Pharmacokinetics and Tissue Distribution of Enavogliflozin in Mice Using a Validated Liquid Chromatography–Tandem Mass Spectrometry Method
Applied Sciences,
Год журнала:
2025,
Номер
15(3), С. 1445 - 1445
Опубликована: Янв. 31, 2025
Enavogliflozin,
a
sodium–glucose
cotransporter
2
inhibitor,
was
approved
in
2022
by
the
Korean
Ministry
of
Food
and
Drug
Safety
as
therapeutic
agent
for
type
diabetes
mellitus
has
been
investigated
expanded
efficacy
diabetic
retinopathy
cardioprotection.
In
this
study,
we
developed
validated
an
analytical
method
to
precisely
detect
enavogliflozin
mouse
plasma,
employing
liquid–liquid
extraction
combined
with
liquid
chromatography–tandem
mass
spectrometry.
Overall,
method,
covering
range
5–3000
ng/mL,
is
reliable
investigating
time-concentration
profiles
enavogliflozin,
demonstrating
acceptable
accuracy,
precision,
recovery,
minimal
matrix
effects
without
stability
concerns
evidenced
assessments
post-treatment
stability,
freeze–thaw
short-term
enavogliflozin.
Pharmacokinetic
all
pharmacokinetic
parameters
mice
did
not
differ
between
fed
fasted
states
after
oral
administration
(1
mg/kg).
Additionally,
no
differences
were
observed
among
single,
7-day
repeated,
14-day
repeated
administrations
at
1
mg/kg.
tissue
distribution
showed
highest
kidneys,
followed
large
intestine,
stomach,
small
liver,
heart,
lungs,
spleen,
testes
both
3
mg/kg
doses.
Dose
proportionality
except
kidneys.
conclusion,
can
be
administered
concern
changes,
regardless
single
or
multiple
dosing
whether
states.
Furthermore,
profile
may
offer
valuable
insights
into
potential
drug.
Язык: Английский
The effect of empagliflozin and sitagliptin as an add-on therapy to metformin in blood pressure reduction in diabetic patients in primary health care settings in Riyadh, Saudi Arabia
Mayada Ahmed,
Mohammed Altoyan,
Raghad Hijazi
и другие.
Journal of Family Medicine and Primary Care,
Год журнала:
2025,
Номер
14(3), С. 1116 - 1121
Опубликована: Март 1, 2025
A
BSTRACT
Background/Aim:
Type
2
diabetes
mellitus
(T2DM)
is
a
chronic
condition.
Metformin
the
first-line
treatment,
but
if
inadequate,
sodium-glucose
cotransporter-2
inhibitors
(SGLT2i)
or
dipeptidyl
peptidase-4
(DPP4i)
are
recommended
as
add-on
therapies.
This
study
aimed
to
directly
compare
effects
of
empagliflozin
and
sitagliptin
therapies
metformin
in
reducing
blood
pressure
(BP)
cohort
type
patients
routine
care.
Additionally,
assessed
impact
on
HbA1c
levels
optimize
antidiabetic
medication
selection
for
better
BP
control.
Methods:
retrospective
was
conducted
at
tertiary
center
Riyadh,
Saudi
Arabia,
including
diabetic
aged
18–75.
readings
were
compared
12-
24-week
intervals.
Patients
had
confirmed
diagnosis
T2DM,
prescribed
either
Janumet
Synjardy,
least
one
reading
within
3
months
before
2–24
weeks
after
starting
treatment.
Exclusion
criteria
included
antihypertensive
use,
changes,
taking
drugs
other
than
metformin.
Data
demographics,
vital
signs,
lab
results.
Results:
The
44
participants,
with
mean
age
55.73
years
baseline
9.17%.
Participants
Synjardy
(43.2%)
(56.8%).
No
significant
reduction
systolic
diastolic
found.
However,
decreased
from
9.17%
7.52%
6
months,
greatest
noted
between
months.
Conclusion:
Although
neither
drug
significantly
impacted
BP,
both
combinations
reduced
HbA1c.
Further
research
larger
sample
needed
clarify
their
BP.
Язык: Английский
Sodium-glucose cotransporter 2 inhibitors: mechanisms of cardiorenal protection: A review
Consilium Medicum,
Год журнала:
2024,
Номер
26(4), С. 225 - 231
Опубликована: Май 20, 2024
Sodium-glucose
cotransporter
2
inhibitors
(SGLT-2)
are
a
new
class
of
hypoglycemic
drugs
that
were
initially
approved
for
the
treatment
type
diabetes.
Currently,
5
in
SGLT-2
by
FDA
glycemic
control:
canagliflozin,
dapagliflozin,
empagliflozin,
ertugliflozin
and
sotagliflozin.
However,
their
effectiveness
reducing
risk
heart
failure
progression
chronic
kidney
disease
was
soon
established,
regardless
diabetes
status.
In
addition,
according
to
number
meta-analyses
RCTs
patients
with
cardiometabolic
renal
diseases,
use
reduces
cardiovascular
overall
mortality
serious
adverse
cardiac
events
outcomes
or
without
diabetes,
which
is
reflected
indications
use.
Scientific
data
presented
discussion
mechanisms
cardioprotective
renoprotective
effects
class,
many
considered
as
pleiotropic
not
related
effect
on
levels.
Язык: Английский
Unraveling the Cardiac Matrix: From Diabetes to Heart Failure, Exploring Pathways and Potential Medications
Biomedicines,
Год журнала:
2024,
Номер
12(6), С. 1314 - 1314
Опубликована: Июнь 13, 2024
Myocardial
infarction
(MI)
often
leads
to
heart
failure
(HF)
through
acute
or
chronic
maladaptive
remodeling
processes.
This
establishes
coronary
artery
disease
(CAD)
and
HF
as
significant
contributors
cardiovascular
illness
death.
Therefore,
treatment
strategies
for
patients
with
CAD
primarily
focus
on
preventing
MI
lessening
the
impact
of
after
an
event.
fibrosis,
characterized
by
abnormal
extracellular
matrix
(ECM)
deposition,
is
central
cardiac
remodeling.
Understanding
these
processes
key
identifying
new
targets.
Recent
studies
highlight
SGLT2
inhibitors
(SGLT2i)
GLP-1
receptor
agonists
(GLP1-RAs)
favorable
options
in
managing
type
2
diabetes
due
their
low
hypoglycemic
risk
benefits.
review
explores
inflammation’s
role
fibrosis
evaluates
emerging
anti-diabetic
medications’
effectiveness,
such
SGLT2i,
GLP1-RAs,
dipeptidyl
peptidase-4
(DPP4i),
post-acute
MI.
were
analyzed
identify
effective
medications
reducing
patients.
By
addressing
areas,
we
can
advance
our
understanding
potential
benefits
post-MI
improve
patient
outcomes
individuals
at
HF.
Язык: Английский
Transforming Diabetes Care: The Expanding Role of DPP-4 Inhibitors in Cardiovascular and Renal Protection
Medicina,
Год журнала:
2024,
Номер
60(11), С. 1793 - 1793
Опубликована: Ноя. 1, 2024
The
approach
to
managing
type
2
diabetes
mellitus
(T2DM)
has
significantly
progressed,
evolving
beyond
strict
glycemic
control
addressing
the
wider
complications
associated
with
disease,
including
cardiovascular
disease
(CVD)
and
chronic
kidney
(CKD)
[...].
Язык: Английский
Bibliometric and visual analysis of SGLT2 inhibitors in cardiovascular diseases
Frontiers in Pharmacology,
Год журнала:
2024,
Номер
15
Опубликована: Окт. 30, 2024
Cardiovascular
diseases
(CVD)
pose
a
significant
threat
to
human
health
due
their
high
mortality
and
morbidity
rates.
Despite
advances
in
treatments,
the
prevalence
impact
of
cardiovascular
disease
continue
increase.
Sodium-glucose
transporter
2
inhibitors
(SGLT2i),
initially
approved
for
treatment
type
diabetes,
have
important
research
value
promising
applications
reducing
CVD
risk,
especially
heart
failure
(HF)
atherosclerosis
patients
with
(ASCVD).
This
study
aims
comprehensively
review
latest
progress,
trends,
cutting-edge
hot
spots,
future
development
directions
SGLT2i
field
through
bibliometric
analysis.
Язык: Английский
Vector of glycated hemoglobin in the formation of dysglycemia in postmenopause: Emphasis on early diagnosis and therapy
Meditsinskiy sovet = Medical Council,
Год журнала:
2024,
Номер
16, С. 135 - 147
Опубликована: Окт. 31, 2024
Introduction.
The
close
relationship
of
postmenopause
with
insulin
resistance
(IR)
and
metabolic
syndrome
(MetS)
marks
a
high
cardiometabolic
risk
dysglycemia,
determining
the
need
for
its
early
diagnosis
therapy.
Pathogenetically
substantiated
criteria
prediabetes
nature
drug
therapy
type
2
diabetes
mellitus
(T2DM)
are
debated.
Information
on
between
glucose
homeostasis
parameters
menopausal
MetS
is
fragmentary.
Aim.
To
evaluate
associations
glycated
hemoglobin
(HbA1c)
levels
indices
IR,
β-cell
function
character-
istics
in
cohort
postmenopausal
women
different
carbohydrate
states.
Materials
methods.
In
94
Caucasian
58.0
(53.0;
63.0)
years
old
following
were
determined:
HbA1c,
fasting
glycemia
(FG),
TyG
HOMA2
indices,
C-peptid,
BMI,
waist
circumference
(WC),
blood
pressure
(BP),
triglycerides
(TG),
HDL-C
levels.
When
classifying
by
HbA1c
(ADA
criteria),
15
had
normoglycemia,
24
prediabetes,
55
T2DM.
ME
(25–75%)
was
assessed
using
SPSS
(version
17);
intergroup
differences
according
to
Mann
–
Whitney
test;
Spearman
partial
correlation
analysis
performed.
Results.
age
independently
correlated
IR
parameters:
(R
=
0.590;
p
<
0.001),
HOMA2-IR
0.318;
0.05)
beta
cell
function:
HOMA2-B
-0.355;
0.001);
lipid
markers
(TG,
HDL-C,
respectively
R
0.382;
-0.448;
anthropometric
Conclusion
.
Associations
spectrum
mark
it
as
vector
formation
progression
dysglycemia
due
connection
functional
state
β-cells
importance
lipoglucotoxicity
dynamics
IR.
obtained
data
pathogenetically
determine
use
verification
administration
combined
antihyperglycemic
aimed
at
preserving
function.
potential
dipeptidyl
peptidase-4
inhibitors
slowing
considered
Язык: Английский