DPP-4阻害薬のすべて

出版社: 先端医学社
著者:
発行日: 2010-06-25
分野: 臨床医学:内科  >  糖尿病
ISBN: 9784884076245
電子書籍版: 2010-06-25 (第1版第1刷)
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GIP、GLP-1の基礎、さらにDPP-4の基礎とDPP-4阻害薬の糖尿病治療薬としての現状と展望について、わが国を代表するインクレチン研究の専門家による最新の動向と解説。

目次

  • DPP-4阻害薬のすべて

    ―目次―

    Part 1 インクレチンを知る
     インクレチンの概念と研究の歴史

    Part 2 インクレチンの基礎をみる
     1.GIPの基礎
     2.GLP-1の基礎
     3.その他のインクレチン

    Part 3 DPP-4の基礎をみる
     DPP-4の基礎

    Part 4 DPP-4阻害薬の基礎をみる
     1.DPP-4阻害薬の基礎薬理
     2.DPP-4阻害薬とインスリン/グルカゴン分泌
     3.DPP-4阻害薬のその他の作用

    Part 5 DPP-4阻害薬の臨床データをみる
     1.DPP-4阻害薬の臨床薬理
     2.DPP-4阻害薬の臨床成績
     
    Part 6 糖尿病治療の問題点と
         インクレイチン・DPP-4への期待を探る
     1.現在の2型糖尿病治療の問題点
     2.2型糖尿病とインクレチン作用

    Part 7 DPP-4阻害薬の臨床的意義と将来展望を探る
     1.DPP-4阻害薬の登場で日本の糖尿病治療はこう変わる
     2.DPP-4阻害薬と他の糖尿病治療薬との違い
     3.日本人の糖尿病治療におけるDPP-4阻害薬の位置づけ
     4.DPP-4阻害薬とβ細胞量増加
     5.QOLからみたDPP-4阻害薬の意義

この書籍の参考文献

参考文献のリンクは、リンク先の都合等により正しく表示されない場合がありますので、あらかじめご了承下さい。

本参考文献は電子書籍掲載内容を元にしております。

Part 1 インクレチンを知る

P.21 掲載の参考文献
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21) Ross SA, Brown JC, Dupre J : Hypersecretion of gastric inhibitory polypeptide following oral glucose in diabetes mellitus. Diabetes 26 : 525-529, 1977
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Part 2 インクレチンの基礎をみる

P.31 掲載の参考文献
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6) Takemura J, Seino Y, Yamamura T et al : The role of endogenous gastric inhibitory polypeptide in the enteroinsular axis. J Clin Endocrinol Metab 54 : 909-913, 1982
7) Usdin TB, Mezey E, Button DC et al : Gastric inhibitory polypeptide receptor, a member of the secretin-vasoactive intestinal peptide receptor family, is widely distributed in peripheral organs and the brain. Endocrinology 133 : 2861-2870, 1993
8) Yasuda K, Inagaki N, Yamada Y et al : Hamster gastric inhibitory polypeptide receptor expressed in pancreatic islets and clonal insulin-secreting cells : its structure and functional properties. Biochem Biophys Res Commun 205 : 1556-1562, 1994
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12) Kubota A, Yamada Y, Hayami T et al : Identification of two missense mutations in the GIP receptor gene : a functional study and association analysis with NIDDM : no evidence of association with Japanese NIDDM subjects. Diabetes 45 : 1701-1705, 1996
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Part 3 DPP - 4の基礎をみる

P.56 掲載の参考文献
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19) Chen X : Biochemical properties of recombinant prolyl dipeptidases DPP-IV and DPP8. Adv Exp Med Biol 575 : 27-32, 2006
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Part 4 DPP - 4阻害薬の基礎をみる

P.66 掲載の参考文献
1) Pei Z : From the bench to the bedside : dipeptidyl peptidase IV inhibitors, a new class of oral antihyperglycemic agents. Curr Opin Drug Discov Devel 11 : 512-532, 2008
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3) Croxtall JD, Keam SJ : Vildagliptin : a review of its use in the management of type 2 diabetes mellitus. Drugs 68 : 2387-2409, 2008
4) Dhillon S, Weber J : Saxagliptin. Drugs 69 : 2103-2114, 2009
5) Gallwitz B : Review of sitagliptin phosphate : a novel treatment for type 2 diabetes. Vasc Health Risk Manag 3 : 203-210, 2007
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7) Hansotia T, Baggio LL, Delmeire D et al : Double incretin receptor knockout (DIRKO) mice reveal an essential role for the enteroinsular axis in transducting the glucoregulatory actions of DPP-IV inhibitors. Diabetes 53 : 1326-1335, 2004
8) Nauck MA, Homberger E, Siegel EG et al : Incretin effects of increasing glucose loads in man calculated from venous insulin and C-peptide responses. J Clin Endocrinol Metab 63 : 492-498, 1986
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10) Yamamoto K, Hashimoto H, Tomimoto S et al : Overexpression of PACAP in transgenic mouse pancreatic β-cells enhances insulin secretion and ameliorates streptozotocin-induced diabetes. Diabetes 52 : 1155-1162, 2003
11) Ahren B, Hughes TE : Inhibition of dipeptidyl peptidase-4 augments insulin secretion in response to exogenously administered glucagon-like peptide-1, glucose-dependent insulinotropic polypeptide, pituitary adenylate cyclase-activating polypeptide, and gastrin-releasing peptide in mice. Endocrinology 146 : 2055-2059, 2005
12) Hamagami K, Sakurai Y, Shintani N et al : Over-expression of pancreatic pituitary adenylate cyclase-activating polypeptide (PACAP) aggrevates cerulein-induced acute pancreatitis in mice. J Pharmacol Sci 110 : 451-458, 2009
13) Lamont BJ, Drucker DJ : Differential antidiabetic efficacy of increin agonists versus DPP-4 inhibition in high fat-fed mice. Diabetes 57 : 190-198, 2008
14) Balas B, Baig MR, Watson C et al : The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab 92 : 1249-1255, 2007
15) Azuma K, Radikova Z, Mancino J et al : Measurements of islet function and glucose metabolism with the dipeptidyl peptidase 4 inhibitor vildagliptin in patients with type 2 diabetes. J Clin Endocrinol Metab 93 : 459-464, 2008
16) Duez H, Smith AC, Xiao C et al : Acute dipeptidyl peptidase-4 inhibition rapidly enhances insulin-mediated suppression of endogenous glucose production in mice. Endocrinology 150 : 56-62, 2009
17) Flock G, Baggio LL, Longuet C et al : Incretin receptors for glucagon-like peptide 1 and glucose-dependent insulinotropic polypeptide are essential for the sustained metabolic actions of vildagliptin in mice. Diabetes 56 : 3006-3013, 2007
18) Drucker DJ : Dipeptidyl peptidase-4 inhibition and the treatment of type 2 diabetes : preclinical biology and mechanisms of action. Diabetes Care 30 : 1335-1343, 2007
P.78 掲載の参考文献
1) Meier JJ, Gallwitz B, Salmen S et al : Normalization of glucose concentrations and deceleration of gastric emptying after solid meals during intravenous glucagon-like peptide 1 in patients with type 2 diabetes. J Clin Endocrinol Metab 88 : 2719-2725, 2003
2) Chia CW, Carlson OD, Kim W et al : Exogenous glucose-dependent insulinotropic polypeptide worsens post prandial hyperglycemia in type 2 diabetes. Diabetes 58 : 1342-1349, 2009
3) Mentlein R : Dipeptidyl-peptidase 4 (CD26) --role in the inactivation of regulatory peptides. Regul Pept 85 : 9-24, 1999
4) Zhu L, Tamvakopoulos C, Xie D et al : The role of dipeptidyl peptidase IV in the cleavage of glucagon family peptides : in vivo metabolism of pituitary adenylate cyclase activating Polypeptide- (1-38). J Biol Chem 278 : 22418-22423, 2003
5) Hansotia T, Baggio LL, Delmeire D et al : Double incretin receptor knockout (DIRKO) mice reveal an essential role for the enteroinsular axis in transducing the glucoregulatory actions of DPP-IV inhibitors. Diabetes 53 : 1326-1335, 2004
6) Nauck MA, El-Ouaghlidi A : The therapeutic actions of DPP-IV inhibition are not mediated by glucagon-like peptide-1. Diabetologia 48 : 608-611, 2005
7) Holst JJ, Deacon CF : Glucagon-like peptide-1 mediates the therapeutic actions of DPP-IV inhibitors. Diabetologia 48 : 612-615, 2005
8) Vilsboll T, Krarup T, Madsbad S et al : Both GLP-1 and GIP are insulinotropic at basal and postprandial glucose levels and contribute nearly equally to the incretin effect of a meal in healthy subjects. Regul Rept 114 : 115-121, 2003
9) Preitner F, Ibberson M, Franklin I et al : Gluco-incretins control insulin secretion at multiple levels as revealed in mice lacking GLP-1 and GIP receptors. J Clin Invest 113 635-645, 2004
10) Moens K, Heimberg H, Flamez D et al : Expression and functional activity of glucagon, glucagon-like peptide I, and glucose-dependent insulinotropic peptide receptors in rat pancreatic islet cells. Diabetes 45 : 257-261, 1996
11) Ding WG, Renstrom E, Rorsman P et al : Glucagon-like peptide I and glucose-dependent insulinotropic polypeptide stimulate Ca2+ -induced secretion in rat α-cells by a protein kinase A-mediated mechanism. Diabetes 46 : 792-800, 1997
12) Meier JJ, Gallwitz B, Siepmann N et al : Gastric inhibitory polypeptide (GIP) dose-dependently stimulates glucagon secretion in healthy human subjects at euglycaemia. Diabetologia 46 : 798-801, 2003
13) Tornehave D, Kristensen P, Romer J et al : Expression of the GLP-1 receptor in mouse, rat, and human pancreas. J Histochem Cytochem 56 : 841-851, 2008
14) Heller RS, Kieffer TJ, Habener JF : Insulinotropic glucagon-like peptide I receptor expression in glucagon-producing α-cells of the rat endocrine pancreas. Diabetes 46 : 785-791, 1997
15) Dillon JS, Lu M, Bowen S et al : The recombinant rat glucagon-like peptide-1 receptor, expressed in an α-cell line, is coupled to adenylyl cyclase activation and intracellular calcium release. Exp Clin Endocrinol Diabetes 113 : 182-189, 2005
16) Ishihara H, Maechler P, Gjinovci A et al : Islet β-cell secretion determines glucagon release from neighbouring α-cells. Nat Cell Biol 5 : 330-335, 2003
17) Slucca M, Harmon JS, Oseid EA et al : ATP-sensitive K+ channel mediates the zinc switch-off signal for glucagon response during glucose deprivation. Diabetes 59 : 128-134, 2010
18) Kawamori D, Kurpad AJ, Hu J et al : Insulin signaling in α cells modulates glucagon secretion in vivo. Cell Metab 9 : 350-361, 2009
19) Rorsman P, Salehi SA, Abdulkader F et al : KATP -channels and glucose-regulated glucagon secretion. Trends Endocrinol Metab 19 : 277-284, 2008
20) Foley JE, Ligueros-Saylan M, He YL et al : Effect of vildagliptin on glucagon concentration during meals in patients with type 1 diabetes. Horm Metab Res 40 : 727-730, 2008
21) Aschner P, Kipnes MS, Lunceford JK et al : Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 29 : 2632-2637, 2006
22) Meier JJ : The contribution of incretin hormones to the pathogenesis of type 2 diabetes. Best Pract Res Clin Endocrinol Metab 23 : 433-441, 2009
23) Mari A, Ferrannini E : β-cell function assessment from modelling of oral tests : an effective approach. Diabetes Obes Metab 10 (Suppl 4) : S77-S87, 2008
24) Xu L, Man CD, Charbonnel B et al : Effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on β-cell function in patients with type 2 diabetes : a model-based approach. Diabetes Obes Metab 10 : 1212-1220, 2008
25) Mari A, Scherbaum WA, Nilsson PM et al : Characterization of the influence of vildagliptin on model-assessed-cell function in patients with type 2 diabetes and mild hyperglycemia. J Clin Endocrinol Metab 93 : 103-109, 2008
26) Meier JJ, Deacon CF, Schmidt WE et al : Suppression of glucagon secretion is lower after oral glucose administration than during intravenous glucose administration in human subjects. Diabetologia 50 : 806-813, 2007
27) Ahren B, Schweizer A, Dejager S et al : Vildagliptin enhances islet responsiveness to both hyper- and hypoglycemia in patients with type 2 diabetes. J Clin Endocrinol Metab 94 : 1236-1243, 2009
28) Balas B, Baig MR, Watson C et al : The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab 92 : 1249-1255, 2007
P.84 掲載の参考文献
1) Verspohl EJ : Novel therapeutics for type 2 diabetes : incretin hormone mimetics (glucagon-like peptide-1 receptor agonists) and dipeptidyl peptidase-4 inhibitors. Pharmacol Ther 124 : 113-138, 2009
2) Thornberry NA, Gallwitz B : Mechanism of action of inhibitors of dipeptidyl-peptidase-4 (DPP-4). Best Pract Res Clin Endocrinol Metab 23 : 479-486, 2009
3) Conarello SL, Li Z, Ronan J et al : Mice lacking dipeptidyl peptidase IV are protected against obesity and insulin resistance. Proc Natl Acad Sci USA 100 : 6825-6830, 2003
4) Sudre B, Broqua P, White RB et al : Chronic inhibition of circulating dipeptidyl peptidase IV by FE 999011 delays the occurrence of diabetes in male Zucker diabetic fatty rats. Diabetes 51 : 1461-1469, 2002
5) Matveyenko AV, Dry S, Cox HI et al : Beneficial endocrine but adverse exocrine effects of sitagliptin in the human islet amyloid polypeptide transgenic rat model of type 2 diabetes : interactions with metformin. Diabetes 58 : 1604-1615, 2009
6) Mu J, Woods J, Zhou YP et al : Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic β-cell mass and function in a rodent model of type 2 diabetes. Diabetes 55 : 1695-1704, 2006
7) Pospisilik JA, Martin J, Doty T et al : Dipeptidyl peptidase IV inhibitor treatment stimulates β-cell survival and islet neogenesis in streptozotocin-induced diabetic rats. Diabetes 52 : 741-750, 2003
8) Scott R, Loeys T, Davies MJ et al : Efficacy and safety of sitagliptin when added to ongoing metformin therapy in patients with type 2 diabetes. Diabetes Obes Metab 10 : 959-969, 2008
9) Bolli G, Dotta F, Rochotte E et al : Efficacy and tolerability of vildagliptin vs. pioglitazone when added to metformin : a 24-week, randomized, double-blind study. Diabetes Obes Metab 10 : 82-90, 2008
10) Matikainen N, Manttari S, Schweizer A et al : Vildagliptin therapy reduces postprandial intestinal triglyceride-rich lipoprotein particles in patients with type 2 diabetes. Diabetologia 49 : 2049-2057, 2006
11) Azuma K, Radikova Z, Mancino J et al : Measurements of islet function and glucose metabolism with the dipeptidyl peptidase 4 inhibitor vildagliptin in patients with type 2 diabetes. J Clin Endocrinol Metab 93 : 459-464, 2008
12) Ahren B, Pacini G, Foley JE et al : Improved meal-related β-cell function and insulin sensitivity by the dipeptidyl peptidase-IV inhibitor vildagliptin in metformin-treated patients with type 2 diabetes over 1 year. Diabetes Care 28 : 1936-1940, 2005
13) Ahren B, Winzell MS, Wierup N et al : DPP-4 inhibition improves glucose tolerance and increases insulin and GLP-1 responses to gastric glucose in association with normalized islet topography in mice with β-cell-specific overexpression of human islet amyloid polypeptide. Regul Pept 143 : 97-103, 2007
14) Ahren B, Hughes TE : Inhibition of dipeptidyl peptidase-4 augments insulin secretion in response to exogenously administered glucagon-like peptide-1, glucose-dependent insulinotropic polypeptide, pituitary adenylate cyclase-activating polypeptide, and gastrin-releasing peptide in mice. Endocrinology 146 : 2055-2059, 2005

Part 5 DPP-4阻害薬の臨床データをみる

P.95 掲載の参考文献
1) Herman GA, Stevens C, Van Dyck K et al : Pharmacokinetics and pharmacodynamics 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 78 : 675-688, 2005
2) Bergman AJ, Stevens C, Zhou Y et al : Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor : a double-blind, randomized, placebo-controlled study in healthy male volunteers. Clin Ther 28 : 55-72, 2006
3) Narita H, Nonaka K, Stevens C et al : Multiple dose administration of sitagliptin, a dipeptidyl peptidase IV (DPP-IV) inhibitor, in healthy Japanese subjects. Diabetes 55 (Suppl 1) : A127, 2006
4) Herman GA, Bergman A, Stevens C et al : Effect of single oral doses of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on incretin and plasma glucose levels after an oral glucose tolerance test in patients with type 2 diabetes. J Clin Endocrinol Metab 91 : 4612-4619, 2006
5) He YL, Sabo R, Campestrini J et al : The effect of age, gender, and body mass index on the pharmacokinetics and pharmacodynamics of vildagliptin in healthy volunteers. Br J Clin Pharmacol 65 : 338-346, 2008
6) He YL, Wang Y, Bullock JM et al : Pharmacodynamics of vildagliptin in patients with type 2 diabetes during OGTT. J Clin Pharmacol 47 : 633-641, 2007
7) Balas B, Baig MR, Watson C et al : The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab 92 : 1249-1255, 2007
8) Ahren B, Landin-Olsson M, Jansson PA et al : Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes. J Clin Endocrinol Metab 89 : 2078-2084, 2004
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10) Bergman AJ, Cote J, Yi B et al : Effect of renal insufficiency on the pharmacokinetics of sitagliptin, a dipeptidyl peptidase-4 inhibitor. Diabetes Care 30 : 1862-1864, 2007
11) Chu XY, Bleasby K, Yabut J et al : Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, oganic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein. J Pharmacol Exp Ther 321 : 673-683, 2007
12) Migoya EM, Stevens CH, Bergman AJ et al : Effect of moderate hepatic insufficiency on the pharmacokinetics of sitagliptin. Can J Clin Pharmacol 16 : e165-e170, 2009
13) He H, Tran P, Yin H et al : Absorption, metabolism, and excretion of [14C] vildagliptin, a novel dipeptidyl peptidase 4 inhibitor, in humans. Drug Metab Dispos 37 : 536-544, 2009
14) Thuren T, Byiers S, Mohideen P et al : Vildagliptin is safe and well tolerated in patients with mild or moderate renal impairment. Diabetologia 50 (Suppl 1) : S1, 2007
P.105 掲載の参考文献
1) Nauck MA, Heimesaat MM, Orskov C et al : Preserved incretin activity of glucagon-like peptide 1 [7-36 amide] but not of synthetic human gastric inhibitory polypeptide in patients with type-2 diabetes mellitus. J Clin Invest 91 : 301-307, 1993
2) Vilsboll T, Krarup T, Madsbad S et al : Defective amplification of the late phase insulin response to glucose by GIP in obese type II diabetic patients. Diabetologia 45 : 1111-1119, 2002
3) Mu J, Woods J, Zhou YP et al : 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 : 1695-1704, 2006
4) Drucker DJ : Therapeutic potential of dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes. Expert Opin Investig Drugs 12 : 87-100, 2003
5) Aschner P, Kipnes MS, Lunceford JK et al : Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 29 : 2632-2637, 2006
6) Barzilai N, Mahone E, Guo H et al : Sitagliptin is well tolerated and leads to rapid improvement in blood glucose in the first days of monotherapy in patients aged 65 years and older with T2DM. ADA 69th poster sessions, 2009 (New Orleans, LA)
7) Nonaka K, Tsubouchi H, Okuyama K et al : Effects of once-daily sitagliptin on 24-h glucose control following 4 weeks of treatment in Japanese patients with type 2 diabetes mellitus. Horm Metab Res 41 : 232-237, 2009
8) Nonaka K, Kakikawa T, Sato A et al : Efficacy and safety of sitagliptin monotherapy in Japanese patients with type 2 diabetes. Diabetes Res Clin Pract 79 : 291-298, 2008
9) Scott R, Hartley P, Luo E et al : Use of sitagliptin in patients with type 2 diabetes (T2DM) and renal insufficiency (RI). Diabetes 55 (Suppl 1) : A462, 2006
10) Mistry GC, Maes AL, Lasseter KC et al : Effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on blood pressure in nondiabetic patients with mild to moderate hypertension. J Clin Pharmacol 48 : 592-598, 2008
11) Lumb AN, Gallen IW : Treatment of HNF1-alpha MODY with the DPP-4 inhibitor sitagliptin. Diabet Med 26 : 189-190, 2009
12) Karasik A, Charbonnel B, Liu J et al : Sitagliptin added to ongoing metfbrmin therapy enhanced glycemic control and beta-cell function in patients with type 2 diabetes. Diabetes 55 (Suppl 1) : A119, 2006
13) Williams-Herman D, Johnson J, Teng R et al : Efficacy and safety of initial combination therapy with sitagliptin and metformin in patients with type 2 diabetes : a 54-week study. Curr Med Res Opin 25 : 569-583, 2009
14) Kadowaki T, Tajima N, Odawara M et al : Sitagliptin added to ongoing treatment with metformin improved glycemic control and was well tolerated in Japanese patients with type 2 diabetes (T2DM). ADA 68th poster sessions, 2008 (San Francisco, CA)
15) Goldstein BJ, Feinglos MN, Lunceford JK et al : Effect of initial combination therapy with sitagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin on glycemic control in patients with type 2 diabetes. Diabetes Care 30 : 1979-1987, 2007
16) Rosenstock J, Brazg R, Andryuk PJ et al : 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, placebo-controlled, parallel-group study. Clin Ther 28 : 1556-1568, 2006
17) Kashiwagi A, Tajima N, Kadowaki T et al : Sitagliptin added to ongoing treatment with pioglitazone improved glycemic control and was well tolerated in Japanese patients with type 2 diabetes (T2DM). ADA 68th poster sessions, 2008 (San Francisco, CA)
18) Hermansen K, Kipnes M, Luo E et al : Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin. Diabetes Obes Metab 9 : 733-745, 2007
19) Tajima N, Kadowaki T, Odawara M et al : Sitagliptin added to ongoing treatment with Glimepiride improved glycemic control and was well tolerated in Japanese patients with type 2 diabetes (T2DM). ADA 68th poster sessions, 2008 (San Francisco, CA)
20) Vilsboll T, Rosenstock JM, Yki-Jarvinen H et al : Sitagliptin, a selective DPP-4 inhibitor, improves glycemic control when added to insulin, with or without metformin, in patients with type 2 Diabetes. ADA 69th poster sessions, 2009 (New Orleans, LA)
21) Williams-Herman D, Round E, Swern AS et al : Safety and tolerability of sitagliptin in patients with type 2 diabetes : a pooled analysis. BMC Endocr Disord 8 : 14, 2008
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25) Mu J, Petrov A, Eiermann GJ et al : Inhibition of DPP-4 with sitagliptin improves glycemic control and restores islet cell mass and function in a rodent model of type 2 diabetes. Eur J Pharmacol 623 : 148-154, 2009
P.121 掲載の参考文献
1) He YL, Sadler BM, Sabo R et al : The absolute oral bioavailability and population-based pharmacokinetic modelling of a novel dipeptidyl peptidase-IV inhibitor, vildagliptin, in healthy volunteers. Clin Pharmacokinet 46 : 787-802, 2007
2) Balas B, Baig MR, Watson C et al : The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab 92 : 1249-1255, 2007
3) Kikuchi M, Abe N, Kato M et al : Vildagliptin dose-dependently improves glycemic control in Japanese patients with type 2 diabetes mellitus. Diabetes Res Clin Pract 83 : 233-240, 2009
4) Iwamoto Y, Kashiwagi A, Yamada N et al : Vildagliptin versus voglibose monotherapy in patients with type 2 diabetes (T2DM) : superior efficacy and tolerability with vildagliptin. Diabetes 57 (suppl 1) : A167, 2008
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6) Croxtall JD, Keam SJ : Vildagliptin : a review of its use in the management of type 2 diabetes mellitus. Drugs 68 : 2387-2409, 2008
7) Dejager S, Razac S, Foley JE et al : Vildagliptin in drug-naive patients with type 2 diabetes : a 24-week, double-blind, randomized, placebo-controlled, multiple-dose study. Horm Metab Res 39 : 218-223, 2007
8) Pi-Sunyer FX, Schweizer A, Mills D et al : Efficacy and tolerability of vildagliptin monotherapy in drug-naive patients with type 2 diabetes. Diabetes Res Clin Pract 76 : 132-138, 2007
9) Pan C, Yang W, Barona JP et al : Comparison of vildagliptin and acarbose monotherapy in patients with type 2 diabetes : a 24-week, double-blind, randomized trial. Diabet Med 25 : 435-441, 2008
10) Rosenstock J, Baron MA, Dejager S et al : Comparison of vildagliptin and rosiglitazone monotherapy in patients with type 2 diabetes : a 24-week, double-blind, randomized trial. Diabetes Care 30 : 217-223, 2007
11) Nathan DM, Buse JB, Davidson MB et al : Management of hyperglycemia in type 2 diabetes : A consensus algorithm for the initiation and adjustment of therapy : a consensus statement from the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care 29 : 1963-1972, 2006
12) Schweizer A, Couturier A, Foley JE et al : Comparison between vildagliptin and metformin to sustain reductions in HbA (1c) over 1 year in drug-naive patients with type 2 diabetes. Diabet Med 24 : 955-961, 2007
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17) Fonseca V, Schweizer A, Albrecht D et al : Addition of vildagliptin to insulin improves glycaemic control in type 2 diabetes. Diabetologia 50 : 1148-1155, 2007
18) Bolli G, Dotta F, Rochotte E et al : Efficacy and tolerability of vildagliptin vs. pioglitazone when added to metformin : a 24-week, randomized, double-blind study. Diabetes Obes Metab 10 : 82-90, 2008
19) Ferrannini E, Fonseca V, Zinman B 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 11 : 157-166, 2009
20) Kothny W, Schweizer A, Dickinson S et al : Hepatic safety profile of vildagliptin, a new DPP-4 inhibitor for the treatment of type 2 diabetes. 45th Annual Meeting of European Association for the Study of Diabetes Abstract, 2009
21) Ligueros-Saylan M, Schweizer A, Dickinson S et al : Vildagliptin therapy is not associated with an increased risk of pancreatitis. 45th Annual Meeting of European Association for the Study of Diabetes Abstract, 2009
22) Foley J, Hoffmann P, Ligueros-Saylan M et al : Lack of vildagliptin effects on the immune system. 45th Annual Meeting of European Association for the Study of Diabetes Abstract, 2009

Part 6 糖尿病治療の問題点とインクレチン・DPP - 4への期待を探る

P.130 掲載の参考文献
1) 河盛隆造 : 第45回日本糖尿病学会年次学術集会 会長講演, 糖のながれのシステム生物学. 糖尿病 46 : 101-105, 2003
2) 河盛隆造 : ハーゲドーン賞受賞講演, 糖のながれにおける肝・糖取り込み率制御因子の解明. 糖尿病 49 : 771-773, 2006
3) Kawamori R, Morishima T, Ikeda M et al : Effect of strict metabolic control on glucose handling by the liver and peripheral tissues in non-insulin-dependent diabetes mellitus. Diabetes Res Clin Pract 23 : 155-161, 1994
4) Scheen AJ : Voglibose for prevention of type 2 diabetes mellitus. Lancet 373 : 1579-1580, 2009
5) Kawamori R, Tajima N, Iwamoto Y et al : Voglibose for prevention of type 2 diabetes mellitus : a randomized, double-blind trial in Japanese subjects with impaired glucose tolerance. Lancet 373 : 1607-1614, 2009
6) Ogihara T, Fujitani Y, Uchida T et al : Combined expression of transcription factors induces AR42J-B13 cells to differentiate into insulin-producing cells. Endocr J 55 : 691-698, 2008
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1) Baggio LL, Drucker DJ : Biology of incretins : GLP-1 and GIP. Gastroenterology 132 : 2131-2157, 2007
2) 宮川潤一郎, 美内雅之, 難波光義 : 2. GIP, GLP-1の多彩な作用 2) GLP-1. インクレチン治療-GLP-1受容体作動薬とDPP-4阻害薬による新たな糖尿病治療-, 清野裕監修, 稲垣暢也, 難波光義, 山田祐一郎編, フジメディカル出版, 大阪, 2009, pp26-40
3) Nauck MA, Stockmann F, Ebert R et al : Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia 29 : 46-52, 1986
4) Villsboll T, Krarup T, Deacon CF et al : Reduced postprandial concentrations of intact biologically active glucagon-like peptide 1 in type 2 diabetes patients. Diabetes 50 : 609-613, 2001
5) Toft-Nielsen MB, Damholt MB, Madsbad S et al : Determinants of the impaired secretion of glucagon-like peptide-1 in type 2 diabetic patients. J Clin Endocrinol Metab 86 : 3717-3723, 2001
6) Nauck MA, Heimesaat MM, Orskov C et al : Preserved incretin activity of glucagon-like peptide 1 [7-36 amide] but not of synthetic human gastric inhibitory polypeptide in patients with type-2 diabetes mellitus. J Clin Invest 91 : 301-307, 1993
7) Vollmer K, Holst JJ, Baller B et al : Predictors of incretin concentrations in subjects with normal, impaired, and diabetic glucose tolerance. Diabetes 57 : 678-687, 2008
8) Theodorakis MJ, Carlson O, Muller DC et al : Elevated plasma glucose-dependent insulinotropic polypeptide associates with hyperinsulinemia in impaired glucose tolerance. Diabetes Care 27 : 1692-1698, 2004
9) Kim W, Egan JM : The role of incretins in glucose homeostasis and diabetes treatment. Pharmacol Rev 60 : 470-512, 2008
10) Xu G, Kaneto H, Laybutt DR et al : Down-regulation of GLP-1 and GIP receptor expression by hyperglycemia : possible contribution to impaired incretin effects in diabetes. Diabetes 56 : 1551-1558, 2007
11) Shu L, Matveyenko AV, Kerr-Conte J et al : Decreased TCF7L2 protein levels in type 2 diabetes mellitus correlate with down-regulation of GIP- and GLP-1 receptors and impaired β-cell function. Hum Mol Genet 18 : 2388-2399, 2009

Part 7 DPP - 4阻害薬の臨床的意義と将来展望を探る

P.148 掲載の参考文献
1) 清野裕 : 糖尿病の新しい概念. 最新医学 50 : 639-645, 1995
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3) Rothenberg P, Kalbag J, Smith H et al : Treatment with a DPP-IV inhibitor, NVP-DPP728, increases prandial intact GLP-1 level and reduces glucose exposure in human. Diabetes 49 (suppl 1) : A39, 2000
4) Deacon CF, Nauck MA, Toft-Nielsen M et al : Both subcutaneously and intravenously administered glucagon-like peptide I are rapidly degraded from the NH2-terminus in type II diabetic patients and in healthy subjects. Diabetes 44 : 1126-1131, 1995
5) Nauck MA, Kleine N, Orskov C et al : Normalization of fasting hyperglycaemia by exogenous glucagon-like peptide 1 (7-36 amide) in type 2 (non-insulin-dependent) diabetic patients. Diabetologia 36 : 741-744, 1993
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7) Chiasson JL, Josse RG, Gomis R et al : Acarbose treatment and the risk of cardio-vascular disease and hypertension in patients with impaired glucose tolerance : the STOP-NIDDM trial. JAMA 290 : 486-494, 2003
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10) Balas B, Baig MR, Watson C et al : The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab 92 : 1249-1255, 2007
11) Brazg R, Xu L, Dalla Man C et al : Effect of adding sitagliptin, a dipeptidyl peptidase-4 inhibitor, to metformin on 24-h glycaemic control and β-cell function in patients with type 2 diabetes. Diabetes Obes Metab 9 : 186-193, 2007
12) Baggio LL, Drucker DJ : Biology of incretins : GLP-1 and GIP. Gastroenterology 132 : 2131-2157, 2007
13) Farilla L, Hui H, Bertolotto C et al : Glucagon-like peptide-1 promotes islet cell growth and inhibits apoptosis in Zucker diabetic rats. Endocrinology 143 : 4397-4408, 2002
14) Farilla L, Bulotta A, Hirshberg B et al : Glucagon-like peptide 1 inhibits cell apoptosis and improves glucose responsiveness of freshly isolated human islets. Endocrinology 144 : 5149-5158, 2003
15) Scherbaum WA, Schweizer A, Mari A et al : Evidence that vildagliptin attenuates deterioration of glycaemic control during 2-year treatment of patients with type 2 diabetes and mild hyperglycaemia. Diabetes Obes Metab 10 : 1114-1124, 2008
16) 菊池方利, 宇都宮一典, 守屋達美ほか : 2型糖尿病患者に対するビルダグリプチンの長期投与での臨床評価. 新薬と臨牀 59 : 137-154, 2010
P.153 掲載の参考文献
1) Mu J, Woods J, Zhou YP et al : 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 : 1695-1704, 2006
2) Iwamoto Y, Taniguchi T, Nonaka K et al : Dose-ranging efficacy of sitagliptin, a dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes mellitus. Endocr J, 2010, Mar 24 [Epub ahead of print]
3) Balas B, Baig MR, Watson C et al : The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab 92 : 1249-1255, 2007
4) D'Alessio DA, Denney AM, Hermiller LM et al : Treatment with the dipeptidyl peptidase-4 inhibitor vildagliptin improves fasting islet-cell function in subjects with type 2 diabetes. J Clin Endocrinol Metab 94 : 81-88, 2009
5) 菊池方利, 宇都宮一典, 守屋達美ほか : 2型糖尿病患者に対するビルダグリプチンの長期投与での臨床評価-ビルダグリプチン単独療法またはグリメピリドとの併用療法での52週間安全性試験-. 新薬と臨牀 59 : 137-154, 2010
6) Kikuchi M, Abe N, Kato M et al : Vildagliptin dose-dependently improves glycemic control in Japanese patients with type 2 diabetes mellitus. Diabetes Res Clin Pract 83 : 233-240, 2009
7) 菊池方利, 大西由希子, 羽田勝計ほか : 2型糖尿病におけるビルダグリプチンとグリメピリドの併用効果-二重盲検群間比較試験-. 糖尿病 52 (S1) : 257, 2009
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3) Holman RR, Paul SK, Bethel A et al : Long-term follow-up after tight control of blood pressure in type 2 diabetes. N Engl J Med 359 : 1565-1576, 2008
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