects with complete or nearly complete resolution of CAC-induced itching, both outcomes supporting the clinical benefit of BBOS 1.5%. Adverse events were generally transient and mild. BBOS 1.5% is safe and effective in the treatment of ocular itching associated with allergic conjunctivitis within 3 minutes of a CAC and with a sustained duration of action of at least 8 hours. (ClinicalTrials.gov numbers: NCT00424398 and NCT00586664).
-
Prolonged Effectiveness of Bepotastine Besilate Ophthalmic Solution for the Treatment of Ocular Symptoms of Allergic Conjunctivitis
Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics, 2011Co-Authors: J.i. Williams, James A. Gow, Mark B Abelson, Gail Torkildsen, Kathryn S. Kennedy, Paul J GomesAbstract:Abstract Purpose: This clinical trial evaluated the safety and effectiveness of Bepotastine besilate ophthalmic solutions 1.0% and 1.5% compared with placebo for the treatment of ocular itching and conjunctival hyperemia (redness) using the conjunctival allergen challenge (CAC) model of allergic conjunctivitis when dosed 16 h before a CAC test. Methods: Subjects with a history of allergic conjunctivitis were assigned to receive placebo or Bepotastine besilate ophthalmic solution 1.0% or 1.5% in a single-center, randomized, placebo-controlled clinical trial. Eligible subjects (n=107) aged 10 years and older with a history of allergic conjunctivitis who had a reproducible positive reaction to a CAC were enrolled and dosed with test agent. The primary trial objectives included assessment of ocular itching and conjunctival redness at 16 h after instillation of test agent. Reductions in several CAC-induced secondary symptoms and signs of allergic conjunctivitis were also evaluated for tearing, ciliary and epis...
-
multicenter clinical evaluation of Bepotastine besilate ophthalmic solutions 1 0 and 1 5 to treat allergic conjunctivitis
American Journal of Ophthalmology, 2010Co-Authors: T T Macejko, M T Bergmann, Jon I Williams, Paul J Gomes, T R Mcnamara, Mark B AbelsonAbstract:Purpose To evaluate the effectiveness of Bepotastine besilate ophthalmic solutions 1.0% and 1.5% compared with placebo at reducing ocular itching and conjunctival hyperemia in the conjunctival allergen challenge (CAC) model of allergic conjunctivitis. Design Prospective, double-masked, randomized, placebo-controlled, phase 3 CAC clinical trial. Methods This multicenter trial enrolled 130 subjects with a clinical history of allergic conjunctivitis who were randomized to Bepotastine besilate ophthalmic solution 1.0%, 1.5%, or 0.0% (placebo). One drop of test agent was instilled bilaterally before a CAC test evaluating responses at 15 minutes, 8 hours, or 16 hours after test agent instillation. Primary efficacy outcomes were unit improvements relative to placebo in mean scores for ocular itching and conjunctival hyperemia, each graded on 0- to 4-unit scales. Results Reductions of 1.2 units or more in mean ocular itching scores at all time points for both Bepotastine besilate ophthalmic solutions 1.0% and 1.5% were observed at onset of action and 8-hour duration-of-action CAC tests ( P P ≤ .0125) were observed for Bepotastine besilate ophthalmic formulations only at the onset of action CAC test. Conclusions Bepotastine besilate ophthalmic solutions 1.0% and 1.5% both substantially decreased CAC-induced ocular itching for at least 8 hours after dosing. Reductions in conjunctival hyperemia after a CAC, although statistically significant for Bepotastine besilate ophthalmic solutions 1.0% and 1.5% compared with placebo when assessed at 15 minutes after dosing, were modest.
Haruhiko Manabe - One of the best experts on this subject based on the ideXlab platform.
-
the effects of olopatadine hydrochloride on the number of scratching induced by repeated application of oxazolone in mice
European Journal of Pharmacology, 2005Co-Authors: Tadafumi Tamura, Toru Amano, Kenji Ohmori, Haruhiko ManabeAbstract:Abstract It is suggested that atopic dermatitis is a skin disease associated with itching as subjective symptoms, and histamine H1 receptor antagonists are used in order to prevent the itching, and the deterioration for scratch by itching. Histamine H1 receptor selective anti-histamine olopatadine hydrochloride (olopatadine; Allelock®) shows consistent efficacy and safety in the treatment of allergic disorders. We investigated the possible efficacy of olopatadine on the number of scratching induced by repeated application of oxazolone in BALB/c mice. The repeated treatment of olopatadine significantly inhibited the ear swelling and the increased number of scratching. It significantly inhibited the increased production of interleukin (IL)-4, IL-1β and granulocyte–macrophage colony-stimulating factor (GM-CSF) in the lesioned ear. Moreover, it significantly inhibited the increased production of nerve growth factor (NGF) and substance P. On the other hand, loratadine, Bepotastine and chlorpheniramine did not inhibit the ear swelling and the increased number of scratching. These results indicate that olopatadine inhibited not only the increased production of cytokines but also NGF and substance P unlike other histamine H1 receptor antagonists. It was suggested that olopatadine suppressed the increased number of scratching by the anti-inflammatory effects. Therefore, olopatadine appears to exert additional biological effects besides its blockade of a histamine H1 receptor.
-
The effects of olopatadine hydrochloride on the number of scratching induced by repeated application of oxazolone in mice.
European journal of pharmacology, 2005Co-Authors: Tadafumi Tamura, Toru Amano, Kenji Ohmori, Haruhiko ManabeAbstract:It is suggested that atopic dermatitis is a skin disease associated with itching as subjective symptoms, and histamine H(1) receptor antagonists are used in order to prevent the itching, and the deterioration for scratch by itching. Histamine H(1) receptor selective anti-histamine olopatadine hydrochloride (olopatadine; Allelock shows consistent efficacy and safety in the treatment of allergic disorders. We investigated the possible efficacy of olopatadine on the number of scratching induced by repeated application of oxazolone in BALB/c mice. The repeated treatment of olopatadine significantly inhibited the ear swelling and the increased number of scratching. It significantly inhibited the increased production of interleukin (IL)-4, IL-1beta and granulocyte-macrophage colony-stimulating factor (GM-CSF) in the lesioned ear. Moreover, it significantly inhibited the increased production of nerve growth factor (NGF) and substance P. On the other hand, loratadine, Bepotastine and chlorpheniramine did not inhibit the ear swelling and the increased number of scratching. These results indicate that olopatadine inhibited not only the increased production of cytokines but also NGF and substance P unlike other histamine H(1) receptor antagonists. It was suggested that olopatadine suppressed the increased number of scratching by the anti-inflammatory effects. Therefore, olopatadine appears to exert additional biological effects besides its blockade of a histamine H(1) receptor.
Mark B Abelson - One of the best experts on this subject based on the ideXlab platform.
-
Prolonged Effectiveness of Bepotastine Besilate Ophthalmic Solution for the Treatment of Ocular Symptoms of Allergic Conjunctivitis
Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics, 2011Co-Authors: J.i. Williams, James A. Gow, Mark B Abelson, Gail Torkildsen, Kathryn S. Kennedy, Paul J GomesAbstract:Abstract Purpose: This clinical trial evaluated the safety and effectiveness of Bepotastine besilate ophthalmic solutions 1.0% and 1.5% compared with placebo for the treatment of ocular itching and conjunctival hyperemia (redness) using the conjunctival allergen challenge (CAC) model of allergic conjunctivitis when dosed 16 h before a CAC test. Methods: Subjects with a history of allergic conjunctivitis were assigned to receive placebo or Bepotastine besilate ophthalmic solution 1.0% or 1.5% in a single-center, randomized, placebo-controlled clinical trial. Eligible subjects (n=107) aged 10 years and older with a history of allergic conjunctivitis who had a reproducible positive reaction to a CAC were enrolled and dosed with test agent. The primary trial objectives included assessment of ocular itching and conjunctival redness at 16 h after instillation of test agent. Reductions in several CAC-induced secondary symptoms and signs of allergic conjunctivitis were also evaluated for tearing, ciliary and epis...
-
multicenter clinical evaluation of Bepotastine besilate ophthalmic solutions 1 0 and 1 5 to treat allergic conjunctivitis
American Journal of Ophthalmology, 2010Co-Authors: T T Macejko, M T Bergmann, Jon I Williams, Paul J Gomes, T R Mcnamara, Mark B AbelsonAbstract:Purpose To evaluate the effectiveness of Bepotastine besilate ophthalmic solutions 1.0% and 1.5% compared with placebo at reducing ocular itching and conjunctival hyperemia in the conjunctival allergen challenge (CAC) model of allergic conjunctivitis. Design Prospective, double-masked, randomized, placebo-controlled, phase 3 CAC clinical trial. Methods This multicenter trial enrolled 130 subjects with a clinical history of allergic conjunctivitis who were randomized to Bepotastine besilate ophthalmic solution 1.0%, 1.5%, or 0.0% (placebo). One drop of test agent was instilled bilaterally before a CAC test evaluating responses at 15 minutes, 8 hours, or 16 hours after test agent instillation. Primary efficacy outcomes were unit improvements relative to placebo in mean scores for ocular itching and conjunctival hyperemia, each graded on 0- to 4-unit scales. Results Reductions of 1.2 units or more in mean ocular itching scores at all time points for both Bepotastine besilate ophthalmic solutions 1.0% and 1.5% were observed at onset of action and 8-hour duration-of-action CAC tests ( P P ≤ .0125) were observed for Bepotastine besilate ophthalmic formulations only at the onset of action CAC test. Conclusions Bepotastine besilate ophthalmic solutions 1.0% and 1.5% both substantially decreased CAC-induced ocular itching for at least 8 hours after dosing. Reductions in conjunctival hyperemia after a CAC, although statistically significant for Bepotastine besilate ophthalmic solutions 1.0% and 1.5% compared with placebo when assessed at 15 minutes after dosing, were modest.
-
Bepotastine besilate ophthalmic solution for the relief of nonocular symptoms provoked by conjunctival allergen challenge
Annals of allergy asthma & immunology : official publication of the American College of Allergy Asthma & Immunology, 2010Co-Authors: Gail Torkildsen, J.i. Williams, James A. Gow, Paul J Gomes, Mark B Abelson, Timothy R. McnamaraAbstract:Background Bepotastine besilate is a selective histamine 1 -receptor antagonist and mast cell stabilizer with inhibitory effects on eosinophilic activity. Objective To evaluate the safety and efficacy of 1.5% Bepotastine besilate ophthalmic solution in alleviating nonocular symptoms induced by a conjunctival allergen challenge (CAC), a clinical model of allergic conjunctivitis. Methods This was a single-center, double-masked, randomized, placebo-controlled clinical trial performed from March 1 to April 4, 2007. Patients 10 years or older with a history of allergic conjunctivitis and a reproducible, positive, clinical response to a CAC were eligible. Patients received either placebo or 1.5% Bepotastine besilate, 1 drop in each eye. After 15 minutes, 8 hours, or 16 hours after dosing, a CAC was performed and patients evaluated nonocular symptoms using standardized grading scales. Results Seventy-one patients were enrolled in the study, and 66 comprised the per protocol population. A clinically meaningful reduction (≥1.0 unit) compared to placebo was achieved for rhinorrhea and nasal congestion at most time points after 1.5% Bepotastine besilate instillation at 8 hours before a CAC test. Significant reductions ( P ≤ .05) in mean values were seen with 1.5% Bepotastine besilate at 15 minutes and 8 hours after dosing for CAC-induced nasal congestion, rhinorrhea, ear or palate pruritus, nasal pruritus, and summed nonocular composite symptom (NOCS) scores and also at 16 hours after dosing for nasal congestion and rhinorrhea. Conclusions The 1.5% Bepotastine besilate formulation produced statistically significant reductions after a CAC in individual nonocular symptoms and NOCS scores at onset of allergic response and for at least 8 hours after instillation, with the greatest reduction seen for nasal congestion and rhinorrhea.
-
time to onset and duration of action of the antihistamine Bepotastine besilate ophthalmic solutions 1 0 and 1 5 in allergic conjunctivitis a phase iii single center prospective randomized double masked placebo controlled conjunctival allergen challen
Clinical Therapeutics, 2009Co-Authors: Mark B Abelson, James A. Gow, Jon I Williams, Paul J Gomes, Gail Torkildsen, T R McnamaraAbstract:Abstract Background: Bepotastine besilate is a highly selective histamine H 1 -receptor antagonist with antihistaminic, mast cell stabilizing, and anti-inflammatory activity. Based on a history of clinical effectiveness and tolerability of oral Bepotastine besilate in the treatment of allergic symptoms, Bepotastine besilate is being tested as a potential ophthalmic medication for allergic conjunctivitis. Objective: The aim of this study was to assess the effects of Bepotastine besilate ophthalmic solution 1.0% and 1.5% for the treatment of ocular itching and conjunctival hyperemia in a conjunctival allergen challenge (CAC) model in adults and children. Methods: This Phase III, single-center, prospective, randomized, double-masked, placebo-controlled, CAC clinical trial enrolled patients ≥10 years of age with a history of allergic conjunctivitis, skin-test reaction, and CAC response. Patients received Bepotastine besilate ophthalmic solution 1.0%, Bepotastine besilate ophthalmic solution 1.5%, or placebo, 1 drop on each eye on days 14 ± 3 and 28 ± 3. The primary efficacy end points, patient-assessed ocular itching (at 3, 5, and 7 minutes) and investigator-assessed conjunctival hyperemia (at 7, 15, and 20 minutes), were determined after CAC according to standardized 5-point scales (0 = none to 4=severe). Clinical significance was defined in the protocol as ≥1.0-U between-group difference in mean ocular itching scores at the majority of time points at a study visit and also a ≥0.5-U difference at all time points. Tolerability of the test agent was assessed by visual acuity, slit-lamp biomicroscopy, intraocular pressure, dilated funduscopy, and adverse events. Results: A total of 107 patients (male, 54%; age range, 11–73 years; white race/ethnicity, 93%) received investigational product and comprised the intent-to-treat (ITT) population (Bepotastine besilate ophthalmic solution 1.0%, 36 patients; Bepotastine besilate ophthalmic solution 1.5%, 35; and placebo, 36). All 107 patients received investigational product at visit 3A (day 0) and were included in the ITT population. Of the 107 patients who were enrolled, 103 completed the study without a protocol deviation or violation. The 1.0% and 1.5% solutions were associated with clinically and statistically significant reductions in mean ocular itching scores compared with placebo on the 15-minute onset-of-action and 8-hour duration-of-action CAC tests (reductions, 1.3–1.5 U and 1.0–1.7 U respectively; all, P Conclusions: In this CAC model of allergic conjunctivitis in adults and children, Bepotastine besilate ophthalmic solutions 1.0% and 1.5% were associated with clinically and statistically significant reductions in ocular itching, but not conjunctival hyperemia, within 15 minutes that were maintained for at least 8 hours after administration. Both solutions were well tolerated. ClinicalTrials.gov identifier: NCT00424398.