Clinical safety and efficacy of bepo

tastine besilate ophthalmic solution

to treat allergic conjunctivitis

Gregg J. Nerdy
Herdy Ollifp
Allergic conjunctivitis
Bepostatine Besilate
• is a 2nd generation antihistamine.[
• It was approved in Japan for use in the treatment o
f allergic rhinitis and urticaria/pruritus
• According to a survey of the National Family Opinio
n, Inc. database of 200,000 American households, 3
1.5% of the population ([proportional to]79.5 millio
n Americans) have ocular/nasal symptoms seven or
more times a year
• . In studies of patients with pollen allergy, ocular sy
mptoms occur in approximately 75% of patients wit
h rhinitis
Objective
To evaluate the effectiveness of bepotastine besilate
ophthalmic solutions 1.0% and 1.5% compared with
placebo at reducing ocular itching and conjunctival h
yperemia in the conjunctival allergen challenge (CAC)
model of allergic conjunctivitis.

•
Research Design
• Prospective, double-masked, randomized, placebo-
controlled, phase 3 CAC clinical tria
Methodology
• 130 subjects with a clinical history of allergic conjun
ctivitis who were randomized to bepotastine besilat
e ophthalmic solution 1.0%, 1.5%, or 0.0% (placeb
o).
• One drop of test agent was instilled bilaterally befor
e a CAC
• test evaluating responses at 15 minutes, 8 hours, o
r 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.
Summary
• Reductions of 1.2 units or more in mean ocular itchi
ng scores at all time points for both bepotastine bes
ilate ophthalmic solutions 1.0% and 1.5% were obs
erved at onset of action and 8-hour duration-of-acti
on CAC tests (P < .0001).
• Statistically significant reductions in conjunctival hy
peremia (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 ocu
lar itching for at least 8 hours after dosing. Reductio
ns in conjunctival hyperemia after a CAC, although s
tatistically significant for bepotastine besilate ophth
almic solutions 1.0% and 1.5% compared with place
bo when assessed at 15 minutes after dosing, were
modest.