Recent development of single preparations and fixed-dose combination tablets for the treatment of non-insulin-dependent diabetes mellitus: A comprehensive summary for antidiabetic drugs

Archives of Pharmacal Research

Volumn 39, Issue 6, 2016, Pages 731-746

  Li, Jianwen ^a,b   Lian, He ^a  

^a SHENYANG PHARMACEUTICAL UNIVERSITY   (China)

^b GE HEALTHCARE   (China)

Author keywords

Drug efficiency and safety; FDCs; Fixed dose combination tablets; Medical treatment; NIDDM; Non insulin dependent diabetes mellitus; Single preparations

Indexed keywords

ANTIDIABETIC AGENT; DRUG COMBINATION;

DIABETES MELLITUS, TYPE 2; DRUG COMBINATION; DRUG DEVELOPMENT; HUMAN; METABOLISM; RISK FACTOR;

DIABETES MELLITUS, TYPE 2; DRUG COMBINATIONS; DRUG DISCOVERY; HUMANS; HYPOGLYCEMIC AGENTS; RISK FACTORS;

EID: 84969980955     PISSN: 02536269     EISSN: 19763786     Source Type: Journal    
DOI: 10.1007/s12272-016-0762-4     Document Type: Review

References (98)

1. Aroda VR, Ratner R (2011) The safety and tolerability of GLP-1 receptor agonists in the treatment of type 2 diabetes: a review. Diabetes Metab Res Rev 27:528–542
2. Aschner P, Katzeff HL, Guo H, Sunga S, Williams-Herman D, Kaufman KD, Goldstein BJ (2010) Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes. Diabetes Obes Metab 12:252–261
3. Association AD (2014a) Executive summary: standards of medical care in diabetes-2014. Diabetes Care 37:S5–S13
4. Association AD (2014b) Standards of medical care in diabetes-2014. Diabetes Care 37:S14–S80
5. AstraZeneca UK Limited (2014) Forxiga 5 mg & 10 mg film coated tablets. https://medicines.org.uk/emc/medicine/27188. Accessed 15 Oct 2014
6. Baetta R, Corsini A (2011) Pharmacology of dipeptidyl peptidase-4 inhibitors: similarities and differences. Drugs 71:1441–1467
7. Bell DS (2006) Do sulfonylurea drugs increase the risk of cardiac events? Can Med Assoc J 174:185–186
8. Bell DS (2013) Combine and conquer: advantages and disadvantages of fixed-dose combination therapy. Diabetes Obes Metab 15:291–300
9. Bell DS, Dharmalingam M, Kumar S, Sawakhande RB (2011) Triple oral fixed-dose diabetes polypill versus insulin plus metformin efficacy demonstration study in the treatment of advanced type 2 diabetes (TrIED study-II). Diabetes Obes Metab 13:800–805
10. Benford M, Milligan G, Pike J, Anderson P, Piercy J, Fermer S (2012) Fixed-dose combination antidiabetic therapy: real-world factors associated with prescribing choices and relationship with patient satisfaction and compliance. Adv Ther 29:26–40
11. Bottomley JM, Raymond FD (2007) Pharmaco-economic issues for diabetes therapy. Best Pract Res Clin Endocrinol Metab 21:657–685
12. Burki TK (2012) FDA rejects novel diabetes drug over safety fears. Lancet 379:507
13. Buse JB, DeFronzo RA, Rosenstock J, Kim T, Burns C, Skare S, Baron A, Fineman M (2016) The primary glucose-lowering effect of metformin resides in the gut, not the circulation: results from short-term pharmacokinetic and 12-week dose-ranging studies. Diabetes Care 39:198–205
14. Cheong C, Barner JC, Lawson KA, Johnsrud MT (2008) Patient adherence and reimbursement amount for antidiabetic fixed-dose combination products compared with dual therapy among Texas Medicaid recipients. Clin Ther 30:1893–1907
15. Cho YM, Kieffer TJ (2011) New aspects of an old drug: metformin as a glucagon-like peptide 1 (GLP-1) enhancer and sensitiser. Diabetologia 54:219–222
16. Chou HS, Palmer JP, Jones AR, Waterhouse B, Ferreira-Cornwell C, Krebs J, Goldstein BJ (2008) Initial treatment with fixed-dose combination rosiglitazone/glimepiride in patients with previously untreated type 2 diabetes. Diabetes Obes Metab 10:626–637
17. Consoli A, Formoso G (2013) Do thiazolidinediones still have a role in treatment of type 2 diabetes mellitus? Diabetes Obes Metab 15:967–977
18. Culy CR, Jarvis B (2001) Repaglinide: a review of its therapeutic use in type 2 diabetes mellitus. Drugs 61:1625–1660
19. Derosa G (2011) Pioglitazone is a valid alternative to rosiglitazone. Am J Cardiovasc Drugs 11:357–362
20. Dunn CJ, Peters DH (1995) Metformin: a review of its pharmacological properties and therapeutic use in non-insulin-dependent diabetes mellitus. Drugs 49:721–749
21. Elkinson S, Scott L (2013) Canagliflozin: first global approval. Drugs 73:979–988
22. El-Mir MY, Nogueira V, Fontaine E, Avéret N, Rigoulet M, Leverve X (2000) Dimethylbiguanide inhibits cell respiration via an indirect effect targeted on the respiratory chain complex I. J Biol Chem 275:223–228
23. Fisman EZ, Tenenbaum A, Boyko V, Benderly M, Adler Y, Friedensohn A, Kohanovski M, Rotzak R, Schneider H, Behar S, Motro M (2001) Oral antidiabetic treatment in patients with coronary disease: time-related increased mortality on combined glyburide/metformin therapy over a 7.7-year follow-up. Clin Cardiol 24:151–158
24. Garber AJ, Larsen J, Schneider SH, Piper BA, Henry D (2002) Simultaneous glyburide/metformin therapy is superior to component monotherapy as an initial pharmacological treatment for type 2 diabetes. Diabetes Obes Metab 4:201–208
25. Garber A, Henry R, Ratner R, Garcia-Hernandez PA, Rodriguez-Pattzi H, Olvera-Alvarez I, Hale PM, Zdravkovic M, Bode B (2009) Liraglutide versus glimepiride monotherapy for type 2 diabetes (LEAD-3 Mono): a randomised, 52-week, phase III, double-blind, parallel-treatment trial. Lancet 373:473–481
26. Giugliano D, Maiorino MI, Bellastella G, Chiodini P, Ceriello A, Esposito K (2011) Efficacy of insulin analogs in achieving the hemoglobin A1c target of <7% in type 2 diabetes: meta-analysis of randomized controlled trials. Diabetes Care 34:510–517
27. GlaxoSmithKline (2014) A comparison of atorvastatin and glimepiride fixed dose combination and atorvastatin and glimepiride loose combination in the treatment of patients with type 2 diabetes mellitus. https://clinicaltrials.gov/ct2/show/NCT01495013?term=glimepiride%2Fatorvastatin&rank=1. Accessed Jan 2014
28. Goldstein BJ, Pans M, Rubin CJ (2003) Multicenter, randomized, double-masked, parallel-group assessment of simultaneous glipizide/metformin as second-line pharmacologic treatment for patients with type 2 diabetes mellitus that is inadequately controlled by a sulfonylurea. Clin Ther 25:890–903
29. Gonzalez-Ortiz M, Guerrero-Romero JF, Violante-Ortiz R, Wacher-Rodarte N, Martinez-Abundis E, Aguilar-Salinas C, Islas-Andrade S, Arechavaleta-Granell R, Gonzalez-Canudas J, Rodriguez-Moran M, Zavala-Suarez E, Ramos-Zavala MG, Metha R, Revilla-Monsalve C, Beltran-Jaramillo TJ (2009) Efficacy of glimepiride/metformin combination versus glibenclamide/metformin in patients with uncontrolled type 2 diabetes mellitus. J Diabetes Complicat 23:376–379
30. Goodarzi MO, Bryer-Ash M (2005) Metformin revisited: re-evaluation of its properties and role in the pharmacopoeia of modern antidiabetic agents. Diabetes Obes Metab 7:654–665
31. Halimi S, Le Berre MA, Grange V (2000) Efficacy and safety of acarbose add-on therapy in the treatment of overweight patients with Type 2 diabetes inadequately controlled with metformin: a double-blind, placebo-controlled study. Diabetes Res Clin Pract 50:49–56
32. Hasan FM, Alsahli M, Gerich JE (2014) SGLT2 inhibitors in the treatment of type 2 diabetes. Diabetes Res Clin Pract 104:297–322
33. Henry RR, Murray AV, Marmolejo MH, Hennicken D, Ptaszynska A, List JF (2012) Dapagliflozin, metformin XR, or both: initial pharmacotherapy for type 2 diabetes, a randomised controlled trial. Int J Clin Pract 66:446–456
34. Hu FB (2011) Globalization of diabetes: the role of diet, lifestyle, and genes. Diabetes Care 34:1249–1257
35. Johnsson KM, Ptaszynska A, Schmitz B, Sugg J, Parikh SJ, List JF (2013) Vulvovaginitis and balanitis in patients with diabetes treated with dapagliflozin. J Diabetes Complicat 27:479–484
36. Kaku K, Inoue S, Matsuoka O, Kiyosue A, Azuma H, Hayashi N, Tokudome T, Langkilde AM, Parikh S (2013) Efficacy and safety of dapagliflozin as a monotherapy for type 2 diabetes mellitus in Japanese patients with inadequate glycaemic control: a phase II multicentre, randomized, double-blind, placebo-controlled trial. Diabetes Obes Metab 15:432–440
37. Kalra S (2014) Insulin degludec aspart: the first co-formulation of insulin analogues. Diabetes Ther 5:65–72
38. Kaul S, Diamond GA (2011) Is there clear and convincing evidence of cardiovascular risk with rosiglitazone? Clin Pharmacol Ther 89:773–776
39. Kawamori R, Matsuhisa M, Kinoshita J, Mochizuki K, Niwa M, Arisaka T, Ikeda M, Kubota M, Wada M, Kanda T, Ikebuchi M, Tohdo R, Yamasaki Y (1998) Pioglitazone enhances splanchnic glucose uptake as well as peripheral glucose uptake in non-insulin-dependent diabetes mellitus. AD-4833 Clamp-OGL Study Group. Diabetes Res Clin Pract 41:35–43
40. Krentz AJ, Bailey CJ (2005) Oral antidiabetic agents: current role in type 2 diabetes mellitus. Drugs 65:385–411
41. Lamanna C, Monami M, Marchionni N, Mannucci E (2011) Effect of metformin on cardiovascular events and mortality: a meta-analysis of randomized clinical trials. Diabetes Obes Metab 13:221–228
42. Landgraf R, Bilo HJG, Müller PG (1999) A comparison of repaglinide and glibenclamide in the treatment of type 2 diabetic patients previously treated with sulphonylureas. Eur J Clin Pharmacol 55:165–171
43. Lau DT, Nau DP (2004) Oral antihyperglycemic medication nonadherence and subsequent hospitalization among individuals with type 2 diabetes. Diabetes Care 27:2149–2153
44. Lee YJ, Han HJ (2007) Regulatory mechanisms of Na(+)/glucose cotransporters in renal proximal tubule cells. Kidney Int 72(Suppl):S27–S35
45. Lee H, Ko G (2014) Effect of metformin on metabolic improvement and gut microbiota. Appl Environ Microbiol 80:5935–5943
46. Leroux-Stewart J, Rabasa-Lhoret R, Chiasson J-L (2015) α-Glucosidase inhibitors. In: DeFronzo RA, Ferrannini E, Zimmet P, George K (eds) International textbook of diabetes mellitus, 4th edn. Wiley, New Jersey, pp 673–685
47. List JF, Woo V, Morales E, Tang W, Fiedorek FT (2009) Sodium-glucose cotransport inhibition with dapagliflozin in type 2 diabetes. Diabetes Care 32:650–657
48. Liu Y, Hong T (2014) Combination therapy of dipeptidyl peptidase-4 inhibitors and metformin in type 2 diabetes: rationale and evidence. Diabetes Obes Metab 16:111–117
49. Luk AOY, Lau ESH, So W-Y, Ma RCW, Kong APS, Ozaki R, Chow FCC, Chan JCN (2014) Prospective study on the incidences of cardiovascular-renal complications in Chinese patients with young-onset type 1 and type 2 diabetes. Diabetes Care 37:149–157
50. Madiraju AK, Erion DM, Rahimi Y, Zhang XM, Braddock DT, Albright RA, Prigaro BJ, Wood JL, Bhanot S, Macdonald MJ, Jurczak MJ, Camporez JP, Lee HY, Cline GW, Samuel VT, Kibbey RG, Shulman GI (2014) Metformin suppresses gluconeogenesis by inhibiting mitochondrial glycerophosphate dehydrogenase. Nature 510:542–546
51. Meier JJ, Nauck MA (2005) Glucagon-like peptide 1 (GLP-1) in biology and pathology. Diabetes Metab Res Rev 21:91–117
52. Meyer C, Woerle HJ, Dostou JM, Welle SL, Gerich JE (2004) Abnormal renal, hepatic, and muscle glucose metabolism following glucose ingestion in type 2 diabetes. Am J Physiol Endocrinol Metab 287:E1049–E1056
53. Miller RA, Chu Q, Xie J, Foretz M, Viollet B, Birnbaum MJ (2013) Biguanides suppress hepatic glucagon signalling by decreasing production of cyclic AMP. Nature 494:25–260
54. Mohan V, Yang W, Son HY, Xu L, Noble L, Langdon RB, Amatruda JM, Stein PP, Kaufman KD (2009) Efficacy and safety of sitagliptin in the treatment of patients with type 2 diabetes in China, India, and Korea. Diabetes Res Clin Pract 83:106–116
55. Mulherin AJ, Oh AH, Kim H, Grieco A, Lauffer LM, Brubaker PL (2011) Mechanisms underlying metformin-induced secretion of glucagon-like peptide-1 from the intestinal L cell. Endocrinology 152:4610–4619
56. Nauck M, Frid A, Hermansen K, Shah NS, Tankova T, Mitha IH, Zdravkovic M, During M, Matthews DR (2009) Efficacy and safety comparison of liraglutide, glimepiride, and placebo, all in combination with metformin, in type 2 diabetes: the LEAD (liraglutide effect and action in diabetes)-2 study. Diabetes Care 32:84–90
57. Nissen SE, Wolski K (2007) Effect of rosiglitazone on the risk of myocardial infarction and death from cardiovascular causes. N Engl J Med 356:2457–2471
58. Odawara M, Kadowaki T, Tajima N, Nishii M, Taniguchi T, Arjona Ferreira J (2011) Long-term safety, tolerability, and efficacy of the dipeptidyl peptidase-4 inhibitor sitagliptin in Japanese patients with type 2 diabetes. Diabetol Int 2:94–105
59. Ozbek M, Erdogan M, Karadeniz M, Cetinkalp S, Ozgen AG, Saygili F, Yilmaz C, Tuzun M (2006) Preprandial repaglinide decreases exogenous insulin requirements and HbA1c levels in type 2 diabetic patients taking intensive insulin treatment. Acta Diabetol 43:148–151
60. Pan F, Chernew ME, Fendrick AM (2008) Impact of fixed-dose combination drugs on adherence to prescription medications. J Gen Intern Med 23:611–614
61. Pandit V, Pai RS, Yadav V, Devi K, Surekha BB, Inamdar MN, Suresh S (2013) Pharmacokinetic and pharmacodynamic evaluation of floating microspheres of metformin hydrochloride. Drug Dev Ind Pharm 39:117–127
62. Parris ES, Lawrence DB, Mohn LA, Long LB (2005) Adherence to statin therapy and LDL cholesterol goal attainment by patients with diabetes and dyslipidemia. Diabetes Care 28:595–599
63. Paternostro-Bayles M, Wing RR, Robertson RJ (1989) Effect of life-style activity of varying duration on glycemic control in type II diabetic women. Diabetes Care 12:34–37
64. Perez A, Zhao Z, Jacks R, Spanheimer R (2009) Efficacy and safety of pioglitazone/metformin fixed-dose combination therapy compared with pioglitazone and metformin monotherapy in treating patients with T2DM. Curr Med Res Opin 25:2915–2923
65. Pérez-Monteverde A, Seck T, Xu L, Lee MA, Sisk CM, Williams-Herman DE, Engel SS, Kaufman KD, Goldstein BJ (2011) Efficacy and safety of sitagliptin and the fixed-dose combination of sitagliptin and metformin vs. pioglitazone in drug-naïve patients with type 2 diabetes. Int J Clin Pract 65:930–938
66. Perry C (2011) Liraglutide. Drugs 71:2347–2373
67. Pickup JC, Renard E (2008) Long-acting insulin analogs versus insulin pump therapy for the treatment of type 1 and type 2 diabetes. Diabetes Care 31(Suppl 2):140–145
68. Plosker G (2012) Dapagliflozin. Drugs 72:2289–2312
69. Poole RM, Nowlan ML (2014) Albiglutide: first global approval. Drugs 74:929–938
70. Pratley RE, Fleck P, Wilson C (2014) Efficacy and safety of initial combination therapy with alogliptin plus metformin versus either as monotherapy in drug-naïve patients with type 2 diabetes: a randomized, double-blind, 6-month study. Diabetes Obes Metab 16:613–621
71. Rahmoune H, Thompson PW, Ward JM, Smith CD, Hong G, Brown J (2005) Glucose transporters in human renal proximal tubular cells isolated from the urine of patients with non-insulin-dependent diabetes. Diabetes 54:3427–3434
72. Rao AD, Kuhadiya N, Reynolds K, Fonseca VA (2008) Is the combination of sulfonylureas and metformin associated with an increased risk of cardiovascular disease or all-cause mortality?: a meta-analysis of observational studies. Diabetes Care 31:1672–1678
73. Raskin P, Lewin A, Reinhardt R, Lyness W (2009a) Twice-daily and three-times-daily dosing of a repaglinide/metformin fixed-dose combination tablet provide similar glycaemic control. Diabetes Obes Metab 11:947–952
74. Raskin P, Lewin A, Reinhardt R, Lyness W (2009b) Twice-daily dosing of a repaglinide/metformin fixed-dose combination tablet provides glycaemic control comparable to rosiglitazone/metformin tablet. Diabetes Obes Metab 11:865–873
75. Reasner C, Olansky L, Seck TL, Williams-Herman DE, Chen M, Terranella L, Johnson-Levonas AO, Kaufman KD, Goldstein BJ (2011) The effect of initial therapy with the fixed-dose combination of sitagliptin and metformin compared with metformin monotherapy in patients with type 2 diabetes mellitus. Diabetes Obes Metab 13:644–652
76. Rendell M (2004) The role of sulphonylureas in the management of type 2 diabetes mellitus. Drugs 64:1339–1358
77. Rodbard HW, Jellinger PS, Davidson JA, Einhorn D, Garber AJ, Grunberger G, Handelsman Y, Horton ES, Lebovitz H, Levy P, Moghissi ES, Schwartz SS (2009) Statement by an American Association of Clinical Endocrinologists/American College of Endocrinology consensus panel on type 2 diabetes mellitus: an algorithm for glycemic control. Endocr Pract 15:540–559
78. Rosenstock J, Rood J, Cobitz A, Biswas N, Chou H, Garber A (2006) Initial treatment with rosiglitazone/metformin fixed-dose combination therapy compared with monotherapy with either rosiglitazone or metformin in patients with uncontrolled type 2 diabetes. Diabetes Obes Metab 8:650–660
79. Sanford M (2014) Dulaglutide: first global approval. Drugs 74:2097–2103
80. Sanofi (2014) Efficacy and Safety of the Fixed Dose Combination of Glimepiride + Metformin in Type 2 Diabetic Patients Inadequately Controlled (LEGEND). https://clinicaltrials.gov/ct2/show/NCT01699932?term=glimepiride%2Fmetformin&rank=12. Accessed May 2014
81. Scheen AJ (1997) Drug treatment of non-insulin-dependent diabetes mellitus in the 1990’s. Drugs 54:355–368
82. Scheen AJ (2012) DPP-4 inhibitors in the management of type 2 diabetes: a critical review of head-to-head trials. Diabetes Metab 38:89–101
83. Scheen AJ, Lefebvre PJ (1998) Oral antidiabetic agents. A guide to selection. Drugs 55:225–236
84. Schneider SH, Khachadurian AK, Amorosa LF, Clemow L, Ruderman NB (1992) Ten-year experience with an exercise-based outpatient life-style modification program in the treatment of diabetes mellitus. Diabetes Care 15:1800–1810
85. Shah M, Chandalia M, Adams-Huet B, Brinkley LJ, Sakhaee K, Grundy SM, Garg A (2009) Effect of a high-fiber diet compared with a moderate-fiber diet on calcium and other mineral balances in subjects with type 2 diabetes. Diabetes Care 32:990–995
86. Shaw RJ, Lamia KA, Vasquez D, Koo SH, Bardeesy N, Depinho RA, Montminy M, Cantley LC (2005) The kinase LKB1 mediates glucose homeostasis in liver and therapeutic effects of metformin. Science 310:1642–1646
87. Singh-Franco D (2015) Potential for dipeptidyl peptidase-4 inhibitor and sodium glucose cotransporter 2 inhibitor single-pill combinations. Expert Rev End Metab 10:305–317
88. Solun B, Marcoviciu D, Dicker D (2013) Dipeptidyl peptidase-4 inhibitors and their effects on the cardiovascular system. Curr Cardio Rep 15:382
89. Sripalakit P, Maphanta S, Neamhom P, Saraphanchotiwitthaya A, Polnok S, Yokubol D (2007) Comparative study on the bioequivalence of two formulations of pioglitazone tablet in healthy Thai male volunteers. Drug Dev Ind Pharm 33:1362–1368
90. Steffes MW, Sibley S, Jackson M, Thomas W (2003) β-Cell function and the development of diabetes-related complications in the diabetes control and complications Trial. Diabetes Care 26:832–836
91. Taylor SI, Kadowaki T, Kadowaki H, Accili D, Cama A, Mckeon C (1990) Mutations in insulin-receptor gene in insulin-resistant patients. Diabetes Care 13:257–279
92. Thule PM, Umpierrez G (2014) Sulfonylureas: a new look at old therapy. Curr Diab Rep 14:473
93. Van De Laar FA, Lucassen PL, Akkermans RP, Van De Lisdonk EH, Rutten GE, Van Weel C (2005) Alpha-glucosidase inhibitors for patients with type 2 diabetes: results from a cochrane systematic review and meta-analysis. Diabetes Care 28:154–163
94. Wang JS, Huang CN, Hung YJ, Kwok CF, Sun JH, Pei D, Yang CY, Chen CC, Lin CL, Sheu WH (2013) Acarbose plus metformin fixed-dose combination outperforms acarbose monotherapy for type 2 diabetes. Diabetes Res Clin Pract 102:16–24
95. Wiernsperger N, Bailey C (1999) The antihyperglycaemic effect of metformin: therapeutic and cellular mechanisms. Drugs 58:31–39
96. Wild S, Roglic G, Green A, Sicree R, King H (2004) Global prevalence of diabetes: estimates for the year 2000 and projections for 2030. Diabetes Care 27:1047–1053
97. Yki-Järvinen H (2004) Thiazolidinediones. N Engl J Med 351:1106–1118
98. Zhou G, Myers R, Li Y, Chen Y, Shen X, Fenyk-Melody J, Wu M, Ventre J, Doebber T, Fujii N, Musi N, Hirshman MF, Goodyear LJ, Moller DE (2001) Role of AMP-activated protein kinase in mechanism of metformin action. J Clin Invest 108:1167–1174