- |||||||||| pioglitazone / Generic mfg., rosiglitazone / Generic mfg.
Journal: Babesia duncani Pyruvate Kinase Inhibitor Screening and Identification of Key Active Amino Acid Residues. (Pubmed Central) - Jun 27, 2024
Subsequently, key amino acid residues were mutated in both BdPyK I and Homo sapiens pyruvate kinase I (HPyK I), and two differential amino acid residues (isoleucine and phenylalanine) were identified between HPyK I and BdPyK I through PyK activity detection experiments. These findings lay foundation for understanding the role of PyK I in the growth and development of B. duncani, providing insights for babesiosis prevention and drug development.
- |||||||||| Invokana (canagliflozin) / J&J, Daiichi Sankyo, Mitsubishi Tanabe
Journal: Diverse Strategies for Modulating Insulin Resistance: Causal or Consequential Inference on Metabolic Parameters in Treatment-Na (Pubmed Central) - Jun 27, 2024
Group X consistently demonstrated more pronounced reductions in FBG compared to Group Y across all treatments, while other parameters including HbA1c, HOMA-B, TC, TG, HDL-C, non-HDL-C, TG/HDL-C ratio, or UA exhibited distinct regulatory responses depending on the treatment administered. These findings suggest that (1) regression to the mean is observed in the changes in insulin resistance across these therapies and (2) the modulation of insulin resistance with these therapies, either causally or consequentially, results in differential effects on glycemic parameters, beta-cell function, specific lipids, body weight, or UA.
- |||||||||| Eyevinal (ibudilast) / MediciNova
Review, Journal, Immunomodulating: Promising immunomodulators for management of substance and alcohol use disorders. (Pubmed Central) - Jun 18, 2024
These immunomodulators are currently being investigated in clinical trials described herein, specifically for their potential to decrease substance use, withdrawal severity, central and peripheral inflammation, comorbid neuropsychiatric disorder symptomology, as well as their ability to improve cognitive outcomes. We argue that although mixed, findings from recent preclinical and clinical studies underscore the potential benefit of immunomodulation in the treatment of the behavioral, cognitive, and inflammatory processes that underlie compulsive substance use.
- |||||||||| pioglitazone / Generic mfg., acarbose / Generic mfg.
Journal: Discovery of novel 6-(piperidin-1-ylsulfonyl)-2H-chromenes targeting ?-glucosidase, ?-amylase, and PPAR-?: Design, synthesis, virtual screening, and anti-diabetic activity for type 2 diabetes mellitus. (Pubmed Central) - Jun 17, 2024
We argue that although mixed, findings from recent preclinical and clinical studies underscore the potential benefit of immunomodulation in the treatment of the behavioral, cognitive, and inflammatory processes that underlie compulsive substance use. In-vitro ?-glucosidase activity was conducted firstly at 100?
- |||||||||| pioglitazone / Generic mfg.
PK/PD data, Journal: Molecular docking of antidiabetic molecules of libas (Spondias pinnata) fruit and prediction of their pharmacokinetic properties. (Pubmed Central) - Jun 17, 2024
Seven compounds namely squalene (-9.1 kcal/mol), rutin (-9 kcal/mol), catechin (-8.7 kcal/mol), quercetin (-8.5 kcal/mol), tocopherol (-8.4 kcal/mol), myricetin (-8.4 kcal/mol), and ellagic acid (-8.3 kcal/mol) showed binding affinities comparable to those of pioglitazone, a standard drug, with peroxisome proliferator-activated receptor gamma (PPAR?)...Thus, catechin could be a potential compound for the development of antidiabetic drugs. The online version contains supplementary material available at 10.1007/s40203-024-00230-3.
- |||||||||| lithium carbonate ER / Generic mfg.
Biomarker, Review, Journal: Pharmacotherapeutic value of inflammatory and neurotrophic biomarkers in bipolar disorder: A systematic review. (Pubmed Central) - Jun 16, 2024
The online version contains supplementary material available at 10.1007/s40203-024-00230-3. Inflammation in BD requires further investigation to understand the underlying immunologic mechanism, to identify predictors of treatment response, and to make informed decisions about the use and development of more effective pharmacological interventions for BD.
- |||||||||| pioglitazone / Generic mfg., rosiglitazone / Generic mfg.
Journal: Assessing immune hepatotoxicity of troglitazone with a versatile liver-immune-microphysiological-system. (Pubmed Central) - Jun 14, 2024
Through the LIMPS, we discovered that 1) TGZ can promote neutrophils to adhered hepatocytes, 2) the presence of TGZ enhances the crosstalk between macrophages and neutrophils, 3) the induction of damage in hepatocytes by TGZ at clinically relevant blood concentrations not observed in other in vitro experiments, 4) no hepatotoxicity was observed in LIMPS when exposed to rosiglitazone and pioglitazone, structurally similar analogs of TGZ, even at the higher multiples of blood drug concentration levels. As an immune-mediated liver toxicity assessment method, LIMPS is simple to operate and can be used to test multiple drug candidates to detect whether they will cause severe liver toxicity in clinical settings as early as possible.
- |||||||||| pioglitazone / Generic mfg.
Journal: Discovery of 2-deoxy glucose surfaced mixed layer dendrimer: a smart neuron targeted systemic drug delivery system for brain diseases. (Pubmed Central) - Jun 10, 2024
We further evaluated the systemic neuronal targeting and biodistribution of 2DG-D, and brain delivery of a neuroprotective agent pioglitazone (Pio) in a pediatric traumatic brain injury (TBI) model...Upon systemic administration in a pediatric mouse model of traumatic brain injury (TBI), the 2DG-D localizes in neurons at the injured brain site, clears rapidly from off-target locations, effectively delivers Pio, ameliorates neuroinflammation, and improves behavioral outcomes. The promising in vivo results coupled with a convenient synthetic approach for the construction of 2DG-D makes it a potential nanoplatform for addressing brain diseases.
- |||||||||| metformin / Generic mfg.
Clinical, Review, Journal: Metformin for preventing the progression of chronic kidney disease. (Pubmed Central) - Jun 5, 2024
Future research in this field requires adequately powered RCTs comparing metformin to placebo or standard care in those with CKD. Seven ongoing studies were identified in this review, and future updates, including their findings, may further inform the results of this review.
- |||||||||| Biomarker, Clinical, Journal: Organokines and liver enzymes in adolescent girls with polycystic ovary syndrome during randomized treatments. (Pubmed Central) - May 31, 2024
As a post hoc endpoint, the organokines fibroblast growth factor-21 (FGF21), diazepam-binding protein-1 (DBI), and meteorin-like protein (METRNL) were assessed by ELISA after 6 months of OC (N = 26) or spiomet (N = 28)...The on-treatment increase in ALT and GGT levels occurring only in OC-treated girls is associated with circulating METRNL levels, suggesting enhanced METRNL synthesis as a reaction to the hepatic changes elicited by OC treatment. https://doi.org, identifiers 10.1186/ISRCTN29234515, 10.1186/ISRCTN11062950.
- |||||||||| pioglitazone / Generic mfg.
Preclinical, Journal: Mogroside Alleviates Diabetes Mellitus and Modulates Intestinal Microflora in Type 2 Diabetic Mice. (Pubmed Central) - May 30, 2024
Kunming mice with type 2 diabetes mellitus (T2DM) induced by high-fat diet and intraperitoneal injection of streptozotocin were randomly divided into model, pioglitazone (2.57?mg/kg) and mogroside (200, 100, and 50?mg/kg) groups...Moreover, mogroside treatment reduced the relative abundance of Firmicutes and Proteobacteria (the inhibition rate of Proteobacteria was 85.17% in the low-dose group) and increased the relative abundance of Bacteroidetes (growth rate up to 40.57%, high-dose group) in the intestines of diabetic mice. This study reveals that mogroside can relieve T2DM, regulating intestinal flora and improving intestinal mucosal barrier, indicating that mogroside can be a potential therapeutic agent or intestinal microbiota regulator in the treatment of T2DM.
- |||||||||| pioglitazone / Generic mfg.
Journal: Pioglitazone-induced alterations of purine metabolism in healthy male subjects. (Pubmed Central) - May 21, 2024
Pioglitazone-dependent endogenous metabolites and metabolic ratio indicated the potential effect of pioglitazone on the activation of PPAR and fatty acid synthesis. Additional studies involving patients are required to validate these findings.
- |||||||||| Potential for New Oral Insulin Sensitizers in Combination with GLP-1 Agonists (Poster Hall (West A4-B2); 892) - May 20, 2024 - Abstract #ADA2024ADA_2897;
MSDC-0602K (azemiglitazone) is a second-generation insulin sensitizer that was designed based on the knowledge of the activity of active metabolites of the first-generation insulin sensitizer pioglitazone...Here we have looked specifically at the 23 subjects with NASH (MASH) and type 2 diabetes who had been enrolled in the trial while on a stable dose of a GLP1 agonist (11 liraglutide, 8 dulaglutide, and 4 exenatide)...Some subjects who had been on a GLP1 continued to lose weight while others did not. Given the major effects of his pharmacology to improve insulin sensitivity Iin skeletal muscle and based on some existing precedent with high dose pioglitazone, maintenance of lean mass could be a component of the overall pharmacology achieved with oral metabolic modulators.
- |||||||||| Victoza (liraglutide) / Novo Nordisk, Jardiance (empagliflozin) / Eli Lilly, Boehringer Ingelheim, Leqvio (inclisiran) / Novartis
Nonhuman Primate Obesity Model for the Translation of Target-Based Precision Medicine (Poster Hall (West A4-B2); 1647) - May 20, 2024 - Abstract #ADA2024ADA_2594;
This benefit was seen even in absence of concurrent use of sglt2 inhibitors or glucagon-like peptide 1 receptor agonists. Furthermore, monkeys showed similar response as observed in humans after the administration of reference or test compounds, such as liraglutide, semaglutide, inclisiran, pioglitazone, empagliflozin etc. Significant reduction in food intake (-38.5
- |||||||||| pioglitazone / Generic mfg.
Feasibility and Acceptability of an Intervention to Improve Metabolic Liver Disease in Latino/a and Black Patients with Diabetes (Poster Hall (West A4-B2); 1986) - May 20, 2024 - Abstract #ADA2024ADA_1637;
The intervention was entirely remote and included: a) MASLD education; b) monthly diet/lifestyle counseling sessions; c) T2D medication management, with prioritization of glucagon-like peptide-1 receptor agonists and pioglitazone as appropriate; and d) clinically-indicated ordering of liver tests and referrals...Of the 10 participants, 5 had their T2D medications adjusted, 2 underwent liver ultrasound (both had steatosis) and 1 was referred to Hepatology. This study demonstrates feasibility and acceptability of an intervention that delivers evidence-based care for MASLD in Latino/a and Black patients with T2D.
- |||||||||| pioglitazone / Generic mfg.
Journal: Pioglitazone Phases and Metabolic Effects in Nanoparticle-Treated Cells Analyzed via Rapid Visualization of FLIM Images. (Pubmed Central) - May 11, 2024
PGZ is recognized for its efficacy in addressing insulin resistance and hyperglycemia in type 2 diabetes mellitus, and polymeric nanoparticles offer versatile platforms for drug delivery due to their biocompatibility and controlled release kinetics. This study lays the foundation for a better understanding via phasor-FLIM of the organization and effects of drugs, in particular, PGZ, within NPs, aiming at better control of encapsulation and pharmacokinetics, and potentially at novel anti-diabetics theragnostic nanotools.
- |||||||||| topiramate / Generic mfg., pioglitazone / Generic mfg.
Journal: The combined pioglitazone and topiramate therapy for management of pediatric patients with severe MASLD. (Pubmed Central) - May 10, 2024
This study lays the foundation for a better understanding via phasor-FLIM of the organization and effects of drugs, in particular, PGZ, within NPs, aiming at better control of encapsulation and pharmacokinetics, and potentially at novel anti-diabetics theragnostic nanotools. In summary, this case series provides encouraging results about the efficacy of the combined pioglitazone and topiramate therapy for the management of adolescents with severe MASLD, which should be further explored in clinical studies.
- |||||||||| Preclinical, Review, Journal: Alternative treatment of polycystic ovary syndrome: pre-clinical and clinical basis for using plant-based drugs. (Pubmed Central) - May 10, 2024
Recently, herbal products are gaining popularity due to their wide biological activities, safety, availability, and efficacy. The present review covers aetiology, current treatment, pathophysiology, and detailed pre-clinical and clinical studies on plants and phytochemicals that are proven to be useful for the treatment of symptoms associated with PCOS.
- |||||||||| pioglitazone / Generic mfg.
Preclinical, Journal: AGPAT3 Deficiency Impairs Adipocyte Differentiation and Leads to a Lean Phenotype in Mice. (Pubmed Central) - May 8, 2024
Interestingly, pioglitazone treatment rescued the adipogenic deficiency in Agpat3 deficient cells...It is possible that adipogenic impairment in Agpat3 deficient cells potentially leads to reduced adipose mass. Findings from this work support the unique role of AGPAT3 in adipose tissue.
- |||||||||| pioglitazone / Generic mfg.
Ex-Vivo Administration of Pioglitazone during Normothermic Machine Preservation for Reduction of Liver Injury (Poster Hall, Exhibit Hall A, Level 2) - May 6, 2024 - Abstract #ATC2024ATC_472;
agonists have been shown to mediate chronic liver inflammation in NASH and the current preliminary study suggests they may be able to mediate acute reperfusion injury response as well. The effects were seen within a relatively short NMP treatment duration making its use optimal for further studies in ex-vivo treatment of marginal livers to prevent reperfusion and ischemia reperfusion related injury.
- |||||||||| Retrospective data, Journal: Meta-analysis of the global distribution of clinically relevant CYP2C8 alleles and their inferred functional consequences. (Pubmed Central) - Apr 29, 2024
These results can serve as a valuable resource for CYP2C8 allele frequencies and distribution estimates of CYP2C8 phenotypes that could help identify populations at risk upon treatment with CYP2C8 substrates. The high variability between ethnic groups incentivizes high-resolution pharmacogenetic profiling to guide precision medicine and maximize its socioeconomic benefits, particularly for understudied populations with distinct genetic profiles.
- |||||||||| Review, Journal: Advancements in pharmacological treatment of NAFLD/MASLD: a focus on metabolic and liver-targeted interventions. (Pubmed Central) - Apr 29, 2024
The first is to repurpose drugs that originally targeted T2DM and/or obesity, such as pioglitazone, glucagon-like peptide 1 receptor agonists (liraglutide and semaglutide), multi-agonists (tirzepatide and retatrutide), and sodium-glucose transporter 2 inhibitors...Among those, we focused on resmetirom, fibroblast growth factor 21 analogs, and lanifibranor, as they are currently in Phase 3 of their clinical trial development...As occurs in many chronic conditions, combination therapy might lead to better outcomes. In the case of non-alcoholic steatohepatitis, we speculate that drugs treating underlying metabolic co-morbidities might play a bigger role in the earlier stages of disease, while liver-targeting molecules will become vital in patients with more advanced disease in terms of inflammation and fibrosis.
- |||||||||| pioglitazone / Generic mfg., rosiglitazone / Generic mfg.
Journal: Cytotoxicity and toxicoproteomics analysis of thiazolidinedione exposure in human-derived cardiomyocytes. (Pubmed Central) - Apr 24, 2024
Regarding pioglitazone, the findings suggested the potential activation of the interplay between the complement and coagulation systems and the disruption of the cytoskeletal architecture, which was primarily mediated through the integrin-signalling pathways responsible for pioglitazone-induced myocardial contractile failure. Collectively, this study unlocks substantial mechanistic insight into TZD cardiotoxicity, providing the rationale for future optimisation of antidiabetic therapies.
- |||||||||| pioglitazone / Generic mfg.
Preclinical, Journal: The Active Ingredient Catalpol in Rehmannia glutinosa Reduces Blood Glucose in Diabetic Rats via the AMPK Pathway. (Pubmed Central) - Apr 22, 2024
The T2DM model was constructed by intraperitoneal injection of streptozotocin into Sprague-Dawley (SD) rats, which were randomly grouped into diabetes model group, pioglitazone group, Rehmannia glutinosa group, catalpol high-dose group, catalpol low-dose group and normal control group.The intervention was continued for 28 d, and changes in body weight, fasting blood glucose, insulin and lipid levels were observed...The low dose of catalpol decreased the concentration of low-density lipoprotein cholesterol (LDL), while the high dose of catalpol increased the concentration of LDL. As an active ingredient in Rehmannia glutinosa, catalpol has the potential to lower blood glucose and improve blood lipids in diabetes treatment, and its action may be achieved by regulating the adenosine 5'-monophosphate (AMP)-activated protein kinase (AMPK) signaling pathway, which provides a new idea for the development of new diabetes therapeutic approaches.
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