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Publications (4)11.44 Total impact

  • [Show abstract] [Hide abstract] ABSTRACT: To investigate the efficacy and tolerability of vildagliptin, a potent and selective dipeptidyl peptidase-4 inhibitor, as add-on to glimepiride in Japanese patients with Type 2 diabetes mellitus (T2DM) who were inadequately controlled. This 12-week, randomized, double-blind, placebo-controlled study compared vildagliptin 50mg twice-daily (n=102) with placebo (n=100) when added to a stable dose of glimepiride (>or=1mg/d). Treatment groups were balanced at baseline (glycosylated hemoglobin [HbA(1c)], 7.9%; fasting plasma glucose, 163.8 mg/dL). During treatment HbA(1c) decreased progressively with vildagliptin, but remained unchanged with placebo. The adjusted mean change (AMDelta) at endpoint was -1.0+/-0.1 and -0.1+/-0.1% in vildagliptin- and placebo-treated patients (between-group Delta=-1.0+/-0.1%, P<0.001). A greater proportion of vildagliptin-treated patients had HbA(1c) <or=6.5% compared to placebo-treated patients (45% vs. 3%, P<0.001). The AMDelta FPG was -20.9+/-2.8 mg/dL with vildagliptin compared to 6.3+/-2.8 mg/dL with placebo (between-group Delta=-27.2+/-3.9 mg/dL, P<0.001). Patients in vildagliptin and placebo groups reported similar incidences of adverse events (AEs) (59.8% vs. 57.0%), serious AEs (0% vs. 2.0%), suspected drug-related AEs (21.6% vs. 23.0%), and discontinuation due to AEs (1.0% vs. 3.0%). Hypogylcaemia was reported in two (vildagliptin) and one (placebo) patient. Vildagliptin is effective and well tolerated as an add-on to glimepiride in Japanese patients with T2DM.
    No preview · Article · Sep 2010 · Diabetes research and clinical practice
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    [Show abstract] [Hide abstract] ABSTRACT: To confirm the efficacy of vildagliptin in patients with type 2 diabetes (T2D) by testing the hypothesis that glycosylated haemoglobin (HbA1c) reduction with vildagliptin is superior to that with voglibose after 12 weeks of treatment. In this 12-week, randomized, double-blind, active-controlled, parallel-group study, the efficacy and safety of vildagliptin (50 mg bid, n = 188) was compared with that of voglibose (0.2 mg tid, n = 192) in patients with T2D who were inadequately controlled with diet and exercise. The characteristics of two groups were well matched at baseline. The mean age, body mass index (BMI) and HbA1c were 59.1 years, 24.9 kg/m(2) and 7.6%, respectively. At baseline, fasting plasma glucose (FPG) and 2-h postprandial glucose (PPG) were 9.01 mmol/l (162.2 mg/dl) and 13.57 mmol/l (244.3 mg/dl), respectively. The adjusted mean change in HbA1c from baseline to endpoint was -0.95 +/- 0.04% in the vildagliptin-treated patients and -0.38 +/- 0.04% in those receiving voglibose (between-group change = 0.57 +/- 0.06%, 95% confidence interval (CI) (-0.68 to -0.46%), p < 0.001), showing that vildagliptin was superior to voglibose. Endpoint HbA1c < or = 6.5% was achieved in 51% vildagliptin-treated patients compared with 24% patients who were on voglibose (p < 0.001). Vildagliptin also exhibited significantly (p < 0.001) greater reduction compared with voglibose in both FPG [1.34 vs. 0.43 mmol/l (24.1 vs. 7.8 mg/dl)] and 2-h PPG [2.86 vs. 1.1 mmol/l (51.5 vs. 19.8 mg/dl)]. Overall adverse events (AEs) were lower in the vildagliptin-treated patients compared with that in the voglibose-treated patients (61.2 vs. 71.4%), with no incidence of hypoglycaemia and serious adverse events with vildagliptin. Gastrointestinal AEs were significantly lower with vildagliptin compared with that of the voglibose (18.6 vs. 32.8%; p = 0.002). Vildagliptin (50 mg bid) showed superior efficacy and better tolerability compared with voglibose in Japanese patients with T2D.
    Full-text · Article · Aug 2010 · Diabetes Obesity and Metabolism
  • [Show abstract] [Hide abstract] ABSTRACT: エクア®はノバルティス ファーマ社で創製されたビルダグリプチンを有効成分とする新規経口糖尿病薬である.ビルダグリプチンはin vitroにおいて,組換えヒトdipeptidyl peptidase IV(DPP-4)に高い親和性で結合すると共に(Ki = 2~3 nM),ヒト血漿DPP-4を強力に阻害した(IC50 = 2.7 nM).2型糖尿病患者にビルダグリプチン(50 mg,1日2回)を反復投与すると,血漿DPP-4活性は24時間にわたって90%以上阻害され,活性型glucagon-like peptide-1(GLP-1)濃度が上昇した.2型糖尿病患者にビルダグリプチンを単回投与すると,インスリン分泌が亢進すると共にグルカゴン分泌が低下し,血糖値が低下した.しかし,血糖値が正常な健康被験者にビルダグリプチン(100 mg)を投与してもインスリン分泌の有意な亢進を認めず,また血糖値の有意な低下を認めなかった.2型糖尿病患者にビルダグリプチン(50 mg,1日2回)を反復投与すると,膵βおよびα細胞機能が改善すると共に,インスリン抵抗性が改善した.また,動物実験において,ビルダグリプチン(30または60 mg/kg)は膵β細胞の分化促進ならびにアポトーシスの抑制作用を示したことから,膵β細胞に対する保護作用が示唆された.ヒトにおける経口投与時のビルダグリプチンの吸収は速やかで,バイオアベイラビリティは良好であった(BA = 85%).ビルダグリプチンの投与後血漿中未変化体濃度は用量の増加に応じて上昇し,約2時間の半減期で消失した.ビルダグリプチンは臨床で併用が予想される様々な薬剤との薬物間相互作用が検討されているが,薬物動態への明らかな影響は認められなかった.2型糖尿病患者を対象に,HbA1c値の低下量を指標として臨床試験が実施された.ビルダグリプチン(10,25,50 mg,1日2回)の12週間投与では,用量依存性が確認された.ビルダグリプチン(50 mg,1日2回),またはボグリボースの12週間投与では,ビルダグリプチンの優越性が検証された.グリメピリドとの12週間併用投与では,プラセボに対するビルダグリプチン(50 mg,1日2回)の優越性が検証された.さらにビルダグリプチンの単独療法,もしくはグリメピリドとの併用療法の52週間投与では,長期投与時の安全性と有効性が確認された.これらの臨床試験における低血糖発現率は低く忍容性は良好であった.以上のように,ビルダグリプチンは経口投与で有効な選択的DPP-4阻害薬であり,血漿GLP-1濃度を上昇させ,膵島機能を改善すると共にインスリン抵抗性を改善した.ビルダグリプチンは2型糖尿病患者を対象とした臨床試験で優れた有効性と安全性を示したことから,新しいタイプの経口糖尿病治療薬として期待される.
    No preview · Article · Jan 2010 · Folia Pharmacologica Japonica
  • [Show abstract] [Hide abstract] ABSTRACT: To assess the efficacy and tolerability of vildagliptin (10, 25 or 50mg bid) in Japanese patients with type 2 diabetes mellitus (T2DM). This 12-week, multicenter, randomized, double-blind, placebo-controlled, parallel-group study was performed in 291 patients. The primary assessment was change from baseline to endpoint in HbA1c. Baseline HbA1c averaged 7.4%, and the between-treatment difference (vildagliptin-placebo) in the HbA1c adjusted mean change was -0.8%, -1.0% and -1.2% with vildagliptin 10, 25 and 50mg bid, respectively (p<0.001). Relative to baseline, body weight did not change significantly in vildagliptin groups. There was no increase in incidence of adverse events in the vildagliptin groups (62.0%, 62.5% and 61.8%, 10, 25 and 50mg bid, respectively) compared to placebo (73.6%). No deaths or drug-related serious adverse events were reported. Seven hypoglycemic events were observed (four events (n=3), two events (n=2), and one event (n=1) in the vildagliptin 10 and 50mg bid, and placebo, respectively) and none of them were severe or dose related. Vildagliptin 50mg bid was considered to be the most effective and well-tolerated dose, and therefore can be considered the recommended clinical dose for Japanese patients with T2DM.
    No preview · Article · Feb 2009 · Diabetes research and clinical practice