SA JOURNAL OF DIABETES & VASCULAR DISEASE
REVIEW
VOLUME 9 NUMBER 1 • MARCH 2012
13
assessment report (EPAR) – scientific discussion. Available from URL: http://www.
emea.europa.eu/humandocs/PDFs/EPAR/januvia/H-722-en6.pdf. Accessed 5 July
2010.
Augeri DJ, Robl JA, Betebenner DA,
16.
et al.
Discovery and preclinical profile of
Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl
peptidase IV inhibitor for the treatment of type 2 diabetes.
J Med Chem
2005;
48
: 5025–5037.
European Medicines Agency (EMEA). Onglyza (saxagliptin) – European public
17.
assessment report (EPAR) –CHMP Assessment Report. Available from URL:
http://www.emea.europa.eu/humandocs/PDFs/EPAR/onglyza/H-1039-en6.pdf.
Accessed 5 July 2010.
Feng J, Zhang Z, Wallace MB,
18.
et al
. Discovery of alogliptin: a potent, selective,
bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.
J Med Chem
2007;
50
: 2297–2300.
Karim A, Bridson WE, Fleck P,
19.
et al
. Disposition of the dipeptidyl peptidase-4
inhibitor [14C] alogliptin benzoate ([14C]SYR-322) after oral administration to
healthy male subjects (Abstract). AAPS Annual Meeting and Exposition, 9–15
November 2007.
Eckhardt M, Langkopf E, Mark M,
20.
et al
. 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-
ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione
(BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4
inhibitor for the treatment of type 2 diabetes.
J Med Chem
2007;
50
: 6450–
6453.
Blech S, Ludwig-Schwellinger E, Gräfe-Mody EU, Withopf B, Wagner K. The
21.
metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin,
in humans.
Drug Metab Dispos
2010;
38
: 667–678.
Deacon CF. Dipeptidyl peptidase-4 inhibitors in the treatment of type 2 diabetes:
22.
a comparative review.
Diabetes Obes Metab
2011;
13
: 7–18.
Thomas L, Eckhardt M, Langkopf E, Tadayyon M, Himmelsbach F, Mark M.
23.
(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-
2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based
dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of
action compared with other dipeptidyl peptidase-4 inhibitors.
J Pharmacol Exp
Ther
2008;
325
: 175–182.
Covington P, Christopher R, Davenport M,
24.
et al.
Pharmacokinetic, pharmaco-
dynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor alogliptin:
a randomized, double-blind, placebo-controlled, multiple-dose study in adult
patients with type 2 diabetes.
Clin Ther
2008;
30
: 499–512.
Heise T, Graefe-Mody EU, Hüttner S, Ring A, Trommeshauser D, Dugi KA.
25.
Pharmacokinetics, pharmacodynamics and tolerability of multiple oral doses of
linagliptin, a dipeptidyl peptidase-4 inhibitor in male type 2 diabetes patients.
Diabetes Obes Metab
2009;
11
: 786–794.
He YL, Wang Y, Bullock JM et al. Pharmacodynamics of vildagliptin in patients
26.
with type 2 diabetes during OGTT
. J Clin Pharmacol
2007;
47
: 633–641.
Boulton DW, Geraldes M. Safety, tolerability, pharmacokinetics and
27.
pharmacodynamics of once daily oral doses of saxagliptin for 2 weeks in type
2 diabetic and healthy subjects (Poster 0606-P).
Diabetes
2007;
56
(Suppl. 1):
A161.
Burkey BF, Hoffmann PK, Hassiepen U, Trappe J, Juedes M, Foley JE. Adverse
28.
effects of dipeptidyl peptidases 8 and 9 inhibition in rodents revisited.
Diabetes
Obes Metab
2008;
10
: 1057–1061.
Kirby MS, Dorso C, Wang A,
29.
et al. In vitro
enzymologic characteristics of
saxagliptin, a highly potent and selective DPP4 inhibitor with “slow binding”
characteristic (Abstract).
Clin Chem Lab Med
2008;
46
: A79.
O’Brien P, O’Connor BF. Seprase: an overview of an important matrix serine
30.
protease.
Biochim Biophys Acta
2008;
1784
: 1130–1145.
Lankas GR, Leiting B, Roy RS,
31.
et al
. Dipeptidyl peptidase IV inhibition for the
treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl
peptidases 8 and 9.
Diabetes
2005;
54
: 2988–2994.
Herman GA, Stein PP, Thornberry NA, Wagner JA. Dipeptidyl peptidase-4 inhibitors
32.
for the treatment of type 2 diabetes: focus on sitagliptin.
Clin Pharmacol Ther
2007;
81
: 761–767.
He YL, Sadler BM, Sabo R,
33.
et al
. The absolute oral bioavailability and population-
based pharmacokinetic modelling of a novel dipeptidylpeptidase-IV inhibitor,
vildagliptin, in healthy volunteers.
Clin Pharmacokinet
2007;
46
: 787–802.
Fura A, Khanna A, Vyas V,
34.
et al
. Pharmacokinetics of the dipeptidyl peptidase
4 inhibitor saxagliptin in rats, dogs, and monkeys and clinical projections.
Drug
Metab Dispos
2009;
37
: 1164–1171.
Dittberner S, Duval V, Staab A, Troconiz I, Graefe-Mody U, Jaehde U.
35.
Determination of the absolute bioavailability of BI 1356, a substance with
nonlinear pharmacokinetics, using a population pharmacokinetic modelling
approach (abstract 1110). Poster presented at 16th Annual Meeting of the
Population Approach Group in Europe, København, Denmark; June 2007.
Available from URL: http://www.page-meeting.org/?abstract=1110. Accessed
5 July 2010.
Fuchs H, Binder R, Greischel A. Tissue distribution of the novel DPP-4 inhibitor
36.
BI 1356 is dominated by saturable binding to its target in rats.
Biopharm Drug
Dispos
2009;
30
: 229–240.
HermanGA, StevensC, VanDyckK,
37.
et al
. Pharmacokinetics andpharmacodynamics
of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results
from two randomized, double-blind, placebo-controlled studies with single oral
doses.
Clin Pharmacol Ther
2005;
78
: 675–688.
Christopher R, Covington P, Davenport M,
38.
et al.
Pharmacokinetics, pharmaco-
dynamics, and tolerability of single increasing doses of the dipeptidyl peptidase-4
inhibitor alogliptin in healthy male subjects.
Clin Ther
2008;
30
: 513–527.
Bergman AJ, Cote J, Yi B,
39.
et al.
Effect of renal insufficiency on the pharmacokinetics
of sitagliptin, a dipeptidyl peptidase-4 inhibitor.
Diabetes Care
2007;
30
: 1862–
1864.
Chan JC, Scott R, Arjona Ferreira JC,
40.
et al
. Safety and efficacy of sitagliptin in
patients with type 2 diabetes and chronic renal insufficiency.
Diabetes Obes
Metab
2008;
10
: 545–555.
Graefe-Mody U, Friedrich C, Port A,
41.
et al.
Linagliptin, a novel DPP-4 inhibitor:
no need for dose adjustment in patients with renal impairment (Abstract 822).
Diabetologia
2010;
53
(Suppl. 1): S326.
Press Release, 4th February 2008: Galvus
42.
®
, a new treatment for patients with type
2 diabetes, receives European approval for label update paving the way for EU
launches. Available from URL: http://www.medicalnewstoday.com/articles/95931.
php. Accessed 5 July 2010.
Ligueros-Saylan M, Foley JE, Schweizer A, Couturier A, Kothny W. An assessment
43.
of adverse effects of vildagliptin versus comparators on the liver, the pancreas,
the immune system, the skin and in patients with impaired renal function from a
large pooled database of Phase II and II clinical trials.
Diabetes Obes Metab
2010;
12
: 495–509.
Williams-Herman D, Engel SS, Round E,
44.
et al
. Safety and tolerability of sitagliptin
in clinical studies: a pooled analysis of data from 10,246 patients with type 2
diabetes.
BMC Endocr Disord
2010;
10
: 7.
Schweizer A, Dejager S, Foley JE, Couturier A, Ligueros-Saylan M, Kothny W.
45.
Assessing the cardio-cerebrovascular safety of vildagliptin: meta-analysis of
adjudicated events from a large phase III type 2 diabetes population.
Diabetes
Obes Metab
2010;
12:
485–494.
Frederich R, Alexander JH, Fiedorek FT,
46.
et al.
A systematic assessment of
cardiovascular outcomes in the saxagliptin drug development program for type 2
diabetes.
Postgrad Med
2010;
122
: 16–27.
Engel SS, Williams-Herman DE, Golm GT,
47.
et al.
Sitagliptin: review of preclinical
and clinical data regarding incidence of pancreatitis.
Int J Clin Pract
2010;
64
:
984–990.
Dore DD, Seeger JD, Arnold Chan K. Use of a claims-based active drug safety
48.
surveillance system to assess the risk of acute pancreatitis with exenatide or
sitagliptin compared to metformin or glyburide.
Curr Med Res Opin
2009;
25
:
1019–1027.
Scheen AJ, Charpentier G, Ostgren CJ, Hellqvist A, Gause-Nilsson I. Efficacy and
49.
safety of saxagliptin in combination with metformin compared with sitagliptin
in combination with metformin in adult patients with type 2 diabetes mellitus.
Diabetes Metab Res Rev
2010;
26
: 540–549.
Aschner P, Katzeff HL, Guo H,
50.
et al.
Efficacy and safety of monotherapy of
sitagliptin compared with metformin in patients with type 2 diabetes.
Diabetes
Obes Metab
2010;
12
: 252–261.
Schweizer A, Dejager S, Bosi E. Comparison of vildagliptin and metformin
51.
monotherapy in elderly patients with type 2 diabetes: a 24-week, double-blind,
randomized trial.
Diabetes Obes Metab
2009;
11
: 804–812.
Ferrannini E, Fonseca V, Zinman B,
52.
et al.
Fifty-two-week efficacy and safety of
vildagliptin vs. glimepiride in patients with type 2 diabetes mellitus inadequately
controlled on metformin monotherapy.
Diabetes Obes Metab
2009;
11
: 157–
166.
Nauck MA, Meininger G, Sheng D, Terranella L, Stein PP. Efficacy and safety of
53.
the dipeptidyl peptidase-4 inhibitor, sitagliptin, compared with the sulfonylurea,
glipizide, in patients with type 2 diabetes inadequately controlled on metformin
alone: a randomized, double-blind, non-inferiority trial.
Diabetes Obes Metab
2007;
9
: 194–205.
Bolli G, Dotta F, Rochotte E, Cohen SE. Efficacy and tolerability of vildagliptin vs.
54.
pioglitazone when added to metformin: a 24-week, randomized, double-blind
study.
Diabetes Obes Metab
2008;
10
: 82–90.
Scott R, Loeys T, Davies MJ, Engel SS. Efficacy and safety of sitagliptin when
55.
added to ongoing metformin therapy in patients with type 2 diabetes.
Diabetes
Obes Metab
2008;
10
: 959–969.