Kinedak (epalrestat) / Ono Pharma 
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  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Fostering Collaborative Care in Multiple Myeloma: An Update on the Impact of Holistic Education on Decision-Making with Antibody and CAR-T Platforms () -  Dec 7, 2024 - Abstract #ASH2024ASH_9980;    
    ABSTRACT e21008)...In a meta-analysis of outcomes from the 9 activities, learning objectives were grouped by key themes, with changes in knowledge and skills averaged across them.Results : Total learners : 13,260 (including hematologist-oncologists/oncologists : 8,179; oncology nurses : 1,296). In all activities, learners' knowledge and skills improved, with increases of : 35 percentage points (ppt) in knowledge of new evidence and changing practice guidelines supporting BCMA antibody platforms in RRMM (45% to 80%); 36 ppt in skills in treatment planning and evidence-based integration of CD38 and BCMA-targeting antibodies in the management of MM (52% to 88%); 54 ppt in ability to address safety considerations related to the use of antibody therapy and BCMA immunotherapy (32% to 86%); and 58 ppt in patient interaction skills (eg, counseling, shared decision-making) when using antibody-based and CAR-T platforms (28% to 86%).Conclusions : Improvements in knowledge and skills, combined with a greater focus on patient-centricity, suggest that learners are poised to more effectively integrate CD38 antibodies and BCMA immunotherapy into guideline-recommended MM care that improves the overall well-being and outcomes of patients with MM.
  • ||||||||||  Preclinical, Journal:  Aldose reductase with quinolone antibiotics interaction: In vitro and in silico approach of its relationship with diabetic complications. (Pubmed Central) -  Nov 13, 2024   
    Pharmacokinetic and toxicity studies in silico revealed optimal properties of AK-4 for oral administration without potential side effects. In this study, we evaluated the inhibitory potential of five quinolone antibiotics-gatifloxacin, lomefloxacin, nalidixic acid, norfloxacin, and sparfloxacin-as ARIs relevant to various physiological and pathological conditions...Our findings reveal that these quinolones moderately inhibit AR at micromolar concentrations, with inhibition constants (KIs) ranging from 1.03
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma, Farxiga (dapagliflozin) / Ono Pharma, AstraZeneca
    Clinical, Retrospective data, Journal:  Establishing a Risk Model for Diabetic Nephropathy and Addressing the Therapeutic Effect of  (Pubmed Central) -  Oct 18, 2024   
    Therefore, the present study highlights the rational development of the fluorogenic prodrugs of EPA, which will help enhance its anticancer potential with better therapeutic potential. In the phase II of the study, the research group showed better glucose metabolism and renal function than the control group after treatment (P .05).
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma, GLM101 / Glycomine
    Journal:  Treatment of congenital disorders of glycosylation: An overview. (Pubmed Central) -  Oct 14, 2024   
    Innovative therapies, targeting both the root cause and resulting manifestations, have transitioned from the research stage to practical application. The present paper aims to provide a detailed overview of these exciting developments and the rising concepts that are used to treat these ultra-rare diseases.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Journal, Metabolomic study:  Metabolomics and molecular dynamics unveil the therapeutic potential of epalrestat in diabetic nephropathy. (Pubmed Central) -  Aug 31, 2024   
    Surface-plasmon resonance assay further verified epalrestat could bind GLUT1 and NF?B proteins specifically. Overall, integrated system network analysis not only demonstrated that epalrestat could attenuate DN induced metabolic disorders and renal injuries, but also revealed that it could interact with multi-targets to play a synergistic regulatory role in the treatment of DN.
  • ||||||||||  pregabalin / Generic mfg., duloxetine / Generic mfg.
    Pregabalin & Duloxetine combination & PPAR -Gamma & Akt genes in Diabetic Peripheral Neuropathy (Exhibition Hall/Poster Area) -  Jul 18, 2024 - Abstract #IASP2024IASP_1487;    
    The mRNA expression of PPAR-gamma was observed to be significantly ( p<0.05) more upregulated following utilization of combination pharmacotherapy of pregabalin and duloxetine as compared to pregabalin monotherapy, and it indicates longer lasting analgesic efficacy of this combination, possibly due to significant ( p<0.05) modulation of PPAR-Gamma gene, which is essentially involved in insulin metabolism pathway. There is an urgent need to undertake larger prospective, multicentric RCTs to validate our clinical findings & to substantiate our findings of mRNA expressions of PPAR-Gamma gene and Akt gene following combination pharmacotherapy in patients of DPN.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Trial primary completion date:  Oral Epalrestat Therapy in Pediatric Subjects With PMM2-CDG (clinicaltrials.gov) -  Jun 2, 2024   
    P3,  N=40, Active, not recruiting, 
    Epalrestat has the potential to advance to clinical trials in drug-resistant NSCLC patients due to favorable toxicity, pharmacological profile, and bioavailability. Trial primary completion date: Feb 2024 --> Feb 2025
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Preclinical, Journal:  Oleogels for the ocular delivery of epalrestat: formulation, in vitro, in ovo, ex vivo and in vivo evaluation. (Pubmed Central) -  May 23, 2024   
    Finally, the capacity of the developed oleogels to sustain release and provide significant amounts of epalrestat to the ocular tissues was demonstrated in vivo against aqueous-based niosomes and micelles formulations loaded with the same drug concentration. Overall, the gathered information provides valuable insights into the development of oleogels for ocular drug delivery, emphasizing their safety and controlled release capabilities, which have implications for the treatment of diabetic neuropathy and other ocular conditions.
  • ||||||||||  Bystolic (nebivolol) / Menarini, AbbVie
    Trial initiation date:  EVANESCENT-DPN: Evaluating a Nitric Oxide Generator, Nebivolol As a Disease Modifier in Patients with Diabetic Neuropathy. (clinicaltrials.gov) -  May 22, 2024   
    P2/3,  N=120, Not yet recruiting, 
    Overall, the gathered information provides valuable insights into the development of oleogels for ocular drug delivery, emphasizing their safety and controlled release capabilities, which have implications for the treatment of diabetic neuropathy and other ocular conditions. Initiation date: Jan 2024 --> Jul 2024
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Journal:  Bioequivalence Study of Epalrestat for Healthy Chinese Subjects. (Pubmed Central) -  Apr 24, 2024   
    The bioequivalence study of epalrestat in healthy Chinese subjects suggests that the test and reference formulations have similar pharmacokinetics and both formulations are well tolerated in the dose range studied in healthy Chinese subjects. All these findings provided valuable pharmacokinetic knowledge for further clinical development.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Journal:  The Promise of Inferring the Past using the Ancestral Recombination Graph (ARG). (Pubmed Central) -  Feb 5, 2024   
    2019:15(9):e1008384.; Hubisz MJ, Williams AL, Siepel A. Mapping gene flow between ancient hominins through demography-aware inference of the ancestral recombination graph...In this perspective we highlight three topics that pertain to these main issues: The development of computational innovations that enable the estimation of the ARG; remaining challenges in estimating the ARG; and methodological advances for deducing evolutionary forces and mechanisms using the ARG. This perspective serves to introduce the readers to the types of questions that can be explored using the ARG, and to highlight some of the most pressing issues that must be addressed in order to make ARG-based inference an indispensable tool for evolutionary research.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Journal:  A Study of a New Certified Reference Material for Accurate Determination of the Main Fusarium Mycotoxins in Whole-Wheat Flour. (Pubmed Central) -  Jan 17, 2024   
    Compounds 1 and 5 exhibited significant AKR1B10 inhibitory activities, with IC50 values of 156.0 A certified reference material (GBW(E)100813) for whole-wheat flour was developed to ensure an accurate and reliable measurement of the main Fusarium mycotoxins (deoxynivalenol (DON), nivalenol (NIV), deoxynivalenol-3-glucoside (DON-3G), and zearalenone (ZEN))...The CRM was sufficiently homogeneous between and within bottles, and remained stable for up to 12 months at 20
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Enrollment closed:  Oral Epalrestat Therapy in Pediatric Subjects With PMM2-CDG (clinicaltrials.gov) -  Jan 11, 2024   
    P3,  N=40, Active, not recruiting, 
    Consequently, AKR1B1 holds promise as a target for treating sepsis-associated acute kidney injuries. Recruiting --> Active, not recruiting
  • ||||||||||  cisplatin / Generic mfg.
    Journal:  Drug screening identifies aldose reductase as a novel target for treating cisplatin-induced hearing loss. (Pubmed Central) -  Dec 22, 2023   
    Both Tiliroside and another clinically approved aldose reductase inhibitor, Epalrestat, inhibited cisplatin-induced oxidative stress and subsequent cell death and thus protected hearing function. These findings discovered the role of aldose reductase in the pathogenesis of cisplatin-induced deafness and identified aldose reductase as a new target for the prevention and treatment of hearing loss.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Preclinical, Journal:  A dual-acting aldose reductase inhibitor impedes oxidative and carbonyl stress in tissues of fructose- and streptozotocin-induced rats: comparison with antioxidant stobadine. (Pubmed Central) -  Oct 5, 2023   
    Malondialdehyde (MDA), glutathione S-transferase (GST), nitric oxide synthase (NOS), and catalase (CAT) were increased in the sciatic nerve of F and D. These increases were attenuated by low doses of CMTI and STB in D, but exacerbated by low-dose EPA and high-dose CMTI in F. STB and CMTI and to a lesser extent EPA improved MDA, protein-carbonyl, GST and CAT in the hearts and lungs of F and D. CMTI and STB were more effective than EPA in improving the increased MDA and protein-carbonyl levels in the kidneys of F and especially D. CMTI ameliorated renal GST inhibition in D. In the lungs, hearts, and kidneys of F and D, the GSH to GSSG ratio decreased and caspase-3 activity increased, but partially resolved with treatments. In conclusion, CMTI with ARI/AO activity may be advantageous in overcoming OS, CS, and their undesirable consequences, with low dose efficacy and limited toxicity, compared to ARI or antioxidant alone.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Journal:  Pharmacophore derived 3D-QSAR, molecular docking, and simulation studies of quinoxaline derivatives as ALR2 inhibitors. (Pubmed Central) -  Sep 12, 2023   
    In the present work, molecular dynamic simulation studies in conjugation with pharmacophore mapping and atom-based 3D-QSAR were performed on a dataset of 99 molecules in comparison with Epalrestat (reference) to mark the desirable structural features of quinoxaline analogs to generate a probable template for designing novel and effective ALR2 inhibitors...Furthermore, the pharmacophore mapping provided a five-point hypothesis (AADRR) and docking analysis revealed the active ligand-binding orientations on the active site's amino acid residues TYR 48, HIE 110, TRP 111, and TRP 219. The results of this study will help in designing potent inhibitors of ALR2 for the management of diabetic complications.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Journal, Metabolomic study:  Tracer metabolomics reveals the role of aldose reductase in glycosylation. (Pubmed Central) -  May 31, 2023   
    Using tracer studies, we demonstrate that AR inhibition diverts glucose flux away from polyol production toward the synthesis of sugar nucleotides, and ultimately glycosylation. Finally, PMM2-CDG individuals treated with epalrestat show a clinical and biochemical improvement.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Journal:  Congenital disorder of glycosylation - one size does not fit all: a parent's perspective. (Pubmed Central) -  May 14, 2023   
    This article is written by the parent of a child living with PMM2-congenital disorder of glycosylation (abbreviated to PMM2-CDG). It provides a parental perspective of the journey taken from diagnosis to present day and details the effect of off-label treatment with epalrestat.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Trial completion date, Trial primary completion date:  Oral Epalrestat Therapy in Pediatric Subjects With PMM2-CDG (clinicaltrials.gov) -  Feb 13, 2023   
    P3,  N=40, Recruiting, 
    Our results provide the first evidence that AR may be a major pathogenic contributor and novel therapeutic target for skin fibrosis in human SSc, with a treatment perspective of its inhibitor epalrestat. Trial completion date: Dec 2026 --> Dec 2025 | Trial primary completion date: Feb 2026 --> Feb 2024
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Journal:  A new series of hydrazones as small-molecule aldose reductase inhibitors. (Pubmed Central) -  Jan 6, 2023   
    Compound 4 markedly inhibited AR (IC  = 0.297 µM) in a competitive manner (K  = 0.177 µM) compared to epalrestat (K  = 0.857 µM, IC  = 0.267 µM)...In silico QikProp data of all hydrazones (1-15) were also determined to assess their pharmacokinetic profiles. Taken together, compound 4 stands out as a promising inhibitor of AR for further in vivo studies.
  • ||||||||||  Kinedak (epalrestat) / Ono Pharma
    Journal:  Mannose metabolism normalizes gut homeostasis by blocking the TNF-α-mediated proinflammatory circuit. (Pubmed Central) -  Dec 6, 2022   
    Finally, we revealed that activating PMM2 activity with epalrestat, a clinically approved drug for the treatment of diabetic neuropathy, elicited further sensitization to the therapeutic effect of mannose. Therefore, mannose metabolism prevents TNF-α-mediated pathogenic crosstalk between IECs and intestinal macrophages, thereby normalizing aberrant immunometabolism in the gut.