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 ale manufacture of the antidiabetic compound sitagliptin.

4 ion by 37 +/- 12% during DPP-4 inhibition by sitagliptin.

5 the dipeptidyl peptidase 4 (DPP-4) inhibitor sitagliptin.

6 tients chronically taking the DPP4 inhibitor sitagliptin.

7 risk of the primary end point compared with sitagliptin.

8 r liraglutide, and 427 (380 to 483) days for sitagliptin.

9 er, glargine), glimepiride, liraglutide, and sitagliptin.

10 drug molecules, for example, bortezomib and sitagliptin.

11 gine, liraglutide, and glimepiride than with sitagliptin.

12 odels alone or in treatment combination with sitagliptin.

13 us GIP to the effects of the DPP-4 inhibitor sitagliptin.

14 patient pairs who initiated empagliflozin or sitagliptin.

15 us a hypocaloric diet or the DPP-4 inhibitor sitagliptin.

16 on during treatment with the DPP-4 inhibitor sitagliptin.

17 DS events during ART, declined markedly with sitagliptin.

18 tive synthesis of the antihyperglycemic drug sitagliptin.

19 ditional glucose lowering when combined with sitagliptin.

20 ly increased by metformin and not changed by sitagliptin.

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

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

23 lives were estimated for sotalol (0.7 h) and sitagliptin (0.2 h) along the shortest flowpath.

24 7, 95% confidence interval 0.43 to 0.75) and sitagliptin (0.55, 0.41 to 0.73).

25 with glargine (1.3%), liraglutide (1.0%), or sitagliptin (0.7%).

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

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

28 95% CI, 0.70 to 0.99) for saxagliptin versus sitagliptin, 0.63 (CI, 0.47 to 0.85) for saxagliptin ver

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

30 glucose-lowering drugs (pioglitazone 30 mg, sitagliptin 100 mg and canagliflozin 100 mg).

31 trial of 16 weeks of treatment with each of sitagliptin 100 mg once daily, canagliflozin 100 mg once

32 adjustments to 3, 7, or 14 mg once daily or sitagliptin 100 mg once daily.

33 and obesity were recruited and treated with sitagliptin 100 mg QD on Day 1-5, followed by a combinat

34 QD on Day 1-5, followed by a combination of sitagliptin 100 mg QD with dorzagliatin 75 mg BID at sec

35 le dose adjustments of oral semaglutide with sitagliptin 100 mg.

36 muL CD4 cells were randomized to 16 weeks of sitagliptin 100 mg/day vs placebo in a multicenter trial

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

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

39 two randomized, 13-day treatment courses of sitagliptin (100 mg/day) and placebo, respectively.

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

41 tential contribution of GIP to the effect of sitagliptin (100%), defined as the difference between th

42 lower than those with glimepiride (30.4) and sitagliptin (38.1).

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

44 glycemic control (HbA1c on pioglitazone 59.5 sitagliptin 59.9, canagliflozin 60.5 mmol mol(-1), P = 0

45 the three drugs: pioglitazone 59.6 mmol/mol, sitagliptin 60.0 mmol/mol and canagliflozin 60.6 mmol/mo

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

47 e peptide-1 receptor agonist liraglutide, or sitagliptin, a dipeptidyl peptidase 4 inhibitor.

48 to patients, we investigated the effects of sitagliptin, a dipeptidyl peptidase-4 (DPP4) inhibitor a

49 T2D patients initiating empagliflozin versus sitagliptin, a dipeptidyl peptidase-4 inhibitor.

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

51 s with cardiovascular disease history and to sitagliptin across all patient subgroups.

52 sulin glargine, glimepiride, liraglutide, or sitagliptin, added to baseline metformin, in GRADE (Glyc

53 We show that sitagliptin administration via drinking water (50 and 10

54 3 SGLT2i initiators vs. 43 352 initiators of sitagliptin aged >=65 years with type 2 diabetes and HF

55 ts well-known effects on glucose metabolism, sitagliptin also prevents the degradation of NPY, thereb

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

57 These sitagliptin-analogue precursors could potentially intera

58 ) preferred pioglitazone, 158 patients (35%) sitagliptin and 175 patients (38%) canagliflozin.

59 At 3 mo, 61.54% of sitagliptin and 43.48% of placebo patients had a normal

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

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

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

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

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

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

66 no differences in HbA1c at 3 or 6 mo between sitagliptin and placebo groups.

67 saline but were 5- to 10-fold higher during sitagliptin and the combination of sitagliptin/sacubitri

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

69 ssue in patients who received liraglutide or sitagliptin and then reported these add-on therapies to

70 isk of HHF (relative to both liraglutide and sitagliptin) and the modified MACE outcome (relative to

71 -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

72 98.14 (90% CI, 83.73, 115.03) in combination/sitagliptin, and 100.34 (90% CI, 96.08, 104.79) and 102.

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

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

75 itagliptin cohort, 11 257 for tirzepatide vs sitagliptin, and 28 100 for tirzepatide vs semaglutide.

76 inetic interactions between dorzagliatin and sitagliptin, and an improvement of glycemic control unde

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

78 caemic control and weight loss compared with sitagliptin, and with a safety profile consistent with s

79 ff study drug was 27.56 + 52.74 mg/dL in the sitagliptin arm and -0.14 + 45.80 mg/dL in the placebo a

80 treatment) was 141.00 +/- 62.44 mg/dL in the sitagliptin arm and 165.22 +/- 72.03 mg/dL ( P = 0.218)

81 follow-up) was 174.38 +/- 77.93 mg/dL in the sitagliptin arm and 171.86 +/- 83.69 ng/dL ( P = 0.918)

82 Relative to placebo, the sitagliptin arm had 47% greater decline in CXCL10 (95% c

83 New use of semaglutide, tirzepatide, or sitagliptin as a placebo proxy.

84 utcome trials, SUSTAIN-6 (semaglutide versus sitagliptin as placebo proxy) and SURPASS-CVOT (tirzepat

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

86 Sitagliptin attenuated glycemic excursions in healthy le

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

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

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

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

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

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

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

94 A novel synthesis of sitagliptin based on a redox-active ester derived from t

95 Sitagliptin before cardiac surgery was associated with a

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

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

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

99 Liraglutide and diet, but not sitagliptin, caused weight loss.

100 patients were included in the semaglutide vs sitagliptin cohort, 11 257 for tirzepatide vs sitaglipti

101 s liraglutide (cohort 1) or empagliflozin vs sitagliptin (cohort 2).

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

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

104 ons, indicating that early intervention with sitagliptin could be an effective strategy for treating

105 Compared with placebo, sitagliptin decreased intestinal lipoprotein concentrati

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

107 or the active pharmaceutical ingredient for sitagliptin, diflunisal, and other pharmaceutically impo

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

109 Compared with sitagliptin, empagliflozin was associated with reduced r

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

111 were higher with oral semaglutide than with sitagliptin (estimated mean change in bodyweight, treatm

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

113 We tested whether early intervention with sitagliptin for hyperglycemia (blood glucose >200 mg/dL)

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

115 ed populations, comparing semaglutide versus sitagliptin for the composite outcome of myocardial infa

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

117 s >=18 years old initiating empagliflozin or sitagliptin from August 2014 through September 2016.

118 /min/1.73 m2 per year for patients receiving sitagliptin; glimepiride, -1.92 (95% CI, -2.08 to -1.75)

119 n occurred in 135 (10.6%) patients receiving sitagliptin; glimepiride, 155 (12.4%); liraglutide, 152

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

121 Two deaths occurred in the sitagliptin group during the trial.

122 glutide group versus 172 (69%) of 250 in the sitagliptin group, and nausea was the most common advers

123 study drug except for one participant in the sitagliptin group.

124 e group, and 1.2 (95% CI, 1.0 to 1.5) in the sitagliptin group.

125 the glargine, glimepiride, liraglutide, and sitagliptin groups, respectively.

126 Sixteen weeks of sitagliptin had no effect on sCD14 levels in virological

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

128 urrent drugs targeting human DPP4, including sitagliptin, had little effect on microbial DPP4.

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

130 s based on our new reaction pathway provided sitagliptin in an overall yield of 33%.

131 In this nonrandomized trial, sitagliptin in combination with tacrolimus and sirolimus

132 the comparative effectiveness of SGLT2i vs. sitagliptin in older adults with HF and type 2 diabetes

133 ynamics of dorzagliatin co-administered with sitagliptin in patients with T2D and obesity.

134 , it can inform future studies in the use of sitagliptin in the very early posttransplant period.

135 Sitagliptin increased endogenous GLP-1 and GIP values wi

136 Notably, sitagliptin increased GIP without altering weight.

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

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

139 Metformin more than sitagliptin inhibited beta-cell apoptosis.

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

141 rats and evaluated three antidiabetic drugs (Sitagliptin, Liraglutide, Saxagliptin) for Cer-modulatin

142 Sitagliptin lowered mean fasting plasma glucose by 1.1 m

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

144 Whether inhibition of DPP-4 with sitagliptin may prevent acute GVHD after allogeneic stem

145 We calculated an estimate of the absolute sitagliptin-mediated impact of GIP on beta-cell function

146 7% vs. 68.6 +/- 1.9% perfused vessels in non-sitagliptin-medicated patients, P < 0.05) and with 2.3-f

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

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

149 8, 4.79) lower HbA1c on pioglitazone than on sitagliptin (n = 356, P = 0.003).

150 omly assigned to oral semaglutide (n=253) or sitagliptin (n=251).

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

152 istration/European Medicines Agency-approved sitagliptin on preclinical models of murine HF activatio

153 n important role in mediating the effects of sitagliptin on social fear and comorbid depression.

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

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

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

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

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

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

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

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

162 iver disease (NAFLD) to receive liraglutide, sitagliptin, or insulin glargine as add-on to metformin.

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

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

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

166 nfusion minus the insulinogenic index during sitagliptin plus GIP(3-30)NH2.

167 rgine (n = 6), short-acting insulin (n = 2), sitagliptin plus metformin (n = 2), and dulaglutide (n =

168 Sitagliptin plus metformin had synergistic effects to pr

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

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

171 tage, phase 2 clinical trial to test whether sitagliptin plus tacrolimus and sirolimus would reduce t

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

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

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

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

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

177 de (rate ratio, 1.61 [95% CI, 1.13-2.29]) or sitagliptin (rate ratio 1.75; [95% CI, 1.24-2.48]).

178 Sitagliptin reduced the serum concentration of DPP-4.

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

180 Administration of the DPP4 inhibitor sitagliptin resulted in higher concentrations of the che

181 n progress, whereas treatment of wounds with sitagliptin results in reduced expression of fibrosis ma

182 er during sitagliptin and the combination of sitagliptin/sacubitril.

183 t effect, including actions mediated by GIP (sitagliptin + saline), and the physiological response mi

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

185 However, in NPY-deficient mice, sitagliptin showed reduced efficacy, suggesting that NPY

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

187 In a five weeks pilot study (n = 24), Sitagliptin (Sita) outperformed Liraglutide and Saxaglip

188 es, high quantities of the antidiabetic drug sitagliptin (STG) enter wastewater treatment plants (WWT

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

190 rial Evaluating Cardiovascular Outcomes With Sitagliptin (TECOS).

191 mmol/mol (95% CI: 1.19, 4.61) lower HbA1c on sitagliptin than on canagliflozin (n = 342, P = 0.001).

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

193 Compared with sitagliptin, the initiation of empagliflozin decreased t

194 lysis from EMPRISE showed that compared with sitagliptin, the initiation of empagliflozin was associa

195 Sitagliptin therapy for 12 months reduces DPP4 activity

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

197 sulin glargine, glimepiride, liraglutide, or sitagliptin to metformin, with the medication combinatio

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

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

200 Sitagliptin treatment also attenuated cardiac remodeling

201 Sitagliptin treatment decreases profibrotic signaling in

202 , defined as the difference between the full sitagliptin treatment effect, including actions mediated

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

204 l function as the insulinogenic index during sitagliptin treatment plus saline infusion minus the ins

205 However, sitagliptin treatment was associated with increased panc

206 Insulin secretion with sitagliptin treatment was similarly stimulated with oral

207 SEM 7.3 +/- 2.8%) but were unchanged during sitagliptin treatment.

208 than 7% with oral semaglutide than did with sitagliptin (treatment policy estimand: 58% [134 of 230]

209 nificantly better with oral semaglutide than sitagliptin (treatment policy estimand: odds ratio [OR]

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

211 dogenous GLP-1 values during liraglutide and sitagliptin treatments.

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

213 78 553 saxagliptin users and 298 124 sitagliptin users contributed an average of 7 to 9 month

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

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

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

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

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

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

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

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

222 Initiation of SGLT2i vs. sitagliptin was associated with a lower risk of the prim

223 Sitagliptin was given orally at a dose of 600 mg every 1

224 Sitagliptin was noninferior to placebo for the primary c

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

226 Participants tolerated sitagliptin well.

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

228 Absolute benefits of empagliflozin vs sitagliptin were larger in patients with a history of AS

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

230 ating treatment with either empagliflozin or sitagliptin) were included in cohort 2.

231 taining glycemic control than glimepiride or sitagliptin when added to metformin monotherapy.

232 0.15 mol % of Rh(I)/(t)Bu JOSIPHOS, affords sitagliptin, which is finally isolated as its phosphate

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

234 it more from empagliflozin vs liraglutide or sitagliptin with respect to the risk of HHF; with respec

235 or a DPP-4 inhibitor (valine pyrrolidide or sitagliptin) with or without an NEP-inhibitor (sacubitri

236 ) and the modified MACE outcome (relative to sitagliptin), with larger absolute benefits in patients

237 for the synthesis of the antidiabetic drug, sitagliptin, with a single carbon isotope label.

238 ts with HF and type 2 diabetes compared with sitagliptin, with no evidence of heterogeneity across th