nateglinide / Generic mfg. - LARVOL DELTA

Asymmetric α-amination of aldehydes at low catalytic loading: application to the synthesis of solriamfetol and nateglinide. (PubMed, Org Biomol Chem) - "This method exhibits a broad substrate scope, affording products in up to 96% yield and 94% ee. This scalable methodology is applied to the concise asymmetric synthesis of solriamfetol and nateglinide."

Journal

Dynamic stability-driven machine learning improves binding pose identification on human serum albumin. (PubMed, J Comput Aided Mol Des) - "External validation using a temporally independent nateglinide-HSA complex further supported the utility of the framework for discriminating plausible binding modes within the HSA setting...These findings show that short MD simulations can provide practically useful and interpretable features for machine-learning-based binding-pose identification on HSA. While broader validation will be required to establish applicability beyond HSA, the proposed framework offers a practical strategy for improving binding-mode analysis in pharmacokinetically relevant HSA studies."

Journal

Renoprotective Potential of Nateglinide in an Acute Kidney Injury Model. (PubMed, Int J Mol Sci) - "Histopathology confirmed attenuated renal damage in Nat-treated groups (p < 0.0001). These results indicate that Nat confers significant renoprotection against renal I/R injury via suppression of oxidative stress and inflammation."

Journal • Acute Kidney Injury • Cardiovascular • Inflammation • Nephrology • Oncology • Renal Disease • Reperfusion Injury • CAT • IL1B • TNFA

Tissue-Specific Differential Flux Analysis Reveals Metabolic Insights Into Pancreatic β-Cell Dysfunction in Type 2 Diabetes. (PubMed, Biotechnol Bioeng) - "The most commonly used antidiabetic drugs, such as metformin, glyburide, nateglinide, and insulin, overlapped with our identified drug candidates, supporting the reliability of our predictions. Additionally, 341 FDA-approved drug candidates were identified that may serve as potential therapeutics targeting T2D biomarker genes. These results pave the way for developing targeted therapeutic interventions to restore healthy β-cell function and improve glucose homeostasis in T2D patients."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

IG20/MADD gene functional isoform KIAA0358 can promote glucose and insulin secretion in repaglinide-induced pancreatic β-cells. (PubMed, Acta Pharmacol Sin) - "Glucose tolerance tests revealed that repaglinide, mitiglinide, and nateglinide failed to lower blood glucose levels or enhance insulin secretion in KMA1ko mice, suggesting that IG20 deficiency significantly diminishes the therapeutic efficacy of glinides. Therefore, by regulating the activation states of Rab3A and Rab27A, KIAA0358 mediated the transport and docking of insulin granules to the plasma membrane. This study also highlights that the genes encoding non-drug target proteins can influence drug efficacy and provides a novel conceptual foundation for precision medicine strategies aimed at reducing drug resistance and enhancing the clinical efficacy of glinides."

Journal • Diabetes • Metabolic Disorders • MLPH • RAB27A

Noninsulin drugs for type 2 diabetes. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

An Isocratic RP-HPLC Method for Simultaneous Quantification of Nateglinide and Furosemide: Application to In Vitro Caco-2 Intestinal Permeability Studies of Nanodrugs. (PubMed, Biomed Chromatogr) - "Varying stabilizers impact intestinal permeability. This work simulates pragmatic conditions, as cardiovascular patients are co-administered these drugs, paving the pathway to using our novel method for a wide range of "bench-to-bedside" nanomedicine research designs to tackle the challenges of polypharmacy in this complex population."

Journal • Preclinical • Cardiovascular

Insights into Dual Binding Modes of Nateglinide to Human Serum Albumin. (PubMed, ACS Med Chem Lett) - "The calculated binding free energy values were consistent with experimentally determined data. Our results highlight the structural adaptability of HSA and emphasize the possibility of alternative ligand binding modes existing within a single binding site, as well as the importance of identifying and characterizing these modes to enhance our understanding of drug-plasma protein interactions."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Structural similarity-based search for glinides exhibiting cis- and trans-inhibitory activity toward uric acid transporter 1. (PubMed, Mol Pharmacol) - "Three glinides (nateglinide, mitiglinide, and repaglinide) all inhibited urate uptake by HEK-hURAT1 cells concentration-dependently (IC50: nateglinide, 39 μM; mitiglinide, 63 μM; repaglinide, 3.9 μM). SIGNIFICANCE STATEMENT: Some types of loop diuretics, statins, angiotensin receptor blockers, and glinides were predicted to affect URAT1, based on their chemical structural similarity to salicylic acid, the structure of which allows it to interact with URAT1. Glinides in particular showed cis- and trans-inhibitory activity toward URAT1."

Journal

An Underlying Mechanism for the Altered Hypoglycemic Effects of Nateglinide in Rats with Acute Peripheral Inflammation. (PubMed, Biol Pharm Bull) - "As a result, the expression of preproinsulin and ABCC8 mRNA increased in API rats. These findings suggest that the hypoglycemic effect of NTG was potentiated in API rats due to increased insulin secretion in the pancreas, which was caused by enhanced preproinsulin synthesis and expression of the sulfonylurea receptor."

Journal • Preclinical • Inflammation

Nateglinide: A comprehensive profile. (PubMed, Profiles Drug Subst Excip Relat Methodol) - "Additionally, the chapter covers a literature review of various methods of analysis of Nateglinide, such as X-ray powder diffraction pattern analysis, differential scanning calorimetry, spectrophotometric, chromatographic, capillary electrophoresis and immunoassay methods. Moreover, the pharmacology of the title drug including pharmacokinetics, pharmacodynamics, mechanism of action, drug-drug and drug-food interactions are also reviewed."

Journal • Review • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Microwave-derivatized enhanced-spectrofluorophotometric characterization of nateglinide-loaded solid dispersion adsorbate and greenness profile assessment of method. (PubMed, Anal Sci) - "The published analytical methods were compared to the enhanced-spectrofluorophotometric method for user-friendliness, efficiency, cost-of-analysis, and environmental friendliness. The proposed sensitive-spectrofluorophotometric method was found to be robust, rapid, eco-friendly, cost-effective, and simple for the estimation of nateglinide."

Journal • Diabetes • Metabolic Disorders

Long-term effects of different hypoglycemic drugs on carotid intima-media thickness progression: a systematic review and network meta-analysis. (PubMed, Front Endocrinol (Lausanne)) - "This network meta-analysis compared the effects of 14 antidiabetic drugs (acarbose, alogliptin, exenatide, glibenclamide, glimepiride, ipragliflozin, metformin, nateglinide, pioglitazone, rosiglitazone, sitagliptin, tofoglifozin, troglitazone, voglibose) on the progression of cIMT. Long-term treatment of exenatide, alogliptin, and metformin may be more effective than other hypoglycemic drugs in slowing the progression of cIMT. https://www.crd.york.ac.uk/PROSPERO/, identifier CRD42024519474."

Clinical • Journal • Retrospective data • Review • Atherosclerosis • Cardiovascular • Diabetes • Dyslipidemia • Metabolic Disorders

Loss of ATP-sensitive potassium channel expression and function in the nervous system decreases opioid sensitivity in high-fat-diet-fed mouse model of diet-induced obesity. (PubMed, Diabetes) - "HFD mice had decreased antinociception to systemic morphine compared to control diet (CON) mice, which was expected as KATP channels are downstream targets of opioid receptors. Mechanical hypersensitivity in HFD mice was exacerbated after systemic treatment with glyburide or nateglinide, KATP channel antagonists clinically used to control blood glucose levels...These data present a potential link between KATP channel function and neuropathy during early stages of diabetes. There is a need for increased knowledge in how diabetes affects structural and molecular changes in the nervous system, including ion channels, to lead to the progression of chronic pain and sensory issues."

Journal • Preclinical • Diabetes • Genetic Disorders • Immunology • Metabolic Disorders • Obesity • Pain • KCNJ11

The use of carboxyfluorescein reveals the transport function of MCT6/SLC16A5 associated with CD147 as a chloride-sensitive organic anion transporter in mammalian cells. (PubMed, J Pharm Sci) - "Monocarboxylate transporter 6 (MCT6/SLC16A5) has been reported to localize to the apical and basolateral membranes of human enterocytes and to transport organic anions such as bumetanide and nateglinide in the Xenopus oocyte expression system; however, its transport functions have not been elucidated in detail. MCT6-mediated 5-CF uptake was saturable with a K of 1.07 mM and inhibited by several substrates/inhibitors of organic anion transporters and extracellular Cl ion with an IC of 53.7 mM. These results suggest that MCT6 is a chloride-sensitive organic anion transporter that can be characterized using 5-CF as a fluorescent probe."

Journal • BSG

Analysis of Hypoglycemic Drugs by Liquid Chromatography-Tandem Mass Spectrometry. (PubMed, Methods Mol Biol) - "Isotopic labeled chlorpropamide-d4, glimepiride-d5, glyburide-d11, nateglinide-d5, repaglinide-ethyl-d5, rosiglitazone-d3, and zomepirac were used as the internal standards. The cutoffs for each drug were as follows: chlorpropamide 100 ng/mL, tolazamide 50 ng/mL, tolbutamide 20 ng/mL, glimepiride 20 ng/mL, glipizide 5 ng/mL, glyburide 5 ng/mL, repaglinide 5 ng/mL, rosiglitazone 20 ng/mL, pioglitazone 20 ng/mL, and nateglinide 5 ng/mL."

Journal • Hypoglycemia • Solid Tumor

Identification of Novel Alkaloids from Portulaca oleracea L. and Characterization of Their Pharmacokinetics and GLP-1 Secretion-Promoting Activity in STC-1 Cells. (PubMed, J Agric Food Chem) - "Furthermore, compound 3 also exhibited slightly faster absorption than nateglinide, as shown by pharmacokinetic analysis conducted in rats. Therefore, the results showed that some purslane alkaloids (such as compound 3) had good pharmacological activity in vivo and may have preventive and therapeutic effects on diabetes."

Journal • PK/PD data • Diabetes • Metabolic Disorders • STC1

Resolving D-Amino Acid Containing Peptides Using Ion Mobility-Mass Spectrometry: Challenges and Recent Developments. (PubMed, Crit Rev Anal Chem) - "Indeed, some peptide molecules with D-amino acids in their structure have already found their way to clinical use such as the antibacterial gramicidin and the antidiabetic nateglinide...Similarly, we emphasized how recent developments in IM-MS have improved their detection and analysis. Consequently, the LC-IM-MS/MS platform appears to be promising in isomeric mixture analysis."

Journal • Review

Deep Eutectic Solvents Based on L-Arginine and 2-Hydroxypropyl-β-Cyclodextrin for Drug Carrier and Penetration Enhancement. (PubMed, AAPS PharmSciTech) - "The solubility of ibuprofen, norfloxacin, and nateglinide in DES with 45% of water were increased by 79.3, 44.1, and 3.2 times higher than that in water, respectively. The permeation mechanism of DES with lower content of water (45%) was mainly by changing the fluidization of lipids, while changing the secondary structure of keratin in stratum corneum (SC) at higher water content (50% and 60%). These nonirritant and viscous fluid like DESs with good drug solubility and permeation enhancing effects have broad application prospect in the field of drug solubilization and transdermal drug delivery system."

Journal

Helical-Like Assembly of Nateglinide as Coating for Oral Delivery of Insulin and Their Synergistic Prevention of Diabetes Mellitus. (PubMed, Adv Sci (Weinh)) - "This further confirms that Ins@Alg/NG ameliorated Ins resistance mainly through activating Insreceptor substrate 1 (IRS1), protein kinase B (AKT), and AMP-activated protein kinase (AMPK), as well as by repressing glycogen synthase kinase-3β (GSK-3β). The strategy of using the assembly of NG as a coating achieves the oral delivery of insulin and showcases a potential for the treatment of diabetes."

Journal • Diabetes • Gastrointestinal Disorder • Metabolic Disorders • AMPK • GSK3B

Identification of Potential Insulinotropic Cytotoxins from Indian Cobra Snake Venom Using High-Resolution Mass Spectrometry and Analyzing Their Possible Interactions with Potassium Channel Receptors by In Silico Studies. (PubMed, Appl Biochem Biotechnol) - "Nateglinide and repaglinide are synthetic small-molecule drugs that control sugar levels in the blood in type 2 diabetes, which were used as a positive control in ELISA. At this stage, the focus is on the efficiency of the cytotoxins to induce insulin. Additional work is ongoing on animal models to see the extent of the beneficial effects and efficiency to cure diabetes using streptozotocin-induced models."

Journal • CNS Disorders • Diabetes • Metabolic Disorders • Oncology • Type 2 Diabetes Mellitus

Long-term effects of lowering postprandial glucose level on cardiovascular outcomes in early-stage diabetic patients with coronary artery disease: 10-year post-trial follow-up analysis of the DIANA study. (PubMed, J Diabetes Complications) - "The early improvement of PPG significantly reduced MACE and unplanned coronary revascularization in IGT subjects during the post-trial 10-year period."

Journal • Acute Coronary Syndrome • Atherosclerosis • Cardiovascular • Coronary Artery Disease • Diabetes • Dyslipidemia • Metabolic Disorders • Type 2 Diabetes Mellitus

Integration of Human and Viral miRNAs in Epstein-Barr Virus-Associated Tumors and Implications for Drug Repurposing. (PubMed, OMICS) - "Importantly, we used the DEMs during EBV latent infection types I, II, and III to identify the candidate drugs for repurposing: Glyburide, Levodopa, Nateglinide, and Stiripentol, among others. To the best of our knowledge, this is the first integrative analyses that identified DEmiRs and DEMs as potential therapeutic targets and predicted drugs as potential candidates for repurposing against EBV-related tumors."

Journal • Epstein-Barr Virus Infections • Hematological Malignancies • Hodgkin Lymphoma • Infectious Disease • Lymphoma • Nasopharyngeal Carcinoma • Oncology • Solid Tumor • MIR3651 • MIR98

The effect of Nateglinide and Octreotide on follicular morphology and free radical scavenging system in letrazole-induced rat model of PCOS. (PubMed, Eur Rev Med Pharmacol Sci) - "Both NG and OCT reverses atretic and degenerate follicle damage due to PCOS through TLR-4, antioxidant and anti-inflammatory pathways."

Journal • Preclinical • Gynecology • Polycystic Ovary Syndrome • IGF1 • IL6 • TLR4 • TNFA

Drugs for type 2 diabetes. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus