Oleh :
Billy
PT Dexa Medica
PHYTOCHEMICALS
No
Medicinal Plants
Contain of
Usage
Catharanthus roseus(formerly
known asVinca rosea)
Vincristine
Vinblastine
Cancer therapy
Digitalis purpurea
Digitoxin
Heart disease
Taxus baccata
Paclitaxel
Cancer therapy
Papaver somniferum
Opium
Analgetic
Galega officinalis
metformin
OAD
DEVELOPMENT
PROCESS
Fractionatio
n, Isolation,
Synthesis
Inlacin
Extraction &
Fractionation
Fractionation
followed by
Molecular
Screening
Extraction
Drying
DLBS, 2010
FACILITIES
October 2010
August 2011
January 2011
June 2011
Bioactive Fraction
DLBS3233
Target gen/Target Protein
DLBS3233
(Lagerstroemin dan
Cinamommum sebagai
bioactive)
Lagerstroemin, an
ellagitannin
Improvement of Insulin
Resistance with INLACIN
(DLBS3233)
Inlacin (DLBS3233)
MECHANISM
Phosporylation on the right
insulin receptor
TNF
CLINICAL
STUDY
Trial ID
Projects
Therapy
1.
DLBS32
330209
Safety study in
Healthy volunteers
(Phase-1)
Prof. K Suastika, Dr. RR
Tjandrawinata
2.
DLBS32
330309
Preliminary study in
T2DM
RS Sanglah, Denpasar
Prof. Ketut Suastika
3.
DLBS32
330411
Sampl
e
size
6
Inlacin vs Placebo
20
54
No
Trial ID
Projects
Therapy
Sampl
e size
4.
DLBS32 Pre DM
33-0711 RS M.Djamil, Padang
Prof. Asman Manaf
DLBS3233 capsule
50 mg (od), titration
at W4 to 100 mg (if
necessary) vs
placebo capsule of
DLBS3233 (od),
titration at W4 (if
necessary
80
5.
DLBS32 PCOS
33-0811 RS Cipto
Mangunkusumo,
Dr. Andon +
RSHS, Bandung,
Dr. Wiryawan
DLBS3233 capsule
100 mg (once daily)
and placebo tablet of
Metformin (twice
daily) vs Metformin
tablet 500 mg
(twice daily) and
placebo capsule of
DLBS3233 (once daily)
124
6.
DLBS3233 capsule
100 mg (od) vs
104
FASTING PLASMA
GLUCOSE
POST-PRANDIAL PLASMA
GLUCOSE
HbA1c REDUCTION 6
WEEKS
Diabetes
Complication
Diabetes-related
death
21%
Myocardial Infarction
14%
Stroke
12%
Peripheral vascular
disease
43%
HOMA-IR REDUCTION
LIPID PROFILE
PROFILE SAFETY
Paramete
r
SGPT
Group
Placebo
DLBS 50
mg
Alkalin
Placebo
Phosphata DLBS 50
se
mg
Serum
Placebo
Creatinin DLBS 50
mg
Baseline
Mean (SD)
End of
study
Mean (SD)
18.20 (12.38) 18.33 (13.63)
30.50 (10.81) 21.86 (16.28)
77.30 (6.05)
75.63 (21.59)
77.22 (6.40)
73.43 (9.67)
0.76 (0.14)
0.78 (0.15)
0.76 (0.19)
0.79 (0.16)
DLBS3233
IN PRIMARY PREVENTION OF TYPE
2 DIABETES MELLITUS
[DIPPER-DM]
Study site : M.Djamil Hospital, Padang
Principal Investigator : Prof. Dr. dr. Asman Manaf, SpPD-KEMD
165
164.97
160.37
160
155
151.06
150
145.94
Glucose Level (mg/dL)
DLBS 3233
145
Placebo
140
135
130
125
120
Baseline
143.36
Week 8
137.95
Week 12
REDUCTION IN FASTING TG
Reduction in Fasting Tryglyceride
0
Week 8
Week 12
p = versus baseline
level in each group
-5
-10
*P =
0.082
*P =
0.080
-12.71
Triglyceride Level (mg/dL)
-15
-15.06
-20
*P =
0.007
*P =
0.003
-25
-26.2
-30
-28.5
DLBS 3233
Placebo
SURABAYA INLACIN
STUDY
Study in patient with diabetes
INSULIN
RECEPTOR BINDING AFFINITY
1
DECREASED TNF
5
(due to PPAR
FFA, then PKC & , & Apn)
thus SERINE
PHOSPHORYLATION (I.R.)
RESISTIN
2
TYROSINE PHOSPHORYLATIO
TYROSINE
PHOSPHORYLATION
INSULIN
RESISTANCE (I.R.):
DLBS-3233
(INLACIN)
THE NOVEL
INSULIN SENSITIZER
2016
4 STIMULATE GLUT-4
FROM
CYTOPLASM TO CELL
TRANSLOCATION
MEMBRANE
8
ACC1 & ACC2,
Malonyl CoA
-Oxidation, FFA
ADIPONECTIN
0.0
0-
5.0
010.0
015.0
020.0
025.0
030.0
035.0
0
18.98
FPG
11.71
Week 6
Week
12
p = 0.298
p = 0.072
Week
Delta vs
baseline
SD
p versus
baseline
Mean
SD
187,10
167,00
72,25
58,85
-18,98
69,14
0,072
175,64
65,42
-11,71
64,21
0,298
0.0
05.00
10.0
0
15.00
20.0
0
25.0
0
30.0
0
35.0
0
40.0
0
GLUCOSE
GLUCOSE (PPG)
(PPG)
PPG
23.31
26.06
Week 6
Week
12
*p=
0.047
Week
*p=
0.021
Delta vs
baseline
SD
p versus
baseline
Mean
SD
275,46
250,22
80,88
70,84
-23,31
76,14
0,047*
(mg/dL)
One hour plasma glucose at Week
12
249,92
74,13
-26,06
70,08
0,021*
1C
0.0A1C
00.1
00.200.300.400.500.600.700.800.901.00
A1C
-0.36
A1C
12% subjects
reached A1c <
7.0% within 12
weeks of
treatment
Week 6
Week
12
-0.65
*p=
0.009
Week
*p=
0.001
Delta vs
baseline
SD
p versus
baseline
Mean
SD
9,67
2,11
9,34
2,21
-0,36
1,13
0,009*
9,02
2,04
-0,65
1,58
0,001*
Delta HOMA-IR
0.0
00.2
0
-0.40
-0.50
-0.77
-0.60
HOMA
-R
-0.80
-1.00
-1.20
-1.40
HOMA-R
Week 6
Week
12
p = 0.281
*p=
0.043
Week
Delta vs
baseline
SD
p versus
baseline
Mean
SD
4,59
3,45
3,69
2,41
-0,77
3,19
0,043*
4,09
2,72
-0,50
3,45
0,281
9 BODY WEIGHT
8 ADIPONECTIN
(Apn)
+0.45g/mL
(W 6: 8.99%)
p = 0.148 (NS)
+1.05g/mL (W 12: 21.18%)
p = 0.001
7TRIGLYCERIDE
-8.39 mg/dL (p = 0.405)
-8,00 mg/dL (p =
0217)
TOTAL
-11.49 mg/dL (W 6:
CHOLESTEROL
5.05%)
p=
-10.39 mg/dL
0.002(W 12:
4.56%)
p=
0.013
CHOLESTEROL
6.93%)
p=
-10.59 mg/dL
0.006 (W 12:
7.31%)
p=
0.020
A1C
-0.36 % (W 6: 3.69%) p
= 0.009
-0.65 % (W 12:
6.76%)
p=
0.001
HOMA-R
-0.77 (W 6: 16.84%) p =
0.043
-0.50 (W 12: 10.88%) p =
0.281 (NS)
PACK
HNA/BOX
HNA/CAPSULE
DOSAGE
INLACIN 50 mg
BOX, 5 STRIPS
@ 6 CAPSULES
Rp. 120.000,-
Rp. 4.000,-
Once daily
INLACIN 100
mg
BOX, 5 STRIPS
@ 6 CAPSULES
Rp. 150.000,-
Rp. 5.000,-
Once daily
DOSAGE:
Newly Diagnosed DM: 1 x 50-100 mg/ day
ADD ON with the other OADs: 1 x 100 mg/day
CONCLUSIONS
80% incidence of type 2 diabetes is caused by
insulin resistance
INLACIN is a bioactive fraction DLBS3233
INLACIN can improve insulin resistance
through four working mechanisms, namely:
1)
2)
3)
4)
INLACIN
PUBLICATION
http://www.foodnavigator-asia.com/Business/Indonesianherbal-diabetic-drug-to-target-EU-and-Asia