- |||||||||| Zafatek (trelagliptin) / Takeda, Remozen (remogliflozin etabonate) / Islet Sci
Biomarker, Preclinical, Journal, Combination therapy: Impacts of trelagliptin and remogliflozin alone and in combination with Alpha Lipoic Acid on cardiac function in streptozotocin-induced diabetes mellitus (Pubmed Central) - Nov 1, 2023 The combination of trelagliptin, remogliflozin, and ALA may have additional clinical value in managing DCM by targeting oxidative stress, inflammation, and glucotoxicity. However, further research is needed to validate these findings and explore their potential clinical applications.
- |||||||||| 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.
- |||||||||| 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.
- |||||||||| 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
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.
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