1. EFFICACY AND MECHANISM
DPP-4 INHIBITORS
EFFICACY AND MECHANISM
OF ACTION

2. DPP IV ACTION/INHIBITION
GIP GLP-1 (biologically
[1-42] [7-36 amide] active)
DPP IV action/
GIP GLP-1 (biologically
[3-42] [9-36 amide] inactive)
inhibition
/04

3. DHbA1c(%) -0.5 -1.0 EFFECT OF SITAGLIPTIN ON HbA1c:
CHANGE FROM BASELINE (HbA1c ~ 8.0%)
Diabetes Care 29:2638, 2006; Clin Ther 28:1556, 2006; Diabetolgia 49:2564, 2006
DHbA1c(%)
-0.5
-0.60
-0.67
-0.85
-1.0
Drug Naive
Metformin
Pioglitazone
ADDITION OF SITAGLIPTIN TO

4. Int J Clin Prac 63:1395, 2009; Diab Ob Metab 10:376, 2008
EFFECT OF SAXAGLIPTIN ON HbA1c: CHANGE FROM PLACEBO (BASELINE HbA1c ≈ 8.0%)
Int J Clin Prac 63:1395, 2009; Diab Ob Metab 10:376, 2008
Diab Care 32:1649, 2009; JCEM 94:4810, 2009
 HbA1c (%)
-0.5
-0.63
-0.64
-0.76
-0.83 -1
DRUG NAIVE
GLYBURIDE
METFORMIN
PIO/ROSI
ADDITION OF SAXAGLIPTIN TO:

5. DPP-4 Combo

6. ADDITION OF LIRAGLUTIDE VERSUS SITAGLIPTIN IN 665 METFORMIN-TREATED T2DM PATIENTS (HbA1c = 8.4%)
Pratley RE, Lancet 375: , 2010
SITA
LIRA mg
LIRA mg
0.5
0.9%
Decrement in HbA1c (%) 1
1.2%
1.5%
P<0.0001
1.5
P<0.0001 2

7. Decreased Incretin Effect Decreased Insulin Secretion
OMINOUS OCTET
Decreased Incretin Effect
Decreased Insulin Secretion
Increased
Lipolysis
Islet–a cell
HYPERGLYCEMIA
Increased
Glucose
Reabsorption
Neurotransmitter Dysfunction
Increased Glucagon Secretion
Increased
HGP
Decreased Glucose
Uptake
DeFronzo RA, Diabetes 58: , 2009