Page 165 - 80_01

Dry
eye
disease
compounds…

pretreatment
is
the
reduction
of
Cyclosporine
stinging
in
chronic
dry
eye
disease

(62).
Lotemax
ophthalmic
suspension,
0.5%
completed
Phase
II
studies

(ClinicalTrials.gov
Identifier:
NCT00560638)
in
July
2011.
From
the
results
it
was

confirmed
its
ability
to
reduce
the
eye
inflammation
rapidly,
causing
limited
side

effects.
Additionally
in
2012
Wan
and
colleagues
performed
a
study
on
34
patients,

confirming
the
efficacy
of
topical
0.5%
loteprednoletabonate
ophthalmic

suspension
for
the
treatment
of
moderate
dry
eye
(63).

ECABET-­-SODIUM

Bausch
&
Lomb
Inc.
is
developing
a
prescription
eye
drop
for
the
treatment

of
dry
eye
syndrome
called
Ecabet
(Accession
Number:
DB05265).

Sulfodehydroabietic
acid
monosodium
salt
pentahydrate
or
ecabet
sodium,

represents
a
new
class
of
small
diffusible
molecules
capable
of
increasing
the

quantity
and
quality
of
mucin
produced
by
conjunctival
goblet
cells
and
corneal

epithelia
(Figure
8)
(64).
This
ability
makes
the
compound
quite
interesting
as
a

treatment
for
muco-­-deficient
dry
eye.
Ecabet
possible
mechanism
of
action
is

through
the
targeting
of
the
prostaglandin
E2
pathway,
inhibiting
the
pepsin

formation,
increasing
blood
flow
and
downregulating
the
reactive
oxygen
species

on
the
ocular
surface.
(65).
It
is
marketed
in
Japan
by
Senju
Pharmaceutical
as
an

oral
agent
for
gastric
ulcers
and
gastritis
treatment
(66).
Bausch
&
Lomb
organized

from
April
2008
to
January
2013
Phase
II
efficacy
and
safety
studies
for
Ecabet

ophthalmic
solution
with
the
purpose
of
treating
the
dry
eye
syndrome

(ClinicalTrials.gov
Identifier:
NCT00667004)
in
183
patients.
Bausch
&
Lomb
Inc.

did
not
yet
distribute
results
information.

BOL-­-303242-­-X

Pharmaceutical
R&D,
Bausch
&
Lomb
Inc.,
presented
the
drug
BOL-­-303242-­-
X
(mapracorat)
(Figure
9)
a
selective
glucocorticoid
receptor
agonist,
as
a
possible

treatment
for
inflammatory
skin
and
eye
diseases.
This
agonist
is
binding
to
the

glucocorticoid
receptor
with
an
affinity
similar
to
dexamethasone.
Zhang
and

colleagues
demonstrated
during
in
vitro
and
in
vivo
studies
that
BOL-­-303242-­-X

inhibited
interleukin-­-1ß
(IL-­-1ß)
and
induced
decreases
of
inflammation
in
human

corneal
epithelial
cells.
It
is
possible
that
BOL-­-303242-­-X
is
acting
as
an
anti-­-
inflammatory
agent
in
various
primary
human
ocular
cells
with
similar
activity
to

classical
steroids.
As
mechanism
of
action
it
is
suggested
its
interference
in
human

ocular
cells
MAPK
(p38
and
JNK)
and
NF?B
signaling
pathways
(67).
Vollmer
T.R.

161