Combining a dipeptidyl peptidase-4 inhibitor, alogliptin, with pioglitazone improves glycaemic control, lipid profiles and β-cell function in db/db mice

British Journal of Pharmacology

Volumn 157, Issue 3, 2009, Pages 415-426

  Moritoh, Y ^a   Takeuchi, K ^a   Asakawa, T ^a   Kataoka, O ^a   Odaka, H ^a  

^a Pharmacology Research Laboratories I   (Japan)

Author keywords

Alogliptin; Db db mice; Dipeptidyl peptidase 4; Glucagon like peptide 1; Glucosedependent insulinotropic polypeptide; Incretin; Pancreatic islets; Pioglitazone; Type 2 diabetes mellitus

Indexed keywords

ADIPONECTIN; ALOGLIPTIN; DIPEPTIDYL PEPTIDASE IV; FATTY ACID; GLUCAGON; GLUCAGON LIKE PEPTIDE 1; GLUCOSE; GLYCOSYLATED HEMOGLOBIN; INCRETIN; INSULIN; LIPID; PIOGLITAZONE; TRANSCRIPTION FACTOR PDX 1; TRIACYLGLYCEROL; 2,4 THIAZOLIDINEDIONE DERIVATIVE; ANTIDIABETIC AGENT; DIPEPTIDYL PEPTIDASE IV INHIBITOR; DRUG DERIVATIVE; PIPERIDINE DERIVATIVE; URACIL;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DISEASE COURSE; DRUG EFFECT; DRUG EFFICACY; DRUG POTENTIATION; ENZYME ACTIVITY; FATTY ACID BLOOD LEVEL; FOOD INTAKE; GLUCOSE BLOOD LEVEL; GLYCEMIC CONTROL; LONG TERM CARE; MONOTHERAPY; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET ALPHA CELL; PANCREAS ISLET BETA CELL; PANCREAS ISLET CELL FUNCTION; PRIORITY JOURNAL; PROTEIN BLOOD LEVEL; SHORT COURSE THERAPY; TREATMENT DURATION; TREATMENT OUTCOME; TRIACYLGLYCEROL BLOOD LEVEL; ANIMAL; BLOOD; BODY WEIGHT; DEGRANULATION; DRUG COMBINATION; EATING; MALE; METABOLISM; PATHOPHYSIOLOGY; PHYSIOLOGY;

ADIPONECTIN; ANIMALS; ANTIGENS, CD26; BLOOD GLUCOSE; BODY WEIGHT; CELL DEGRANULATION; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DRUG THERAPY, COMBINATION; EATING; GLUCAGON; GLUCAGON-LIKE PEPTIDE 1; HYPOGLYCEMIC AGENTS; INSULIN; INSULIN-SECRETING CELLS; LIPIDS; MALE; MICE; PIPERIDINES; THIAZOLIDINEDIONES; URACIL;

EID: 70349918275     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2009.00145.x     Document Type: Article

References (45)

1. Cejvan K, Coy DH, Efendic S (2003). Intra-islet somatostatin regulates glucagon release via type 2 somatostatin receptors in rats. Diabetes 52(5): 1176-1181. (Pubitemid 36523353)
2. Ceriello A (2003). The possible role of postprandial hyperglycaemia in the pathogenesis of diabetic complications. Diabetologia 46 (Suppl. 1): M9-M16.
3. Ceriello A, Johns D, Widel M, Eckland DJ, Gilmore KJ, Tan MH (2005). Comparison of effect of pioglitazone with metformin or sulfonylurea (monotherapy and combination therapy) on postload glycaemia and composite insulin sensitivity index during an oral glucose tolerance test in patients with type 2 diabetes. Diabetes Care 28 (2): 266-272. (Pubitemid 40170924)
4. Charpentier G (2002). Oral combination therapy for type 2 diabetes. Diabetes Metab Res Rev 18 (Suppl. 3): S70-S76. (Pubitemid 35256588)
5. Deacon CF (2004). Therapeutic strategies based on glucagon-like peptide 1. Diabetes 53 (9): 2181-2189.
6. Del Prato S, Marchetti P (2004). Beta- and alpha-cell dysfunction in type 2 diabetes. Horm Metab Res 36 (11-12): 775-781. (Pubitemid 40115899)
7. Drucker DJ (2007). Dipeptidyl peptidase-4 inhibition and the treatment of type 2 diabetes: preclinical biology and mechanisms of action. Diabetes Care 30 (6): 1335-1343.
8. Drucker DJ, Nauck MA (2006). The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 368 (9548): 1696-1705.
9. Dunning BE, Gerich JE (2007). The role of alpha-cell dysregulation in fasting and postprandial hyperglycaemia in type 2 diabetes and therapeutic implications. Endocr Rev 28 (3): 253-283.
10. Farilla L, Hui H, Bertolotto C, Kang E, Bulotta A, Di Mario U et al. (2002). Glucagon-like peptide-1 promotes islet cell growth and inhibits apoptosis in Zucker diabetic rats. Endocrinology 143 (11): 4397-4408. (Pubitemid 35239574)
11. Feng J, Zhang Z, Wallace MB, Stafford JA, Kaldor SW, Kassel DB et al. (2007). Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. J Med Chem 50 (10): 2297-2300. (Pubitemid 46799241)
12. Garber AJ, Schweizer A, Baron MA, Rochotte E, Dejager S (2007). Vildagliptin in combination with pioglitazone improves glycaemic control in patients with type 2 diabetes failing thiazolidinedione monotherapy: a randomized, placebo-controlled study*. Diabetes Obes Metab 9 (2): 166-174. (Pubitemid 46206560)
13. Giorgino F, Laviola L, Leonardini A (2005). Pathophysiology of type 2 diabetes: rationale for different oral antidiabetic treatment strategies. Diabetes Res Clin Pract 68 (Suppl. 1): S22-S29. (Pubitemid 40805488)
14. Gromada J, Rorsman P (2004). New insights into the regulation of glucagon secretion by glucagon-like peptide-1. Harm Metab Res 36 (11-12): 822-829. (Pubitemid 40115905)
15. Heller RS, Aponte GW (1995). Intra-islet regulation of hormone secretion by glucagon-like peptide-l-(7-36) amide. Am J Physiol 269 (6 Pt 1): G852-G860. (Pubitemid 3020499)
16. Kjorholt C, Akerfeldt MC, Biden TJ, Laybutt DR (2005). Chronic hyperglycaemia, independent of plasma lipid levels, is sufficient for the loss of beta-cell differentiation and secretory function in the db/db mouse model of diabetes. Diabetes 54 (9): 2755-2763. (Pubitemid 41233599)
17. Lambeir AM, Durinx C, Scharpe S, De Meester I (2003). Dipeptidylpeptidase IV from bench to bedside: an update on structural properties, functions, and clinical aspects of the enzyme DPPIV. Crit Rev Clin Lab Sci 40 (3): 209-294. (Pubitemid 36775376)
18. Lee B, Shi L, Kassel DB, Asakawa T, Takeuchi K, Christopher RJ (2008). Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys. Eur J Pharmacol 589 (1-3): 306-314.
19. Li Y, Cao X, Li LX, Brubaker PL, Edlund H, Drucker DJ (2005). betaCell Pdx1 expression is essential for the glucoregulatory, proliferative, and cytoprotective actions of glucagon-like peptide-1. Diabetes 54 (2): 482-491.
20. Melloul D (2004). Transcription factors in islet development and physiology: role of PDX-I in beta-cell function. Ann N Y Acad Sci 1014: 28-37.
21. Miller S, St Onge EL (2006). Sitagliptin: a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Ann Pharmacother 40 (7-8): 1336-1343. (Pubitemid 44204964)
22. Mizushige K, Tsuji T, Noma T (2002). Pioglitazone: cardiovascular effects in prediabetic patients. Cardiovasc Drug Rev 20 (4): 329-340. (Pubitemid 36105784)
23. Moritoh Y, Takeuchi K, Asakawa T, Kataoka O, Odaka H (2008). Chronic administration of alogliptin, a novel, potent, and highly selective dipeptidyl peptidase-4 inhibitor, improves glycaemic control and beta-cell function in obese diabetic ob/ob mice. Eur J Pharmacol 588 (2-3): 325-332.
24. Mu J, Woods J, Zhou YP, Roy RS, Li Z, Zycband E et al. (2006) .Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic (beta)-cell mass and function in a rodent model of type 2 diabetes. Diabetes 55 (6): 1695-1704. (Pubitemid 44324122)
25. Nagakura T, Yasuda N, Yamazaki K, Ikuta H, Tanaka I (2003). Enteroinsular axis of db/db mice and efficacy of dipeptidyl peptidase IV inhibition. Metabolism 52 (1): 81-86.
26. Pejic RN, Lee DT (2006). Hypertriglyceridemia. J Am Board Fam Med 19 (3): 310-316.
27. Perfetti R, Hui H (2004). The role of GLP-1 in the life and death of pancreatic beta cells. Horm Metab Res 36 (11-12): 804-810. (Pubitemid 40115903)
28. Rendell MS, Jovanovic L (2006). Targeting postprandial hyperglycaemia. Metabolism 55 (9): 1263-1281.
29. Ristic S, Bates PC (2006). Vildagliptin: a novel DPP-4 inhibitor with pancreatic islet enhancement activity for treatment of patients with type 2 diabetes. Drugs Today (Bare) 42 (8): 519-531. (Pubitemid 44504260)
30. Rolin B, Larsen MO, Gotfredsen CF, Deacon CF, Carr RD, Wilken M et al. (2002). The long-acting GLP-1 derivative NN2211 ameliorates glycaemia and increases beta-cell mass in diabetic mice. Am J Physiol Endocrinol Metab 283 (4): E745-E752. (Pubitemid 35050813)
31. Rosenstock J, Brazg R, Andryuk PJ, Lu K, Stein P (2006). Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing pioglitazone therapy in patients with type 2 diabetes: a 24-week, multicenter, randomized, double-blind, placebocontrolled, parallel-group study. Clin Ther 28 (10): 1556-1568. (Pubitemid 44841980)
32. Rosenstock J, Baron MA, Camisasca RP, Cressier F, Couturier A, Dejager S (2007). Efficacy and tolerability of initial combination therapy with vildagliptin and pioglitazone compared with component monotherapy in patients with type 2 diabetes. Diabetes Obes Metab 9 (2): 175-185. (Pubitemid 46206561)
33. Scheen AJ (2007). Antidiabetic agents in subjects with mild dysglycaemia: prevention or early treatment of type 2 diabetes? Diabetes Metab 33 (1): 3-12.
34. Sloop KW, Cao JX, Siesky AM, Zhang HY, Bodenmiller DM, Cox AL et al. (2004). Hepatic and glucagon-like peptide-1-mediated reversal of diabetes by glucagon receptor antisense oligonucleotide inhibitors. J Clin Invest 113 (11): 1571-1581.
35. Sloop KW, Michael MD, Moyers JS (2005). Glucagon as a target for the treatment of type 2 diabetes. Expert Opin Ther Targets 9 (3): 593-600. (Pubitemid 40883156)
36. Strowski MZ, Parmar RM, Blake AD, Schaeffer JM (2000). Somatostatin inhibits insulin and glucagon secretion via two receptors subtypes: an in vitro study of pancreatic islets from somatostatin receptor 2 knockout mice. Endocrinology 141 (1): 111-117.
37. Taskinen MR (2003). Diabetic dyslipidaemia: from basic research to clinical practice. Diabetologia 46 (6): 733-749. (Pubitemid 36831401)
38. Tomkin GH (2008). Targets for intervention in dyslipidemia in diabetes. Diabetes Care 31 (Suppl. 2): S241-S248.
39. Turner RC, Cull CA, Frighi V, Holman RR (1999). Glycemic control with diet, sulfonylurea, metformin, or insulin in patients with type 2 diabetes mellitus: progressive requirement for multiple therapies (UKPDS 49). UK Prospective Diabetes Study (UKPDS) Group. JAMA 281 (21): 2005-2012. (Pubitemid 29254858)
40. Vilsboll T, Holst JJ (2004). Incretins, insulin secretion and type 2 diabetes mellitus. Diabetologia 47 (3): 357-366. (Pubitemid 38491230)
41. Waugh J, Keating GM, Plosker GL, Easthope S, Robinson DM (2006). Pioglitazone: a review of its use in type 2 diabetes mellitus. Drugs 66 (1): 85-109. (Pubitemid 43144963)
42. Wilding JP (2007). The importance of free fatty acids in the development of type 2 diabetes. Diabet Med 24 (9): 934-945.
43. Xu E, Kumar M, Zhang Y, Ju W, Obata T, Zhang N et al. (2006). Intra-islet insulin suppresses glucagon release via GABA-GABAA receptor system. Cell Metab 3 (1): 47-58.
44. Xu G, Kaneto H, Laybutt DR, Duvivier-Kali VF, Trivedi N, Suzuma K et al. (2007). Downregulation of GLP-1 and GIP receptor expression by hyperglycaemia: possible contribution to impaired incretin effects in diabetes. Diabetes 56 (6): 1551-1558. (Pubitemid 46842610)
45. Yki-Jarvinen H (2004). Thiazolidinediones. N Engl J Med 351 (11): 1106-1118.