Januvia (sitagliptin) / Merck (MSD) 
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  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Environmental techno-economic assessment of biocatalytic chiral amines’ production processes (W186a (McCormick Place Convention Center)) -  Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_8148;    
    The chiral amine products under study are (R)- or (S)-α-methyl benzylamine (MBA) and sitagliptin...For MBA production of Case 1, the synthesis of the chiral amines in the reactor and purification in the substrate ketone extractor and the product extractor have the biggest attributions in the 18 environmental categories. Due to the big amount of 8-fold excess of amine donor IPA, amine donor for chiral amines synthesis has dominant impacts for most categories as well.Process flow diagram and manufacturing cost as a function of membrane flux and selectivities
  • ||||||||||  Enrollment change:  Cognitive Protective Effect of Newer Antidiabetic Drugs (clinicaltrials.gov) -  Jul 26, 2022   
    P=N/A,  N=100, Recruiting, 
    Sitagliptin prevents the diabetes-induced imbalance between ROS production and antioxidant defenses that occurs in diabetic retinas. N=600 --> 100
  • ||||||||||  piceatannol / New York Medical College, Kyushu University
    Preclinical, Journal:  Antidiabetic, Antiglycation, and Antioxidant Activities of Ethanolic Seed Extract of Passiflora edulis and Piceatannol In Vitro. (Pubmed Central) -  Jul 17, 2022   
    The IC of PESE, PIC, and sitagliptin (STG) for dipeptidyl-peptidase-4 (DPP-4) was 71.1 ± 2.6, 1137 ± 120, and 0.005 ± 0.001 µg/mL, respectively...PESE and PIC were found to be capable of protecting cultured human cells from the oxidative stress caused by the carcinogen NNKOAc at 100 µM. The in vitro evidence of the inhibition of alpha-amylase, alpha-glucosidase, and DPP-4 enzymes as well as antioxidant and antiglycation activities, warrants further investigation of the antidiabetic potential of P. edulis seeds and PIC.
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Journal:  Biochemical Investigation of Therapeutic Potentials of Plant-Based Bioactive Compounds as Stimulators of Glucagon like peptide-1 Secretion. (Pubmed Central) -  Jul 15, 2022   
    This study was aimed to investigate the therapeutic potentials of plant-based bioactive compounds; lutein and resveratrol alone and/or in combination with DPP-4 enzyme inhibitor; sitagliptin on the secretion and bioavailability of Glucagon like peptide-1(GLP)...Further, co-administration of LUT and RES with DPP-4i revealed beneficial effects on measures of insulin resistance, circulating lipids, glycemic index, oxidative stress, and inflammatory status along with restoration of histological morphology of pancreatic cells and enterocytes that seemed to improve the level of GLP-1. Hence, substantial verdicts of this study showing therapeutic potentials of LUT and RES would surely help to recognize the potential effects in combination with DPP-4i as stimulators of GLP-1 secretion.
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Journal:  A Clinical Decision Support System for Diabetes Patients with Deep Learning: Experience of a Taiwan Medical Center. (Pubmed Central) -  Jul 13, 2022   
    Discussion & This study found that Bi-LSTM models is a well kernel in a CDSS which help physicians' decision-making, and the increasing the number of seasons will negative impact the performance. In addition, this study found that the most important drug is metformin, which is recommended as first-line treatment OHA in various situations for DM patients.
  • ||||||||||  Rybelsus (semaglutide oral) / Novo Nordisk
    Multifactorial risk reduction with oral semaglutide vs comparators in the treatment of type 2 diabetes (Short Oral Discussion Area) -  Jul 9, 2022 - Abstract #EASD2022EASD_1004;    
    P3
    Multifactorial risk factor management is fundamental to long-term risk reduction in patients with T2D. Oral semaglutide was more effective at improving multiple cardiometabolic risk factors vs comparators, indicating its potential to help address the full cardiometabolic profile for patients with T2D.
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    GABA and sitagliptin prevent impairment of beta cell function caused by high-fat diet (Short Oral Discussion Area) -  Jul 9, 2022 - Abstract #EASD2022EASD_874;    
    Increased activation of unfolded protein response (UPR) could be an important mechanism of compensatory beta-cell proliferation, and beta cells treated with GABA and sitagliptin showed greater UPR activation. Our results suggest that the combined use of these agents produces superior therapeutic outcomes.
  • ||||||||||  Rybelsus (semaglutide oral) / Novo Nordisk
    Greater time spent in glycaemic control with oral semaglutide vs oral comparators (Short Oral Discussion Area) -  Jul 9, 2022 - Abstract #EASD2022EASD_774;    
    P3
    In PIONEER trials of ≥52 weeks, oral semaglutide resulted in greater time spent at glycaemic target and a greater likelihood of maintaining glycaemic control vs oral comparators. Patients receiving oral semaglutide spent a similar time in glycaemic control vs liraglutide, despite a longer dose-escalation with oral semaglutide.
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Review, Journal:  Potential Effect of DPP-4 Inhibitors Towards Hepatic Diseases and Associated Glucose Intolerance. (Pubmed Central) -  Jun 24, 2022   
    Thus, we have discussed the various effects of DPP-4 on the liver diseases like hepatitis C, non-alcoholic fatty liver, hepatic regeneration and stem cell, hepatocellular carcinoma, and the impact of elevated DPP-4 levels in association with liver diseases as a cause of glucose intolerance and their treatment drug of choices. In addition, the effect of DPP-4 inhibitors on obesity and their negative aspects are also discussed in brief.
  • ||||||||||  Trial completion, Trial completion date, Bariatric surgery:  Roux-en-Y Gastric Bypass for BMI 27-32 Type 2 Diabetes Versus Best Medical Treatment (clinicaltrials.gov) -  Jun 23, 2022   
    P4,  N=40, Completed, 
    The online version contains supplementary material available at 10.1007/s42535-022-00404-4. Unknown status --> Completed | Trial completion date: Dec 2020 --> Jun 2022
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Preclinical, Journal:  Efficacy of Sitagliptin on Nonalcoholic Fatty Liver Disease in High-fat-diet-fed Diabetic Mice. (Pubmed Central) -  Jun 22, 2022   
    Our experiment proved that Sig can improve NAFLD, including improvement of the serum transaminase level, hepatic pathological inflammation level, and hepatocyte adiposis, suggesting that Sig may play a role by improving glucose and lipid metabolism, reducing the body weight and liver weight, improving insulin sensitivity, and inhibiting fatty liver inflammation. Sig may be a new direction for the treatment of patients with a nonalcoholic fatty liver and diabetes, delaying the progression of NAFLD.
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Clinical, Journal:  Validation of the WATCH-DM and TRS-HF Risk Scores to Predict the Risk of Incident Hospitalization for Heart Failure Among Adults With Type 2 Diabetes: A Multicohort Analysis. (Pubmed Central) -  Jun 22, 2022   
    Methods and Results Incident HF risk was estimated by the integer-based WATCH-DM and TRS-HF scores in participants with type 2 diabetes free of baseline HF from 2 randomized clinical trials (TECOS [Trial Evaluating Cardiovascular Outcomes With Sitagliptin], N=12 028; and Look AHEAD [Look Action for Health in Diabetes] trial, N=4867)...TRS-HF score could not be validated in the electronic health record because of unavailability of data on urine albumin/creatinine ratio in most patients in the contemporary clinical practice. Conclusions The WATCH-DM and TRS-HF risk scores can discriminate risk of HF among intermediate-risk populations with type 2 diabetes.
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Journal:  Genome-Wide Transcriptome Analysis in Type 2 Diabetes Patients Treated by Sitagliptin. (Pubmed Central) -  Jun 22, 2022   
    The validation results of RT-PCR showed that, in the significantly effective group (M), the expression of IGF1R was significantly increased (P = 0.034), the expression of MAPK3 was significantly reduced (P = 0.002), and the expression of SOCS3 was also significantly reduced (P < 0.001). There was a significant difference in gene level between patients with significant hypoglycemic effect and patients with poor hypoglycemic effect, and the expression of IGF1R increased and the expression of MAPK3 and SOCS3 decreased.
  • ||||||||||  dapagliflozin/sitagliptin / AstraZeneca, Farxiga (dapagliflozin) / Ono Pharma, AstraZeneca
    Trial completion, Enrollment change:  Phase 1 Bioequivalence Study of Dapagliflozin/Sitagliptin FDC vs Loose Combination of Single Components (clinicaltrials.gov) -  Jun 22, 2022   
    P1,  N=46, Completed, 
    There was a significant difference in gene level between patients with significant hypoglycemic effect and patients with poor hypoglycemic effect, and the expression of IGF1R increased and the expression of MAPK3 and SOCS3 decreased. Active, not recruiting --> Completed | N=27 --> 46
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Effect of dipeptidyl peptidase-4 inhibitor on emphysema model in mice (TP-8 in thematic poster area) -  Jun 22, 2022 - Abstract #ERS2022ERS_2430;    
    Conclusions : Our data indicated that Sitagliptin effectively attenuated CSE-induced emphysema. These results provide evidence for the therapeutic potential of Sitagliptin to treat or prevent emphysematous change of lung.
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Trial initiation date:  SITA-one: Effects of Sitagliptin in Relatives of T1D Patients (clinicaltrials.gov) -  Jun 21, 2022   
    P2/3,  N=70, Not yet recruiting, 
    These results provide evidence for the therapeutic potential of Sitagliptin to treat or prevent emphysematous change of lung. Initiation date: Mar 2022 --> Dec 2022
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Journal:  Synthesis of β-Amino Carbonyl 6-(Aminomethyl)- and 6-(Hydroxymethyl)pyrazolopyrimidines for DPP-4 Inhibition Study. (Pubmed Central) -  Jun 18, 2022   
    Those compounds with a methyl group or hydrogen in N-1 position and methyl substituted group in C-3 of pyrazolopyrimidine moiety showed better potent DPP-4 inhibition (IC50 = 21.4-59.8 nM). Furthermore, they had satisfactory selectivity over DPP-8 and DPP-9 Finally, the docking results revealed that compound 9n was stabilized at DPP-4 active site and would be a potential lead drug.
  • ||||||||||  Nesina (alogliptin) / Takeda
    Journal, Adverse events:  Alogliptin Induced Stomatitis: An Adverse Drug Event Case Report. (Pubmed Central) -  Jun 18, 2022   
    A causality assessment determined alogliptin was a "probable" cause of stomatitis experienced by this patient. This adverse effect has not been reported with alogliptin to the authors' knowledge.
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Trial initiation date:  Semaglutide vs Sitagliptin (clinicaltrials.gov) -  Jun 16, 2022   
    P4,  N=140, Not yet recruiting, 
    This adverse effect has not been reported with alogliptin to the authors' knowledge. Initiation date: Apr 2022 --> Aug 2022
  • ||||||||||  Januvia (sitagliptin) / Merck (MSD)
    Journal:  Complete resonance assignment of a pharmaceutical drug at natural isotopic abundance from DNP-Enhanced solid-state NMR. (Pubmed Central) -  Jun 15, 2022   
    Using inputs from DFT calculations, herein we describe a significant improvement to the structure elucidation process for complex organic molecules. Further, we demonstrate that a series of two-dimensional correlation experiments, including N-C TEDOR, C-C INADEQUATE/SARCOSY, F-C HETCOR, and H-C HETCOR, can be obtained at natural isotopic abundance within reasonable experiment times, thus enabling a complete resonance assignment of sitagliptin, a pharmaceutical used for the treatment of type 2 diabetes.
  • ||||||||||  Nesina (alogliptin) / Takeda, Onglyza (saxagliptin) / AstraZeneca, Januvia (sitagliptin) / Merck (MSD)
    Preclinical, Journal:  Prolonged effects of DPP-4 inhibitors on steato-hepatitic changes in Sprague-Dawley rats fed a high-cholesterol diet. (Pubmed Central) -  Jun 9, 2022   
    The potential lipid lowering effects of DPP-4 inhibitors were diminished by high Cho (a significant risk factor for inducing liver damage). The robust inflammatory responses induced by high Cho feeding in long-term experiment were not exacerbated by DPP-4 inhibitors and a consistent hepatic inflammatory environment persisted, implying a prospective physiological adaptation.