glibenclamide / Generic mfg. - LARVOL DELTA

Glibenclamide alleviates hydrocephalus after intraventricular hemorrhage by targeting metabolic reprogramming of border-associated macrophages. (PubMed, Exp Neurol) - "Collectively, our findings uncover the "BAM metabolic reprogramming-fibroblast activation" axis as a key pathophysiological driver of meningeal fibrosis and establish a novel mechanism for glibenclamide in preventing PHH through immunometabolic modulation, offering a promising therapeutic target for clinical intervention."

Journal • CNS Disorders • Fibrosis • Hematological Disorders • Immunology • Metabolic Disorders • Ventriculomegaly • MRC1 • TGFB1

Dapagliflozin-induced integrated improvements in left ventricular diastole, endothelial function, and arterial load: a randomized clinical trial. (PubMed, Cardiovasc Diabetol) - P4 | "In patients with T2D at intermediate risk for HFpEF, dapagliflozin was associated with more favorable changes in left ventricular diastolic function parameters compared with glibenclamide, accompanied by improvements in endothelial function and reductions in arterial impedance. These observations support the hypothesis of a vascular-myocardial pathway through which SGLT2 inhibition may exert cardioprotective effects in this population."

Clinical • Journal • Cardiovascular • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Advanced simulation and numerical evaluation of pharmaceutical solubility estimation under supercritical processing using artificial intelligence computations. (PubMed, Sci Rep) - "Leveraging an innovative combination of experimental data and advanced machine learning techniques, this study investigates the prediction of both SC-CO2 solvent density and glibenclamide solubility...The DNN and CNN models achieved commendable R-squared scores of 0.94799 and 0.88958, underscoring their adeptness in capturing the intricate interplay between temperature, pressure, and solvent density. These results demonstrate that data-driven models can reliably capture the coupled effects of temperature, pressure, and solvent density on drug solubility, providing a practical predictive framework for supercritical pharmaceutical process design."

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REPURPOSING GLYBURIDE TO TARGET KATP CHANNEL ACTIVITY REDUCES TAU PATHOLOGY, DECREASES NEUROINFLAMMATION, AND RESTORES NEURONAL FUNCTION (ADPD 2026) - "KATP channel inhibition via glyburide modulates tau pathology, dampened neuroinflammatory responses, and supported neuronal function in a sex dependent manner. This highlights the therapeutic potential of targeting neuroimmune and metabolic processes to mitigate the pathological interplay between tau accumulation, neuroinflammation, and neurodegeneration in tauopathies."

Alzheimer's Disease • CNS Disorders • Inflammation • GFAP

DAPAGLIFLOZIN-INDUCED IMPROVEMENTS IN LEFT VENTRICULAR DIASTOLE, ENDOTHELIAL FUNCTION, AND VASCULAR LOAD ARE RELATED: A RANDOMIZED CLINICAL TRIAL (ACC 2026) - " We conducted a prespecified secondary analysis of a prospective, open-label, active-controlled trial of patients with T2D on background metformin that were randomized to daily dapagliflozin 10 mg or glibenclamide 5 mg for 12 weeks. Short-term dapagliflozin improves diastolic function in T2D, in parallel with endothelial gains and lower vascular load, implicating vascular-myocardial coupling in early SGLT2 inhibitors effects."

Clinical • Diabetes

Emerging strategies in drug repurposing for decreasing the risk of age-related macular degeneration. (PubMed, Expert Opin Drug Discov) - "Notably, anti-diabetic agents including metformin, sulfonylureas, glucagon-like peptide-1 receptor agonists (GLP-1RAs), and insulin have emerged as modulators of the retinal pigment epithelium (RPE) function, photoreceptors, and retinal vascular integrity...Additional pharmacological agents include statins, glyburide, L-DOPA, fluoxetine, dimethyl fumarate, and nutraceuticals such as curcumin, melatonin, and N-acetylcysteine. Early AMD prevention through repurposed therapeutics, guided by AI-driven design and systems biology, may enable personalized care via multimodal risk stratification incorporating genetic, metabolomic, and microbiome data. Rigorous, stratified clinical trials integrating bioinformatics and precision medicine are essential to validate the most effective candidates."

Journal • Review • Age-related Macular Degeneration • Dry Age-related Macular Degeneration • Inflammation • Macular Degeneration • Ophthalmology • Retinal Disorders

Sodium Nitroprusside Potentiates Capsaicin-Activated TRPV1-mediated Relaxation of Goat Detrusor Smooth Muscle. (PubMed, Neurourol Urodyn) - "The present study demonstrates that goat DSM expresses functional TRPV1 channels and capsaicin elicits relaxation by activating these channels. The NO donor SNP further potentiates the capsaicin-induced relaxation through a NO-cGMP signalling pathway."

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GEN-100: An Open-label Phase 2b Study with Blinded Evaluation of the Combination of Amodiaquine and Potassium Canrenoate with Exenatide or Glibenclamide in Acute Ischemic Stroke (clinicaltrialsregister.eu) - P1/2 | N=150 | Sponsor: Genesis Pharma S.A.

New P1/2 trial • Cardiovascular • Ischemic stroke

Glibenclamide Attenuates Brain Edema After Intracerebral Hemorrhage Through Preservation of Blood-Brain Barrier Integrity and Glymphatic Function. (PubMed, Neurochem Res) - No abstract available

Journal • Cerebral Hemorrhage • CNS Disorders • Hematological Disorders

Modulation of KATP channels by diazoxide preserves mitochondrial function and barrier integrity under staurosporine-induced epithelial stress. (PubMed, Br J Pharmacol) - "Diazoxide may be a potential therapeutic candidate for oxidative stress-driven barrier dysfunction in gastrointestinal diseases. Future studies incorporating physiologically relevant stressors, such as LPS or H₂S, will be important to validate these protective mechanisms in contexts more directly related to microbial dysbiosis."

Journal • Gastroenterology • Gastrointestinal Disorder • MED23

Dual roles of basal NLRP3 expression in cognitive and neurogenic aging. (PubMed, Biogerontology) - "Acute pharmacological modulation of NLRP3 was examined using glibenclamide...The divergence between genetic ablation and acute pharmacological inhibition underscores the temporal specificity of NLRP3 signaling. Targeting inflammaging through selective, stage-specific modulation of NLRP3 may therefore represent a promising strategy to enhance cognitive resilience during aging."

Journal • CNS Disorders • Inflammation • Metabolic Disorders • NES • NLRP3 • SLC2A4

Evaluation of the anti-hyperglycemic and anti-dyslipidemic potential of the hydroethanolic extract of Graptophyllum pictum (Acanthaceae) aerial parts in streptozotocin-nicotinamide-induced diabetic Wistar rats. (PubMed, Metabol Open) - "Glibenclamide (10 mg/kg) as a standard and hydroethanolic extract (250 and 500 mg/kg) were used for the treatment of diabetic rats...The findings revealed that hydroethanolic extract did not have any significant hypoglycemic activity but had a significant effect (P < 0.001) when compared to the diabetic control group on lowering blood glucose levels (106 ± 1.41 versus 322.16 ± 2.08) and body weight of diabetic rats, as well as significantly restoring lipid profile (105.83 ± 1.77 versus 195.33 ± 1.49, P < 0.001, total cholesterol; 128.33 ± 1.38 versus 204.5 ± 1.94, P < 0.01, triglycerides; 42.66 ± 1.32 versus 94.83 ± 1.77, P < 0.01, low-density lipoprotein cholesterol; 29.5 ± 0.42 versus 41.83 ± 0.99, P < 0.01, very low-density lipoprotein..."

Journal • Preclinical • Diabetes • Dyslipidemia • Metabolic Disorders • Type 2 Diabetes Mellitus

Metabolite-rich Saccharomyces cerevisiae cell wall extract counter diabetic tissue damage via AMPK activation and microbiome modulation in rats. (PubMed, Tissue Cell) - "The rats were treated with glibenclamide, SCCWE (25, 50, or 100 mg/kg), or non-diabetic normal rats as a control...Histopathology and FTIR confirmed tissue and membrane restoration. SCCWE demonstrates potent antidiabetic and hepatoprotective activities, supporting its potential as a natural therapeutic for diabetes."

Journal • Preclinical • Diabetes • Dyslipidemia • Metabolic Disorders • SREBF1

Comparative safety of sulfonylurea therapies on cardiovascular and severe hypoglycemia outcomes among adults with type 2 diabetes and moderate cardiovascular risk: a target trial emulation. (PubMed, BMJ Open Diabetes Res Care) - "Among adults with T2D and moderate cardiovascular risk, glimepiride was associated with lowest risk of MACE and glipizide with lowest risk of severe hypoglycemia. These results can help inform treatment selection if sulfonylureas are used for glucose-lowering."

Journal • Cardiovascular • Diabetes • Hypoglycemia • Metabolic Disorders • Severe Hypoglycemia • Type 2 Diabetes Mellitus

Chitosan-Coated Niosomal Nanocarriers for the Co-Delivery of Glibenclamide and Curcumin in Diabetes Mellitus. (PubMed, Polymers (Basel)) - "Both uncoated and CS-coated NIOs displayed good physical and osmotic stability, with CS coating further reducing drug leakage. These results highlight the potential of niosomal systems for efficient Gli and Cur administration in T2DM."

Journal • Diabetes • Gastrointestinal Disorder • Metabolic Disorders • Type 2 Diabetes Mellitus

Glibenclamide attenuates osteoarthritis by suppressing NLRP3 inflammasome activation in synovial macrophages through the MAPK pathway. (PubMed, J Transl Med) - No abstract available

Journal • Immunology • Osteoarthritis • Pain • Rheumatology • NLRP3

Dose escalation in pentylenetetrazol kindling detects differences in chronic seizure susceptibility. (PubMed, Epilepsy Res) - "Lastly, the PTZ-DE model's effectiveness in detecting seizure differences was measured in a condition (glyburide treatment) where alterations to chronic seizure susceptibility were not detected with standard kindling. This study observed that, compared to the standard model, the PTZ-DE model corrects for background differences in PTZ susceptibility, replicates known alterations in chronic seizure thresholds, and uncovers changes in seizure threshold previously unidentified by the standard approach. The PTZ-DE model may be a superior approach for discovering new pathological mechanisms of epileptogenesis and for developing targeted therapies for seizure management."

Journal • CNS Disorders • Epilepsy • Vascular Neurology

Enhanced antidiabetic efficacy of glibenclamide with pumpkin seed extract: insights from computational and in vivo profiling. (PubMed, In Silico Pharmacol) - "Histology confirmed preservation of pancreatic, hepatic, and renal integrity. Co-administration of ethanolic extract of pumpkin seeds and glibenclamide exerts synergistic antidiabetic effects, indicating its potential as an effective adjunct to conventional therapy for managing diabetes and its associated complications."

Journal • Preclinical • Diabetes • Metabolic Disorders • ER • MAPK1 • PIK3R1 • STAT3

Neonatal diabetes linked to two new compound heterozygous mutations of the ABCC8 gene. (HMGC 2026) - "Treatment began with continuous subcutaneous insulin infusion with continuous glucose monitoring, followed by oral glibenclamide... This case highlights the importance of early molecular diagnosis for optimal management of neonatal diabetes. We describe a novel mutation in the ABCC8 gene responsible for NDM, expand the known phenotypic spectrum, and highlight the challenges associated with clinical management. These results provide new insights into the role of ABCC8 in the pathophysiology of neonatal diabetes."

Diabetes • Metabolic Disorders • Rare Diseases

Functional evaluation of pancreatic islets from patients with Beckwith-Wiedemann syndrome and congenital hyperinsulinism. (PubMed, J Clin Endocrinol Metab) - "Our expression analysis and functional evaluation of islets isolated from BWS-HI patients reveal the spectrum of insulin secretion responses found across BWS etiologies and suggest a potential role for loss of KCNQ1 expression in the complex pathophysiology responsible for the hyperinsulinism in BWS."

Journal • Hypoglycemia • KCNQ1OT1

Antidiabetic and Antihyperlipidaemic Effects of Psidium Guajava Leaf Extract in a Diabetic Rabbit Model. (PubMed, J Coll Physicians Surg Pak) - " The P. guajava leaf extract exhibited significant antihyperlipidaemic and modest antihyperglycaemic properties at higher doses (150-200 mg/kg) and exhibited protective effects on the kidney and liver."

Journal • Preclinical • Diabetes • Metabolic Disorders

Progression of diabetic retinopathy during pregnancy in a woman with ABCC8-MODY. (PubMed, Endocrinol Diabetes Metab Case Rep) - "She was managed with glibenclamide, sitagliptin, and dapagliflozin. There is a paucity of literature regarding pregnancy-related complications of ABCC8-MODY. This case highlights the risks of end organ disease in a rare form of diabetes."

Journal • Diabetes • Diabetic Retinopathy • Gestational Diabetes • Metabolic Disorders • Rare Diseases • Renal Disease • Retinal Disorders • Type 2 Diabetes Mellitus

From Agro-Waste to Therapeutic Potential: Spasmolytic Mechanisms of Vaccinium myrtillus L. Leaf Extract on Isolated Rat Ileum. (PubMed, Plants (Basel)) - "The analysis revealed phenolic acids, with chlorogenic acid as the major compound, and flavonoids, predominantly isoquercitrin. Spasmolytic activity was tested on isolated rat ileum, and the mechanism of action was monitored using models of spontaneous contractions and acetylcholine-, histamine-, CaCl2-, Bay K8644-, L-NAME-, ODQ-, apamin-, BaCl2-, charybdotoxin-, glibenclamide-, TRAM-34-, and quinine-modified contractions. The extract's activity on isolated ileum strips is primarily mediated via Ca2+ channels, cGMP, histamine, and NO pathways. Overall, this study affirms V. myrtillus leaves as a valuable source of phenolic compounds with potential for treating spasmodic gastrointestinal disorders."

Journal • Preclinical • Diabetes • Gastroenterology • Gastrointestinal Disorder • Metabolic Disorders

Loss of Beta-Cell Identity and Function as a Mechanism of Secondary Failure of Sulfonylurea Therapy in Diabetes. (PubMed, MedComm (2020)) - "To investigate the mechanisms of sulfonylurea failure, glibenclamide-releasing pellets were implanted in KK mice, a polygenic model that spontaneously develops T2D...Remarkably, KK-Glib mice showed elevated mRNA levels of Ngn3 (dedifferentiation) and α-cell identity markers along with glucagon content, suggesting α-cell neogenesis. These findings suggest that secondary failure of sulfonylurea therapy may, in part, result from loss of β-cell identity-function and increased α-cell number-identity."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Computational modeling and experimental validation for developed non-hormonal in-situ reversible cervical contraceptive plugs. (PubMed, Eur J Contracept Reprod Health Care) - "The plug acts as a physical barrier blocking the sperm cells and combination of glibenclamide and nano-copper oxide (NCO) acts as a chemical spermicidal agent, instantly killing the sperm cells coming in contact...Stability studies indicated robust formulation properties. The developed cervical plug offers a non-hormonal contraceptive option that is reversible, effective, and safe."

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