Zafatek (trelagliptin) / Takeda 
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 8 Diseases   1 Trial   1 Trial   107 News 


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  • ||||||||||  Zafatek (trelagliptin) / Takeda, Januvia (sitagliptin) / Merck (MSD)
    Review, Journal, Gram positive:  Computational tools for exploring peptide-membrane interactions in gram-positive bacteria. (Pubmed Central) -  Mar 25, 2023   
    Herein, we present a comprehensive survey of diverse computational approaches that are suitable for detecting QSPs and QS interference molecules. This review highlights the utility of these methods for developing potential biomarkers against infectious Gram-positive pathogens.
  • ||||||||||  Zafatek (trelagliptin) / Takeda, MG132 / Jilin University, Dorothy M. Davis Heart and Lung Research Institute
    Journal:  ABCC8-Related Maturity-Onset Diabetes of the Young: Clinical Features and Genetic Analysis of One Case. (Pubmed Central) -  Jul 28, 2022   
    The diagnosis of maturity-onset diabetes of the young (MODY)12 was confirmed in our patient. The ABCC8 variant inhibited both ubiquitination and autophagy lysosome degradation pathways, especially the ubiquitination degradation pathway.
  • ||||||||||  Retrospective data, Review:  Effects of Anti-Diabetic Drugs on Fracture Risk: A Systematic Review and Network Meta-Analysis. (Pubmed Central) -  Feb 16, 2022   
    Specifically, trelagliptin raised the risk of fracture, whereas voglibose and albiglutide showed benefit with statistical difference...Some drugs (omarigliptin, sitagliptin, vildagliptin, saxagliptin, empagliflozin, ertugliflozin, rosiglitazone, pioglitazone, and nateglinide) may increase the risk of fracture, while others (such as dulaglutide, exenatide, liraglutide, semaglutide, lixisenatide, linagliptin, alogliptin, canagliflozin, dapagliflozin, glipizide, gliclazide, glibenclamide, glimepiride, metformin, and insulin) may show benefits...When developing individualized treatment strategies, the clinical efficacy of anti-diabetic drugs must be weighed against their benefits and risks brought about by individual differences of patients. This Systematic Review was prospectively registered on the PROSPERO (https://www.crd.york.ac.uk/PROSPERO/, registration number CRD42020189464).
  • ||||||||||  Zafatek (trelagliptin) / Takeda
    Journal:  The anti-diabetic drug trelagliptin induces vasodilation via activation of Kv channels and SERCA pumps. (Pubmed Central) -  Sep 15, 2021   
    From these results, we concluded that the vasodilatory effect of trelagliptin was associated with the activation of Kv channels (primary the Kv7.X subtype) and SERCA pump regardless of other K channels, Ca channels, cAMP/PKA-related or cGMP/PKG-related signaling pathways, and the endothelium. Therefore, caution is required when prescribing trelagliptin to the patients with hypotension and diabetes.
  • ||||||||||  Retrospective data, Journal:  Bullous pemphigoid and dipeptidyl peptidase-4 inhibitors: a meta-analysis of randomized controlled trials. (Pubmed Central) -  Jun 22, 2021   
    In conclusion, available data from randomized controlled trials seem to confirm the association between DPP-4 inhibitors and bullous pemphigoid. This association could be limited to one molecule of the class (i.e., linagliptin), although data on other DPP4-i (e.g., vildagliptin) are insufficient to rule out similar detrimental effects.
  • ||||||||||  Zafatek (trelagliptin) / Takeda
    Journal:  The dipeptidyl peptidase (DPP)-4 inhibitor trelagliptin inhibits IL-1β-induced endothelial inflammation and monocytes attachment. (Pubmed Central) -  May 26, 2021   
    Mechanistically, trelagliptin suppressed the activation of activator protein-1 (AP-1) and NF-κB signaling pathways, which modulate the inflammatory process and monocyte adhesion. Collectively, our results showed that trelagliptin had a powerful inhibitory effect on the attachment of monocytes to endothelial cells, indicating that trelagliptin might have a protective effect on cardiovascular diseases such as atherosclerosis.
  • ||||||||||  Nesina (alogliptin) / Takeda, Zafatek (trelagliptin) / Takeda, Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Journal:  Preparation of (R)-3-aminopiperidine by resolution with optically active cyclic phosphoric acids. (Pubmed Central) -  May 5, 2021   
    (R)-3-aminopiperidine ((R)-APD), a key intermediate for alogliptin, trelagliptin, and linagliptin, was successfully resolved from racemic 3-aminopiperidine with an enantiomerically pure resolving agent, namely, (R)-4-(2-chlohydroxy-1.3.2-dioxaphosphorinane 2-oxide ((R)-CPA), via diastereomeric salt formation. By this resolution approach, (R)-3-aminopiperidine was obtained in 99.5% yield with 99.6%e.e.
  • ||||||||||  Zafatek (trelagliptin) / Takeda
    Trial completion, Trial completion date, Trial primary completion date, Monotherapy:  Clinical Trial of Trelagliptin Succinate Tablets in the Treatment of Type 2 Diabetes (clinicaltrials.gov) -  Jan 12, 2021   
    P3,  N=254, Completed, 
    By this resolution approach, (R)-3-aminopiperidine was obtained in 99.5% yield with 99.6%e.e. Active, not recruiting --> Completed | Trial completion date: Jul 2021 --> Dec 2020 | Trial primary completion date: Jun 2021 --> Dec 2020
  • ||||||||||  Zafatek (trelagliptin) / Takeda
    Journal:  Trelagliptin succinate: DPP-4 inhibitor to improve insulin resistance in adipocytes. (Pubmed Central) -  Nov 28, 2020   
    In addition, the secretion of free fatty acids and resistin were decreased. In conclusion, our study suggested that trelagliptin succinate improved insulin resistance in adipocytes via regulation of PI-3K/AKT/GLUT4 insulin signaling pathway.
  • ||||||||||  Zafatek (trelagliptin) / Takeda
    Enrollment closed, Monotherapy:  Clinical Trial of Trelagliptin Succinate Tablets in the Treatment of Type 2 Diabetes (clinicaltrials.gov) -  Jun 30, 2020   
    P3,  N=254, Active, not recruiting, 
    The decision to administer a once-weekly or once-daily DPP-4i is likely to depend on patient preference, patient-physician discussions, and treatment practices of the prescribing physician. Recruiting --> Active, not recruiting
  • ||||||||||  Zafatek (trelagliptin) / Takeda
    Enrollment open, Trial completion date, Trial primary completion date, Monotherapy:  Clinical Trial of Trelagliptin Succinate Tablets in the Treatment of Type 2 Diabetes (clinicaltrials.gov) -  Apr 27, 2020   
    P3,  N=240, Recruiting, 
    Present data do not suggest any association of DPP4i with pancreatic cancer, although they are insufficient to draw definitive conclusions. Not yet recruiting --> Recruiting | Trial completion date: Feb 2020 --> Jul 2021 | Trial primary completion date: Jan 2020 --> Jun 2021
  • ||||||||||  Zafatek (trelagliptin) / Takeda, omarigliptin (MK-3102) / Merck (MSD)
    Preclinical, Journal:  Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. (Pubmed Central) -  Apr 14, 2020   
    A single dose oral administration of 5 (3 mg/kg) inhibited >80% DPP-4 activity for more than 7 days in diabetic mice. The long-term antidiabetic efficacies of 5 (10 mg/kg, q.w) were better than the once-weekly trelagliptin and omarigliptin, especially in decreasing the hemoglobin A1c (HbA1c) level.
  • ||||||||||  Nesina (alogliptin) / Takeda, Zafatek (trelagliptin) / Takeda
    PK/PD data, Journal:  An HPLC-MS/MS method for quantitation of trelagliptin and application in a comparative pharmacokinetic study. (Pubmed Central) -  Mar 26, 2020   
    Discussion/ Compared with normal groups, the T1/2, apparent volume of distribution, area under the curve and bioavailability in model rats were significantly increased while the apparent plasma clearance decreased. The approach is proved to be straightforward and appropriate for quantitation of trelagliptin and application in pharmacokinetics studies.
  • ||||||||||  Journal:  Repositioning of Omarigliptin as a once-weekly intranasal Anti-parkinsonian Agent. (Pubmed Central) -  Oct 11, 2019   
    Sitagliptin, vildagliptin, saxagliptin & linagliptin showed antioxidant and neurorestorative effects in previous studies linked to DPP-4 inhibition...LC-MS/MS determination of once-weekly anti-diabetic DPP-4 inhibitors; omarigliptin & trelagliptin in plasma and brain tissue was employed after 2 h of oral administration to rats...A novel intranasal formulation was developed using sodium lauryl sulphate surfactant to solubilize the lipophilic omarigliptin with penetration enhancing & antimicrobial properties. Intranasal administration showed enhanced brain/plasma ratio by 3.3 folds compared to the oral group accompanied with 2.6 folds increase in brain glucagon-like peptide-1 concentration compared to the control group.