linagliptin / Generic mfg. 
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  • ||||||||||  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.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Enrollment change, Trial withdrawal:  Effects of DPP4 Inhibition on COVID-19 (clinicaltrials.gov) -  Jun 10, 2021   
    P4,  N=0, Withdrawn, 
    However, its antipsychotic properties have been previously hypothesized, particularly because of its possible ability to block the D2 dopamine receptors. N=20 --> 0 | Not yet recruiting --> Withdrawn
  • ||||||||||  Farxiga (dapagliflozin) / Ono Pharma, AstraZeneca
    Review, Journal:  Renal outcomes with the newer antidiabetes drugs: the era before and after CREDENCE. (Pubmed Central) -  Jun 8, 2021   
    Since 2008, the data from various cardiovascular outcome trials have been reported, including SAVOR-TIMI 53 (saxagliptin), EXAMINE (alogliptin), TECOS (sitagliptin), CARMELINA (linagliptin), CAROLINA (linagliptin), ELIXA (lixisenatide), LEADER (liraglutide), EXSCEL (exenatide once-weekly), SUSTAIN-6 (injectable semaglutide), HARMONY Outcomes (albiglutide), REWIND (dulaglutide), PIONEER-6 (oral semaglutide), EMPA-REG OUTCOME (empagliflozin), the CANVAS Program (canagliflozin) and DECLARE-TIMI 53 (dapagliflozin)...In this review, we aim to highlight the renal outcome data from the cardiovascular outcome trials and CREDENCE trials and understand the differences between their results. The post CREDENCE era would appear to reinforce the position of sodium-glucose co-transporter-2 inhibitors as drugs providing cardiorenal protection, in addition to their anti-glycaemic effects.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Clinical, Journal:  Compliance with the DPP-4 inhibitors dose adjustment recommendations based on renal function in a population database. (Pubmed Central) -  Jun 6, 2021   
    SGLT2i was associated with a lower risk of new-onset AF compared with DPP4i among T2DM patients in real-world practice. Under real-world clinical practice conditions, more than one third of T2DM patients with advanced renal failure were overdosed with DPP4is because the doses were not adequately adjusted to the glomerular filtration rate of each patient.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Enrollment change, Trial completion date, Trial termination:  Efficacy and Safety of Dipeptidyl Peptidase-4 Inhibitors in Diabetic Patients With Established COVID-19 (clinicaltrials.gov) -  Jun 2, 2021   
    P3,  N=64, Terminated, 
    Under real-world clinical practice conditions, more than one third of T2DM patients with advanced renal failure were overdosed with DPP4is because the doses were not adequately adjusted to the glomerular filtration rate of each patient. N=100 --> 64 | Trial completion date: Sep 2021 --> May 2021 | Recruiting --> Terminated; End of COVID-19 outbreak in Israel
  • ||||||||||  Journal:  Action of dipeptidyl peptidase-4 inhibitors on SARS-CoV-2 main protease. (Pubmed Central) -  May 20, 2021   
    We used an enzymatic assay measuring inhibition of M pro catalytic activity in the presence of four different commercially available gliptins (linagliptin, sitagliptin, alogliptin and saxagliptin) and several structural analogues of linagliptin to study binding of DPP-4 inhibitors to M pro and their functional activity. We show here that DPP-4 inhibitors like linagliptin, other gliptins and structural analogues are inactive against M pro .
  • ||||||||||  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.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Enrollment open, Trial completion date, Trial primary completion date, Monotherapy:  Effects of Sequential Treatment Based on Lina/MET After Short-term Intensive Insulin in Newly Diagnosed Type 2 Diabetes (clinicaltrials.gov) -  Apr 29, 2021   
    P4,  N=448, Recruiting, 
    This method showed a good sensitivity with a detection limit (DL) and quantitation limit (QL) of 7.5 and 25.0 ppm, respectively. Not yet recruiting --> Recruiting | Trial completion date: Dec 2020 --> Dec 2022 | Trial primary completion date: Jul 2020 --> Dec 2022
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Preclinical, Journal:  Neuroprotective effects of linagliptin on ischemia/reperfusion in mice (Pubmed Central) -  Apr 28, 2021   
    Compared with the I/R group, the neurological deficit score and infarct volume were significantly decreased in the linagliptin pretreatment group after 24 h reperfusion (P＜0.05); the MDA content in the brain was significantly decreased (P＜0.05), while the GSH, PI3K, p-Akt and mTOR levels were significantly increased (P＜0.05). This study proves that linagliptin exerted a neuroprotective effect in I/R mice, which may be mediated by activation of the PI3K/AKT/mTOR pathway.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Preclinical, Journal:  Linagliptin Ameliorates Hepatic Steatosis via Non-Canonical Mechanisms in Mice Treated with a Dual Inhibitor of Insulin Receptor and IGF-1 Receptor. (Pubmed Central) -  Apr 22, 2021   
    Hepatic quantitative proteomic and phosphoproteomic analyses revealed that perilipin-2 (PLIN2), major urinary protein 20 (MUP20), cytochrome P450 2b10 (CYP2B10), and nicotinamide N-methyltransferase (NNMT) are possibly involved in the process of the amelioration of hepatic steatosis by linagliptin. Thus, linagliptin improved hepatic steatosis induced by IR and IGF1R inhibition via a previously unknown mechanism that did not involve gluconeogenesis, lipogenesis, or inflammation, suggesting the non-canonical actions of DPP-4 inhibitors in the treatment of hepatic steatosis under insulin-resistant conditions.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Journal, Adverse events:  Modern sulphonylureas and cardiovascular adverse effects: Will CAROLINA put an end to the controversy? (Pubmed Central) -  Apr 1, 2021   
    CAROLINA (CARdiovascular Outcome study of LINAgliptin versus glimepiride in patients with type 2 diabetes) trial planned as a cardiovascular outcome trial randomised people with type 2 diabetes and high cardiovascular risk to Linagliptin and Glimepiride. This opinion paper outlines the salient features of this landmark trial and its implications in general cardiology practice.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly
    Trial completion, Enrollment change, Trial completion date, Trial primary completion date:  Covid19DPP4i: Dipeptidyl Peptidase-4 Inhibitor (DPP4i) for the Control of Hyperglycemia in Patients With COVID-19 (clinicaltrials.gov) -  Mar 22, 2021   
    P3,  N=70, Completed, 
    This work highlights GPR35 and AHR as the guardian of kynurenine pathway metabolism and core component of defense responses against intestinal damage. Recruiting --> Completed | N=28 --> 70 | Trial completion date: Sep 2020 --> Feb 2021 | Trial primary completion date: Sep 2020 --> Feb 2021