ライフサイエンスコーパス: sitagliptin

1 rial Evaluating Cardiovascular Outcomes With Sitagliptin).

2 nsulin lispro, liraglutide, pioglitazone, or sitagliptin).

3 tive synthesis of the antihyperglycemic drug sitagliptin.

4 ditional glucose lowering when combined with sitagliptin.

5 ly increased by metformin and not changed by sitagliptin.

6 unteers in response to a single oral dose of sitagliptin.

7 active site, but not small molecules such as sitagliptin.

8 ale manufacture of the antidiabetic compound sitagliptin.

9 CI -1.7 to -1.4) significantly more than did sitagliptin (-0.9%, -1.1 to -0.7) or pioglitazone (-1.2%

10 de (-1.24%, -1.37 to -1.11, n=221) than with sitagliptin (-0.90%, -1.03 to -0.77, n=219).

11 95% CI, 0.70 to 0.99) for saxagliptin versus sitagliptin, 0.63 (CI, 0.47 to 0.85) for saxagliptin ver

12 nts on 1.8 mg; 46 [21%] on 1.2 mg) than with sitagliptin (10 [5%]).

13 were randomly assigned (2:1) to receive oral sitagliptin (100 mg for participants >/=18 years, 50 mg

14 agents, and the second after the addition of sitagliptin (100 mg once daily) for approximately 4 week

15 , the influence of metformin (2,000 mg/day), sitagliptin (100 mg/day), or their combination, on GLP-1

16 HF rats was treated with the DPPIV inhibitor sitagliptin (40 mg/kg BID) for 6 weeks, whereas the rema

17 rm effect on cardiovascular events of adding sitagliptin, a dipeptidyl peptidase 4 inhibitor, to usua

18 A highly efficient synthesis of sitagliptin, a potent and selective DPP-4 inhibitor for

19 The dipeptidyl peptidase-4 inhibitor sitagliptin, an antidiabetic agent, which lowers blood g

20 Of 14671 patients, 7332 were randomized to sitagliptin and 7339 to placebo.

21 The antidiabetic drugs sitagliptin and exenatide, which inhibit GLP-1 breakdown

22 We postulated that sitagliptin and lansoprazole would preserve beta-cell fu

23 establish the extent and mechanisms by which sitagliptin and metformin singly and in combination modi

24 Post-hHF all-cause death was similar in the sitagliptin and placebo groups (29.8% vs 28.8%, respecti

25 in 3.1% (n = 228) and 3.1% (n = 229) of the sitagliptin and placebo groups, respectively (unadjusted

26 ed with the dipeptidyl peptidase-4 inhibitor sitagliptin and the glucagon-like peptide-1 mimetic exen

27 -0.9 to -0.4, p<0.0001) for exenatide versus sitagliptin, and -0.3% (-0.6 to -0.1, p=0.0165) for exen

28 -to-treat analysis (160 on exenatide, 166 on sitagliptin, and 165 on pioglitazone).

29 eceive once weekly exenatide, 172 to receive sitagliptin, and 172 to receive pioglitazone.

30 e for lixisenatide, alogliptin, saxagliptin, sitagliptin, and insulin glargine.

31 logue liraglutide versus the DPP-4 inhibitor sitagliptin, as adjunct treatments to metformin, in indi

32 Sitagliptin attenuated glycemic excursions in healthy le

33 As expected, sitagliptin augmented plasma-intact GIP substantially an

34 d randomly assigned 277 to treatment; 138 to sitagliptin-basal and 139 to basal-bolus.

35 ean daily blood glucose concentration in the sitagliptin-basal group (9.5 mmol/L [SD 2.7]) was not in

36 lycaemia occurred in 13 patients (9%) in the sitagliptin-basal group and in 17 (12%) in the basal-bol

37 ts (5%) developed acute kidney injury in the sitagliptin-basal group and six (4%) in the basal-bolus

38 failure occurred in 22 patients (16%) in the sitagliptin-basal group versus 26 (19%) in the basal-bol

39 agliptin plus basal glargine once daily (the sitagliptin-basal group) or a basal-bolus regimen with g

40 calcium modulating compounds, dantrolene and sitagliptin, both prevent cytokine and ER stress-induced

41 ing and postload intact GLP-1 increased with sitagliptin but not with metformin.

42 After oral glucose, only sitagliptin, but not metformin, significantly augmented

43 was not observed in users of saxagliptin or sitagliptin compared with other selected antihyperglycem

44 s occurred similarly among patients who took sitagliptin compared with other therapies (P=.20).

45 Compared with placebo, sitagliptin decreased intestinal lipoprotein concentrati

46 to -1.7) was significantly greater than with sitagliptin (difference -1.5 kg, 95% CI -2.4 to -0.7, p=

47 the effects of exenatide (GLP-1 agonist) and sitagliptin (DPP-4 inhibitor) during periodontitis induc

48 formin enhanced hepatic insulin sensitivity; sitagliptin enhanced extrahepatic insulin sensitivity wi

49 radiofrequency LV-ablated rats treated with sitagliptin exhibited a significant attenuation of HF-re

50 Liraglutide was superior to sitagliptin for reduction of HbA(1c), and was well toler

51 rial Evaluating Cardiovascular Outcomes With Sitagliptin]) found that these agents neither increased

52 mary outcome occurred in 839 patients in the sitagliptin group (11.4%; 4.06 per 100 person-years) and

53 The combination of metformin and sitagliptin had synergistic actions to preserve beta-cel

54 The DPP4i sitagliptin has been shown to be noninferior to placebo

55 In conclusion, sitagliptin increased intact GLP-1 and GIP through DPP-4

56 Sitagliptin increased plasma glucagon-like peptide-1 (7-

57 Metformin more than sitagliptin inhibited beta-cell apoptosis.

58 Sitagliptin (Januvia(R)) uses a transaminase in the fina

59 This pleiotropic effect of sitagliptin may explain the reduction in postprandial li

60 SEARCH DESIGN AND HIP rats were treated with sitagliptin, metformin, sitagliptin plus metformin, or n

61 o difference in total hHF events between the sitagliptin (n = 345) and placebo (n = 347) groups (unad

62 No heterogeneity for the effect of sitagliptin on hHF was observed in subgroup analyses acr

63 neous liraglutide once daily, or 100 mg oral sitagliptin once daily (n=219).

64 ly plus oral placebo once daily; 100 mg oral sitagliptin once daily plus injected placebo once weekly

65 re commonly reported among patients who took sitagliptin or exenatide as compared with other therapie

66 Use of sitagliptin or exenatide increased the odds ratio for re

67 been suggested to be a risk associated with sitagliptin or exenatide therapy in humans.

68 roid cancer, and all cancers associated with sitagliptin or exenatide, compared with other therapies.

69 id addition of maximum daily doses of either sitagliptin or pioglitazone.

70 y, we assigned 14,671 patients to add either sitagliptin or placebo to their existing therapy.

71 ses of the dipeptidyl peptidase-4 inhibitor, sitagliptin, or the thiazolidinedione, pioglitazone, in

72 ly assigned patients (1:1) to receive either sitagliptin plus basal glargine once daily (the sitaglip

73 Treatment with sitagliptin plus basal insulin is as effective and safe

74 Sitagliptin plus metformin had synergistic effects to pr

75 ts were treated with sitagliptin, metformin, sitagliptin plus metformin, or no drug as controls for 1

76 eta-Cell function was partially preserved by sitagliptin plus metformin.

77 icacy of a dipeptidyl peptidase-4 inhibitor (sitagliptin) plus basal insulin with a basal-bolus insul

78 In addition, sitagliptin preserves function of the ER calcium pump, s

79 es the total waste generated per kilogram of sitagliptin produced in comparison with the first-genera

80 mmonly-used well-tolerated antihyperglycemic sitagliptin, produces a dose-dependent reduction in seiz

81 chronic dipeptidyl peptidase-4 inhibition by sitagliptin protected against ischemic left ventricular

82 Sitagliptin reduced the serum concentration of DPP-4.

83 Pharmacological blockade of CD26, via Sitagliptin, reduced growth of InvEE tumours, while comb

84 als with induced periodontitis that received sitagliptin (SG); 3) animals with induced periodontitis

85 After oral glucose, metformin increased and sitagliptin significantly decreased (by 53%) total GLP-1

86 Mellitus and Acute Coronary Syndrome]), and sitagliptin (TECOS [Trial Evaluating Cardiovascular Outc

87 rial Evaluating Cardiovascular Outcomes With Sitagliptin (TECOS).

88 arbose, the dipeptidyl-peptidase 4-inhibitor sitagliptin, the glucagon-like peptide 1-receptor agonis

89 e and in combination with the DPP4 inhibitor sitagliptin; these only modestly increased GLP-1 ( appro

90 ipeptidyl peptidase-4 inhibitor therapy with sitagliptin to the treatment regime of patients with typ

91 d established cardiovascular disease, adding sitagliptin to usual care did not appear to increase the

92 Sitagliptin treatment also attenuated cardiac remodeling

93 However, adverse actions of sitagliptin treatment on exocrine pancreas raise concern

94 However, sitagliptin treatment was associated with increased panc

95 Insulin secretion with sitagliptin treatment was similarly stimulated with oral

96 Exenatide and sitagliptin treatments have led to a lower percentage of

97 Sitagliptin use does not affect the risk for hHF in T2DM

98 78 553 saxagliptin users and 298 124 sitagliptin users contributed an average of 7 to 9 month

99 minantly stimulates GIP but not GLP-1) after sitagliptin versus control in 12 healthy lean, 12 obese,

100 lfonylureas, and 0.71 (CI, 0.64 to 0.78) for sitagliptin versus insulin.

101 zard ratios were 0.74 (CI, 0.64 to 0.85) for sitagliptin versus pioglitazone, 0.86 (CI, 0.77 to 0.95)

102 us pioglitazone, 0.86 (CI, 0.77 to 0.95) for sitagliptin versus sulfonylureas, and 0.71 (CI, 0.64 to

103 Patients were randomized to sitagliptin vs placebo added to standard care.

104 controlled study evaluating the CV safety of sitagliptin vs placebo, each added to usual antihypergly

105 in levels (least-squares mean difference for sitagliptin vs. placebo, -0.29 percentage points; 95% co

106 The efficacy of liraglutide versus sitagliptin was assessed hierarchically by a non-inferio

107 Sitagliptin was noninferior to placebo for the primary c

108 To determine whether sitagliptin was noninferior to placebo, we used a relati

109 treatment differences for liraglutide versus sitagliptin were -0.60% (95% CI -0.77 to -0.43, p<0.0001

110 t frequent adverse events with exenatide and sitagliptin were nausea (n=38, 24%, and n=16, 10%, respe

111 0.15 mol % of Rh(I)/(t)Bu JOSIPHOS, affords sitagliptin, which is finally isolated as its phosphate

112 nd has been successfully employed to produce sitagliptin with 99.5% ee and 91% assay yield.