 |
12 Diseases |  |
1 Trial |
|
1 Trial |  |
156 News |  |
| 123» |
- | linagliptin / Generic mfg., Marizev (omarigliptin) / Merck (MSD)
Journal: Glucagon-like peptide-1 receptor agonists but not dipeptidyl peptidase-4 inhibitors reduce alcohol intake. (Pubmed Central) - Mar 6, 2025
Convergent findings across humans, mice, and rats indicate that GLP-1RAs but not DPP-4Is reduce alcohol consumption and may be efficacious in treating AUD.
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal: Omarigliptin/rosinidin combination ameliorates cyclophosphamide-induced lung toxicity in rats: The interaction between glucagon-like peptide-1, TXNIP/NLRP3 inflammasome signaling, and PI3K/Akt/FoxO1 axis. (Pubmed Central) - Jul 28, 2024
Both omarigliptin and rosinidin exhibited a synergistic ability to augment the tissue antioxidant defenses, mitigate the inflammatory pathways, restore glucagon-like peptide-1 levels, modulate high mobility group box 1 (HMGB1)/receptors of advanced glycation end products (RAGE)/nuclear factor kappa B (NF-?B) axis, downregulate the fibrogenic mediators, and create a balance between the pathways involved in apoptosis and the autophagy signals in the pulmonary tissues. In conclusion, omarigliptin/rosinidin combination may be introduced as a novel therapeutic modality that attenuates the different forms of lung toxicities induced by cyclophosphamide.
- | Marizev (omarigliptin) / Merck (MSD)
Trial initiation date, HEOR, Real-world evidence: Real-World Evaluation of Omarigliptin for Type 2 Diabetes Meliitus in Bangladesh (clinicaltrials.gov) - Jul 17, 2024
P4, N=938, Not yet recruiting, Sponsor: Bangladesh Institute of Research and Rehabilitation in Diabetes, Endocrine and Metabolic Disorders
In conclusion, omarigliptin/rosinidin combination may be introduced as a novel therapeutic modality that attenuates the different forms of lung toxicities induced by cyclophosphamide. Initiation date: Jun 2024 --> Sep 2024
- | Marizev (omarigliptin) / Merck (MSD)
New P4 trial, HEOR, Real-world evidence: Real-World Evaluation of Omarigliptin for Type 2 Diabetes Meliitus in Bangladesh (clinicaltrials.gov) - Jun 6, 2024
P4, N=938, Not yet recruiting, Sponsor: Bangladesh Institute of Research and Rehabilitation in Diabetes, Endocrine and Metabolic Disorders
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal: Analysis of omarigliptin forced degradation products by ultra-fast liquid chromatography, mass spectrometry, and in vitro toxicity assay. (Pubmed Central) - May 30, 2024
Based on the results from forced degradation studies, OMG was found to be labile to hydrolysis, oxidation, photolytic, and thermal stress conditions. The results of this study contribute to the quality control and stability profile of OMG.
- || Marizev (omarigliptin) / Merck (MSD)
Retrospective data, Review, Journal: Efficacy and Safety of Omarigliptin, a Novel Once-Weekly Dipeptidyl Peptidase-4 Inhibitor, in Type 2 Diabetes Mellitus: A Systematic Review and Meta-Analysis. (Pubmed Central) - Jan 23, 2024
Although the omarigliptin group experienced a higher incidence of hypoglycemic events compared to the PCG, the overall AEs, serious AEs, hypoglycemia, and severe hypoglycemia were comparable between the omarigliptin and control groups (PCG and ACG). Omarigliptin has a favorable glycemic efficacy and safety profile for managing T2DM.
- | Marizev (omarigliptin) / Merck (MSD)
Journal: Omarigliptin inhibits brain cell ferroptosis after intracerebral hemorrhage. (Pubmed Central) - Sep 7, 2023
In addition, the elevation of iron content, lipid peroxidation and FACL4 after ICH; and reduction of GPX4 and AIFM2; were mitigated by MK3102 in vitro and in vivo. The neuroprotective effect of MK3102 may be related to anti-ferroptosis by regulating GLP-1R after ICH injury.
- || Januvia (sitagliptin) / Merck (MSD), Marizev (omarigliptin) / Merck (MSD)
Review, Journal: Insight into Structure Activity Relationship of DPP-4 Inhibitors for Development of Antidiabetic Agents. (Pubmed Central) - Aug 16, 2023
Additionally, various synthesis schemes were developed to make several commercially available DPP4 inhibitors such as vildagliptin, sitagliptin and omarigliptin. In conclusion, the use of halogenated scaffolds for the development of DPP-4 inhibitors is likely to be an area of increasing interest in the future.
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal: Omarigliptin Protects the Integrity of the Blood-Brain Barrier After Intracerebral Hemorrhage in Mice. (Pubmed Central) - Jun 21, 2023
Importantly, MK3102 protected the integrity of the BBB after ICH, associated with decreased expression of MMP-9, and preservation of the tight junction proteins ZO-1 and Occludin on endothelial cells through putative degradation of MMP-9, and inhibition of the expression of CX43 on astrocytes. Omarigliptin protects the integrity of the BBB in mice after ICH injury.
- ||| Journal, Adverse events: Comparison of Adverse Events Occurred During Administration of Dipeptidyl Peptidase-4 Inhibitor in Patients with Diabetes Using FDA Adverse Event Reporting System. (Pubmed Central) - Jan 14, 2023
Although it is impossible to select a DPP-4 inhibitor with aROR of < 1.000 of all occurrences of adverse events, these results may be used for drug selection when the patient has adverse events that need to be avoided. We provided the sample code of software R that can reproduce the results.
- | Marizev (omarigliptin) / Merck (MSD)
Journal: Omarigliptin Mitigates 6-Hydroxydopamine- or Rotenone-Induced Oxidative Toxicity in PC12 Cells by Antioxidant, Anti-Inflammatory, and Anti-Apoptotic Actions. (Pubmed Central) - Oct 28, 2022
Collectively, these results demonstrate that OMG alleviates the neurotoxin-induced oxidative toxicity through Nrf2/HO-1-mediated antioxidant, NF-κB-mediated anti-inflammatory, and anti-apoptotic mechanisms in PC12 cells. Our findings elucidating multiple mechanisms of antiparkinsonian activity strongly support the therapeutic potential of OMG in the treatment of PD.
- || Zafatek (trelagliptin) / Takeda, Marizev (omarigliptin) / Merck (MSD)
PK/PD data, Journal: Prediction of pharmacokinetics and pharmacodynamics of trelagliptin and omarigliptin in healthy humans and in patients with renal impairment using physiologically based pharmacokinetic combined DPP-4 occupancy modeling. (Pubmed Central) - Sep 18, 2022
Our findings elucidating multiple mechanisms of antiparkinsonian activity strongly support the therapeutic potential of OMG in the treatment of PD. The present PBPK-DO model can simultaneously predict PK and PD of TRE and OMA in humans and also provide valuable recommendations for dosing adjustment in renal impairment patients, which cannot be achieved by alone depending on PK change.
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal: Antidiabetic Omarigliptin Dilates Rabbit Aorta by Activating Kv Channels and the SERCA Pump. (Pubmed Central) - Sep 14, 2022
Pretreatment with the sarco/endoplasmic reticulum Ca -ATPase (SERCA) pump inhibitors thapsigargin and cyclopiazonic acid significantly reduced the vasodilatory effect of omarigliptin...Furthermore, pretreatment with the nitric oxide synthase inhibitor L-NAME or small-conductance Ca -activated K channel inhibitor apamin, together with the intermediate-conductance Ca -activated K channel inhibitor TRAM-34, did not influence the vasodilatory effect of omarigliptin. In conclusion, omarigliptin induced vasodilation in rabbit aortic smooth muscle by activating voltage-dependent K channels and the SERCA pump independently of other K channels, cAMP/PKA- and cGMP/PKG-related signaling pathways, and the endothelium.
- glimepiride / Generic mfg.
Cardiovascular Safety of Glimepiride: An Indirect Treatment Comparison of Cardiovascular Safety Outcome Trials of DPP4 Inhibitors (Virtual) - Sep 1, 2022 - Abstract #ISPOREU2022ISPOR_EU_1999;
Glimepiride has a noninferior risk of 3-Point MACE, all-cause death, and CV death compared to placebo, saxagliptin, sitagliptin, linagliptin, and omarigliptin in T2D patients with increased CV risk. Glimepiride may be used in this population to attain glycemic control, particularly in settings where cost of DPP4Is is a concern.
- | Januvia (sitagliptin) / Merck (MSD), Marizev (omarigliptin) / Merck (MSD)
Journal: Anti-Quorum Sensing Activities of Gliptins against Pseudomonas aeruginosa and Staphylococcus aureus. (Pubmed Central) - May 30, 2022
To test the anti-QS activities of gliptins, a detailed molecular docking study was conducted to evaluate the gliptins' binding affinities to P. aeruginosa and S. aureus QS receptors, which helped explain the anti-QS activities of gliptins, particularly sitagliptin and omarigliptin. In conclusion, this study evaluates the possible antivirulence and anti-QS activities of gliptins that could be promising novel candidates for the treatment of aggressive Gram-negative or -positive bacterial infections either alone or as adjuvants to other antibiotics.
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal: Omarigliptin attenuates rotenone-induced Parkinson's disease in rats: Possible role of oxidative stress, endoplasmic reticulum stress and immune modulation. (Pubmed Central) - May 26, 2022
Moreover, OG ameliorated endoplasmic reticulum (ER) stress in rotenone-administered rats; as evidenced by reduced levels of ER resident proteins such as glucose-regulated protein 78, C/EBP homologous protein and apoptotic caspase-12. In conclusion, this study implies repurposing of OG, as a novel neuroprotective agent due to its antioxidant properties, its effects on ER stress in addition to its anti-inflammatory and anti-apoptotic activities.
- | Marizev (omarigliptin) / Merck (MSD)
Journal: Design, synthesis and evaluation of a series of novel long-acting dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes. (Pubmed Central) - May 3, 2022
The inhibitory activity ranged from 0.43 to 12.70 μM while the inhibitory activity of positive control (omarigliptin) was 3.63 μM on DPP-4 in Caco-2 cells...In conclusion, compound 6c was considered as a promising DPP-4 inhibitor, which could be taken once a week or once every two weeks for the treatment of T2DM. More comprehensive researches will be carried out in the future for the further development of compound 6c.
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal: Omarigliptin alleviates cognitive dysfunction in Streptozotocin-induced diabetic mouse. (Pubmed Central) - Apr 14, 2022
Mechanistically, SIRT3 expression is required for the effect of Omarigliptin. This study provided preclinical evidence that Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction.
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal, IO biomarker: Omarigliptin/galangin combination mitigates lipopolysaccharide-induced neuroinflammation in rats: Involvement of glucagon-like peptide-1, toll-like receptor-4, apoptosis and Akt/GSK-3β signaling. (Pubmed Central) - Mar 12, 2022
This study provided preclinical evidence that Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction. Omarigliptin/galangin combination might be proposed as a promising therapeutic line for mitigation of the pathophysiologic events of LPS-induced neuroinflammation.
- | Marizev (omarigliptin) / Merck (MSD)
Journal: Univariate versus multivariate spectrophotometric methods for the simultaneous determination of omarigliptin and two of its degradation products. (Pubmed Central) - Feb 24, 2022
Their linearity ranges were 20.0-60.0 μg mL for OMR and 10.0-30.0 μg mL for the two degradation products. All the methods were validated, effectively applied for quantification of the intact drug in its tablet formulation and favorably compared to the reported one.
- | Marizev (omarigliptin) / Merck (MSD)
Journal: The protective effects of Omarigliptin against Lipopolysaccharide (LPS)- induced inflammatory response and expression of mucin 5AC (MUC5AC) in human bronchial epithelial cells. (Pubmed Central) - Feb 22, 2022
Importantly, we found that this process is mediated by the Adenosine 5'-monophosphate (AMP)-activated protein kinase (AMPK) signaling pathway. Based on these findings, we conclude that Omarigliptin might be a promising agent for the treatment of chronic inflammatory lung diseases.
- || 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).
- | Marizev (omarigliptin) / Merck (MSD)
Journal: The effects of Omarigliptin on promoting osteoblastic differentiation. (Pubmed Central) - Feb 16, 2022
Lastly, Omarigliptin-induced osteoblastic differentiation, promoted ALP activity, and increased expression levels of Sp7, Fgfr2, Fgfr3, BMP-2, Ocn, ALP, Col1a1, and Col1a2, in the osteogenic medium- cultured MC3T3‑E1 cells were dramatically abolished by the knockdown of Runx2. Taken together, our data reveal that Omarigliptin promoted osteoblastic differentiation by regulating Runx2.
- | Marizev (omarigliptin) / Merck (MSD)
Journal: Omarigliptin protects against nonalcoholic fatty liver disease by ameliorating oxidative stress and inflammation. (Pubmed Central) - Feb 15, 2022
Also, the activated NF-κB signaling pathway, as well as suppressed SIRT1 expression level, were significantly reversed by omarigliptin. Omarigliptin protected against NAFLD by ameliorating oxidative stress and inflammation.
- || Marizev (omarigliptin) / Merck (MSD)
Clinical, Journal: Efficacy of omarigliptin, once-weekly dipeptidyl peptidase-4 inhibitor, in patients with type 2 diabetes. (Pubmed Central) - Jan 21, 2022
Omarigliptin protected against NAFLD by ameliorating oxidative stress and inflammation. Administering omarigliptin as add-on therapy or switching to it from sitagliptin and linagliptin, but not vildagliptin, improves glycemic control and thus should help in decision making when selecting DPP-4is for T2D patients.
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal: Omarigliptin Prevents TNF-α-Induced Cellular Senescence in Rat Aorta Vascular Smooth Muscle Cells. (Pubmed Central) - Jan 4, 2022
Importantly, our experiments revealed that blockage of silent information-regulator 1 (SIRT1) abolished the inhibitory effects of OMG on p53 acetylation, SA-β-gal activity, and telomerase activity in VSMCs. These results suggest that OMG may have the potential to delay or prevent the progression of age-related cardiovascular diseases by modulating the activity of SIRT1.
- | Marizev (omarigliptin) / Merck (MSD)
Journal: Omarigliptin ameliorated high glucose-induced nucleotide oligomerization domain-like receptor protein 3 (NLRP3) inflammasome activation through activating adenosine monophosphate-activated protein kinase α (AMPKα) in renal glomerular endothelial cells. (Pubmed Central) - Dec 16, 2021
After the co-administration of the adenosine monophosphate-activated protein kinase α (AMPKα) inhibitor, compound C, the protective effects of Omarigliptin against HG-induced NLRP3 inflammasome activation and production of pro-inflammatory factors were dramatically abolished. Taken together, our data revealed that Omarigliptin ameliorated HG-induced inflammation in renal glomerular endothelial cells through suppressing NLRP3 inflammasome activation mediated by AMPKα.
- || Marizev (omarigliptin) / Merck (MSD)
Clinical, Journal: Effects of omarigliptin on glucose variability and oxidative stress in type 2 diabetes patients: A prospective study. (Pubmed Central) - Nov 29, 2021
Taken together, our data revealed that Omarigliptin ameliorated HG-induced inflammation in renal glomerular endothelial cells through suppressing NLRP3 inflammasome activation mediated by AMPKα. Our findings suggest that switching from once-daily DPP-4 inhibitors to omarigliptin may be efficacious for maintaining FPG and TIR in T2DM patients.
- | Marizev (omarigliptin) / Merck (MSD)
Journal: Quality and Stability Profile Assessment of the Recent Antidiabetic Omarigliptin by Using Different Chromatographic Methods. (Pubmed Central) - Oct 30, 2021
Several factors affecting TLC and HPLC efficiency have been carefully studied. The developed methods were validated according to International Conference on Harmonization guidelines and successfully applied for assessment of OMR in bulk powder and tablets.
- | Retrospective data, Review, Journal: Cardiovascular events and all-cause mortality in patients with type 2 diabetes treated with dipeptidyl peptidase-4 inhibitors: An extensive meta-analysis of randomized controlled trials. (Pubmed Central) - Sep 29, 2021
As a class, DPP4i are not associated with any increase or reduction of MACE, all-cause mortality, and heart failure. Saxagliptin seems to be associated with an increased risk of hospitalization for heart failure.
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal: Intranasal Neuropeptide Y as a Potential Therapeutic for Depressive Behavior in the Rodent Single Prolonged Stress Model in Females. (Pubmed Central) - Sep 28, 2021
The omarigliptin and 600 μg NPY combined treatment, but neither alone, was also sufficient at preventing depressive-like behavior on the FST. The results demonstrate that: (1) SPS elicits several behavioral manifestations of PTSD in females; (2) early intervention with a high dose of intranasal NPY has therapeutic potential also for females; and (3) NPY cleavage by DPP4 may play a role in the higher dose requirement for females.
- || Marizev (omarigliptin) / Merck (MSD)
Clinical, Journal: A Randomized, Placebo-controlled Study to Evaluate the Efficacy and Safety of Adding Omarigliptin to Insulin Therapy in Japanese Patients with Type 2 Diabetes and Inadequate Glycemic Control. (Pubmed Central) - Jul 11, 2021
P4
The addition of once-weekly omarigliptin to insulin therapy for up to 52 weeks was generally well tolerated and provided clinically meaningful improvement in glycemic control throughout the trial period. (ClinicalTrials.gov: NCT02906709).
- || Marizev (omarigliptin) / Merck (MSD)
PK/PD data, Preclinical, Journal: Simultaneous Quantification of Pioglitazone and Omarigliptin in Rat Plasma by UHPLC-MS/MS and Its Application to Pharmacokinetic Study after Coadministration of the Two Drugs. (Pubmed Central) - Jul 3, 2021
The validated method was then successfully applied to pharmacokinetic study of pioglitazone combined with omarigliptin in rats. Results suggested that the combination of the two drugs had little effect on the pharmacokinetic parameters of each other in rats.
- | 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.
- | Marizev (omarigliptin) / Merck (MSD)
Journal, IO biomarker: Omarigliptin Mitigates Lipopolysaccharide-Induced Neuroinflammation and Dysfunction of the Integrity of the Blood-Brain Barrier. (Pubmed Central) - Jun 22, 2021
Mechanistically, Omarigliptin inhibited the activation of the toll-like receptor 4 (TLR4)/myeloid differentiation factor 88/nuclear factor κB (TLR4/Myd88/NF-κB) signaling pathway. On the basis of these findings, we concluded that Omarigliptin might mitigate LPS-induced neuroinflammation and dysfunction of the integrity of the blood-brain barrier.
- | Marizev (omarigliptin) / Merck (MSD)
Preclinical, Journal: Repurposing of Omarigliptin as a Neuroprotective Agent Based on Docking with A Adenosine and AChE Receptors, Brain GLP-1 Response and Its Brain/Plasma Concentration Ratio after 28 Days Multiple Doses in Rats Using LC-MS/MS. (Pubmed Central) - May 11, 2021
Results showed that OMR passed through the BBB more effectively in the multiple dose study as compared to the previously published single dose study by the authors. Thus, the present study suggests potential repositioning of OMR as antiparkinsonian agent that will be of interest for researchers interested in neurodegenerative diseases.
- || Marizev (omarigliptin) / Merck (MSD)
Clinical, Journal: Enhanced Extraction Technique of Omarigliptin from Human Plasma-Applied to Biological Samples from Healthy Human Volunteers. (Pubmed Central) - Mar 12, 2021
Validation results were all satisfactory including successful stability studies with bias below 12%. The proposed study will be valuable for ethnicity comparison studies that will be commenced on omarigliptin in Egypt by the authors in prospective study, following the FDA recommends, to evaluate possible sub-group dissimilarities that include pharmacokinetic parameters.
- || Marizev (omarigliptin) / Merck (MSD)
Clinical, Journal: Beneficial effect of omarigliptin on diabetic patients with non-alcoholic fatty liver disease/non-alcoholic steatohepatitis. (Pubmed Central) - Mar 12, 2021
The proposed study will be valuable for ethnicity comparison studies that will be commenced on omarigliptin in Egypt by the authors in prospective study, following the FDA recommends, to evaluate possible sub-group dissimilarities that include pharmacokinetic parameters. Weekly administration of the DPP4 inhibitor OMG in ameliorating hepatic insulin resistance may cause beneficial effects in liver with NAFLD/NASH.
- || Marizev (omarigliptin) / Merck (MSD)
Clinical, Journal: Effects of the Once-Weekly DPP4 Inhibitor Omarigliptin on Glycemic Control in Patients with Type 2 Diabetes Mellitus on Maintenance Hemodialysis: A 24-Week Open-Label, Multicenter Randomized Controlled Study. (Pubmed Central) - Jan 22, 2021
Our data showed that omarigliptin was non-inferior to linagliptin in glycemic control. Omarigliptin is feasible for glycemic control in patients with T2DM on maintenance HD.
- | HSK7653 / Haisco, Marizev (omarigliptin) / Merck (MSD)
Journal: Design, Synthesis and Evaluation of a Series of Novel Super-long Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. (Pubmed Central) - Nov 18, 2020
Further preclinical development of compound 2 exhibited its extraordinary efficacy in vivo and good safety profile. Clinical studies of compound 2 (Haisco HSK7653) are now ongoing in China, which revealed that inhibitor 2 could serve as an efficient candidate with a once-biweekly therapeutic regimen.
- || Marizev (omarigliptin) / Merck (MSD)
Clinical, PK/PD data, Journal: Pharmacokinetic-Pharmacodynamic (Dipeptidyl Peptidase-4 Inhibition) Model to Support Dose Rationale in Diabetes Patients, Including Those with Renal Impairment, for the Once-Weekly Administered Omarigliptin. (Pubmed Central) - Sep 30, 2020
Clinical studies of compound 2 (Haisco HSK7653) are now ongoing in China, which revealed that inhibitor 2 could serve as an efficient candidate with a once-biweekly therapeutic regimen. The models in the present analysis adequately described PK and PD characteristics of omarigliptin and supported the dosing and administration section of the omarigliptin label.
- | Retrospective data, Journal: Risk of cancer in patients treated with dipeptidyl peptidase-4 inhibitors: an extensive meta-analysis of randomized controlled trials. (Pubmed Central) - Aug 23, 2020
The models in the present analysis adequately described PK and PD characteristics of omarigliptin and supported the dosing and administration section of the omarigliptin label. Available data do not support the hypothesis of an association of DPP4i treatment with malignancies, with a possible beneficial effect for colon-rectal cancer.
- | Retrospective data, Journal: Pancreatitis and pancreatic cancer in patientes treated with dipeptidyl peptidase-4 inhibitors: an extensive and updated meta-analysis of randomized controlled trials. (Pubmed Central) - May 29, 2020
available data do not support the hypothesis of an association of DPP4i treatment with pancreatitis. Present data do not suggest any association of DPP4i with pancreatic cancer, although they are insufficient to draw definitive conclusions.
- | Marizev (omarigliptin) / Merck (MSD)
New trial: Omarigliptin in Four Healthy Egyptian Volunteers (clinicaltrials.gov) - Apr 27, 2020
P=N/A, N=4, Recruiting, Sponsor: British University In Egypt
- | 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.
- || omarigliptin (MK-3102) / Merck (MSD)
Clinical, Journal: Omarigliptin decreases inflammation and insulin resistance in a pleiotropic manner in patients with type 2 diabetes. (Pubmed Central) - Mar 28, 2020
Although how DPP4 inhibitors affect cardiovascular (CV) outcomes remains uncertain, omarigliptin might confer CV benefits at least in part, via pleiotropic anti-inflammatory or anti-insulin resistance effects.Trial registration UMIN Clinical Registry (UMIN000029288). Registered 22 September, 2017, https://upload.umin.ac.jp/UMIN000029288.
- | 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.
- | Marizev (omarigliptin) / Merck (MSD)
Trial completion, Monotherapy: Omarigliptin Add-on to Insulin in Japanese Participants With Type 2 Diabetes Mellitus (T2DM, MK-3102-039) (clinicaltrials.gov) - Sep 4, 2018
P4, N=184, Completed, Sponsor: Merck Sharp & Dohme Corp.
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. Active, not recruiting --> Completed
- Marizev (omarigliptin) / Merck (MSD)
Trial primary completion date: A Study to Assess Cardiovascular Outcomes Following Treatment With Omarigliptin (MK-3102) in Participants With Type 2 Diabetes Mellitus (MK-3102-018) (clinicaltrials.gov) - Dec 12, 2017
P3, N=4202, Terminated, Sponsor: Merck Sharp & Dohme Corp.
Active, not recruiting --> Completed Trial primary completion date: Mar 2017 --> May 2016
- | Zafatek (trelagliptin) / Takeda, Marizev (omarigliptin) / Merck (MSD)
New trial: Omarigliptin & Trelagliptin in Twelve Healthy Egyptian Volunteers (clinicaltrials.gov) - Dec 5, 2017
P=N/A, N=12, Completed, Sponsor: British University In Egypt