Relafen (nabumetone) / GSK 
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  • ||||||||||  Relafen (nabumetone) / GSK
    Clinical Evolution Of Adults Diagnosed of Hypersensitivity Reactions To NSAIDs (Poster Zone) -  May 25, 2024 - Abstract #EAACI2024EAACI_2876;    
    Our aim was to evaluate the clinical evolution of adults diagnosed of NIUA in our unit Method A prospective study was carried out evaluating patients (>18 y.o) diagnosed of NIUA, all of them diagnosed by a positive initial drug provocation test(iDPT) with acetyl-salicylic acid(ASA), between 2009-2019...Concerning the culprit NSAID, ibuprofen was involved in 49%, naproxen in 13,3%, dexketoprofen in 8,8%, ASA in 8,8%, dipyrone in 8,8%, paracetamol in 4,4% and diclofenac, indomethacin and nabumetone in 2,2% respectively...Rechallenge should be considered in patients with NIUA in order to assess the persistence or not of hypersensitivity to NSAIDs. More studies are in progress in order to investigate this observation.
  • ||||||||||  Relafen (nabumetone) / GSK
    Clinical Evolution Of Adults Diagnosed of Hypersensitivity Reactions To NSAIDs (Palma) -  Apr 5, 2024 - Abstract #EAACI2024EAACI_540;    
    Our aim was to evaluate the clinical evolution of adults diagnosed of NIUA in our unit Method A prospective study was carried out evaluating patients (>18 y.o) diagnosed of NIUA, all of them diagnosed by a positive initial drug provocation test(iDPT) with acetyl-salicylic acid(ASA), between 2009-2019...Concerning the culprit NSAID, ibuprofen was involved in 49%, naproxen in 13,3%, dexketoprofen in 8,8%, ASA in 8,8%, dipyrone in 8,8%, paracetamol in 4,4% and diclofenac, indomethacin and nabumetone in 2,2% respectively...Rechallenge should be considered in patients with NIUA in order to assess the persistence or not of hypersensitivity to NSAIDs. More studies are in progress in order to investigate this observation.
  • ||||||||||  Relafen (nabumetone) / GSK
    Journal:  Dissecting CYP1A2 Activation by Arylalkanoic Acid Prodrugs toward the Development of Anti-Inflammatory Agents. (Pubmed Central) -  Jan 15, 2024   
    On the basis of these findings, it is possible to argue that subtle differences in the way CYP1A2 accommodates the ligands depend on the fine details of their molecular structures. Overall, these data suggest that compounds simply formed by an aromatic moiety bearing an appropriate alkane-derived chain could lead to innovative anti-inflammatory agents.
  • ||||||||||  Relafen (nabumetone) / GSK
    Journal:  Identification of Gut Bacterial Enzymes for Keto-Reductive Metabolism of Xenobiotics. (Pubmed Central) -  Jul 20, 2022   
    The selected enzymes display different levels of activities against additional chemicals such as two dietary compounds (i.e., raspberry ketone and zingerone), chemotherapeutic drug doxorubicin, and its aglycone metabolite doxorubicinone. Thus, our results expand the repertoire of enzymes that can reduce the ketone groups in small molecules and could serve as the basis for future personalized medicine approaches.
  • ||||||||||  celecoxib oral / Generic mfg.
    Review, Journal:  New horizons in the roles and associations of COX-2 and novel natural inhibitors in cardiovascular diseases. (Pubmed Central) -  Feb 24, 2022   
    The combination of galangin-like flavonol compounds with these prodrug metabolites may lead to the development of novel COX-2 inhibitors. This review focuses on the most compelling evidence regarding the role and mechanism of COX-2 in cardiovascular diseases and demonstrates that quercetin-like compounds exert potential cardioprotective effects by serving as cofactors of COX-2.
  • ||||||||||  Relafen (nabumetone) / GSK
    Discovery and characterization of gut microbial enzymes involved in keto-reductive metabolism (Zoom Room 1 (Virtual Room)) -  Jan 28, 2022 - Abstract #ACSSp2022ACS_Sp_4771;    
    In addition, we have also identified additional oxidoreductase homologues that have similar ketone-reducing activities from multiple human gut microbial species. Our results expand the gut bacterial enzymatic inventory for the ketone-reduction of pharmaceuticals and dietary chemicals, but it also serves as the basis for elucidating bacteria-chemical interactions and illuminating strategies for future personalized medicines and dietary plans.
  • ||||||||||  Relafen (nabumetone) / GSK
    Preclinical, Journal:  Presence or absence of microbiome modulates the response of mice organism to administered drug nabumetone. (Pubmed Central) -  Nov 6, 2021   
    In the GF mice, the expression of the DMEs (CYP1A) responsible for the formation of active form of the drug are significantly increased in the small intestine and liver after nabumetone application. These results highlight the importance of gut microbiome in processes involved in drug metabolism in the both gastrointestinal tract and in the liver with possible clinical relevance.
  • ||||||||||  Flumadine (rimantadine) / AbbVie, Relafen (nabumetone) / GSK
    Journal:  Synthesis of α-Deuterated Primary Amines via Reductive Deuteration of Oximes Using DO as a Deuterium Source. (Pubmed Central) -  Jul 3, 2021   
    This protocol exhibits excellent chemoselectivity and tolerates a variety of functional groups. The potential application of this new method was showcased in the synthesis of deuterated drugs, such as rimantadine-d, the tebufenpyrad analogue, derivatives of nabumetone and pregnenolone, and a series of building blocks for the rapid and general assembly of deuterated drugs and pesticides.
  • ||||||||||  Relafen (nabumetone) / GSK
    Preclinical, Journal:  Inhibitory effect of Jangkanghwan (Korean traditional food) on experimental ulcerative colitis in mice. (Pubmed Central) -  Jun 22, 2021   
    coloratum, dried Zingiber officinale Roscoe, etc. According to UPLC-Q-TOF MS analysis, JKH consists mainly of 17 active substances, such as pheophorbide A, nabumetone alcohol, dehydrocostus lactone, plantamajoside, kaempferol 3, 7-dirhamnoside, quercetin 3-D-glucuronide, and viscumneoside III. We investigated the preventive effects of JKH on dextran sulfate sodium (DSS)-induced ulcerative colitis in a murine model and found that JKH can reduce the damage in mice caused by DSS treatment.
  • ||||||||||  celecoxib oral / Generic mfg.
    [VIRTUAL] In vitro Anti-Staphylococcal Effect of Anti-inflammatory Drugs (Poster Hall) -  May 9, 2021 - Abstract #WMF2021WMF_139;    
    Sulindac sulfide and tolfenamic acid were only active against certain strains of S. aureus with MIC values128 and 256 μg/mL, respectively. Researchers showed that celecoxib, diacerein, and sulindac sulfide demonstrated anti-staphylococcal and anti-helicobacter pylori activity [1, 3, 4].
  • ||||||||||  ibuprofen / Generic mfg.
    Biomarker, Clinical, Journal:  Dataset of the first report of pharmacogenomics profiling in an outpatient spine setting. (Pubmed Central) -  Mar 2, 2021   
    In supplemental spreadsheets, the raw and analysed pharmacogenomics data for all 30 patients evaluated in the primary research article are additionally provided. Collectively, the presented data offer significant reuse potential in future investigations of pharmacogenomics for pain management.
  • ||||||||||  rasagiline / Generic mfg., amantadine / Generic mfg.
    Journal:  Identification of antiparkinsonian drugs in the 6-hydroxydopamine zebrafish model. (Pubmed Central) -  Jan 9, 2021   
    Among these, we selected stavudine, tapentadol and nabumetone as the most promising candidates. Our results demonstrate the functional similarities of the motor impairments exhibited by 6-hydroxydopamine-lesioned zebrafish with mammalian models of PD and with PD patients, and highlights novel molecules with antiparkinsonian potential.
  • ||||||||||  ibuprofen / Generic mfg.
    Journal:  Albumin-based transport of non-steroidal anti-inflammatory drugs in mammalian blood plasma. (Pubmed Central) -  Nov 18, 2020   
    Our comparative analysis of known SA complexes with FDA-approved drugs clearly shows that multiple medications compete for the same binding sites, indicating possibilities for undesirable physiological effects caused by drug-drug displacement or competition with common metabolites. We discuss the consequences of NSAID binding to SA in a broader scientific and medical context, particularly regarding achieving desired therapeutic effects based on an individual's drug regimen.
  • ||||||||||  Relafen (nabumetone) / GSK
    Preparation and evaluation of different size and shape metal nanoparticles for urine drug screening (Exhibit Hall A, Pennsylvania Convention Center) -  Feb 13, 2020 - Abstract #ACSSp2020ACS_Sp_5546;    
    Pamabrom, Orphenadrine and Nabumetone were the applied drugs for our studies...The LSPR showed a red shift after the binding with the drugs and an evident change in color of the samples. Therefore, the present study indicates that the combination of the nanoparticles with the selected drugs and diuretics works for the development of our outer body more sensitive and effective drug detection sensor.
  • ||||||||||  Relafen (nabumetone) / GSK
    Nephrotic Syndrome in the Elderly: Not Always What It Seems () -  Oct 23, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_5451;    
    Due to a gout flare, our patient had been prescribed Nabumetone 500 mg PO twice daily for one month prior to hospitalization by his primary care provider...Nonsteroidal anti-inflammatory drugs (NSAIDs) may cause AIN with concurrent nephrotic syndrome due to minimal change disease or membranous nephropathy. Given the increased use of medications in the elderly and risk for an ADE, it is of upmost important to be vigilant of the possible side effects of NSAIDs in this population.
  • ||||||||||  Journal:  When to stop anticoagulation, anti-platelet aggregates, and non-steroidal anti-inflammatories (NSAIDs) prior to spine surgery. (Pubmed Central) -  Sep 19, 2019   
    The anti-platelet aggregates include: Aspirin/Clopidogrel (stop >7-10 days preoperatively)...NSAIDs (generic name/commercial names should be stopped preoperatively for at least; 1 day- Diclofenac (Voltaran), Ibuprofen (Advil, Motrin), Ketorolac (Toradol); 2 days- Etodolac (Lodine), Indomethacin (Indocin); 4-days-Meloxicam (Mobic) and Naproxen (Aleve, Naprosyn, Anaprox); 4 days- Nabumetone (Relafen); 6 days - Oxaprozin (Daypro); and 10 days- Piroxicam (Feldene). Spine surgeons need to know when anti-platelet, anticoagulant, and NSAIDs therapies should be stopped prior to spine surgery to avoid perioperative bleeding complications.
  • ||||||||||  Relafen (nabumetone) / GSK
    Journal:  Crystal structure of phospholipase A in complex with 1-naphthaleneacetic acid. (Pubmed Central) -  Aug 1, 2019   
    Spine surgeons need to know when anti-platelet, anticoagulant, and NSAIDs therapies should be stopped prior to spine surgery to avoid perioperative bleeding complications. ...Apart from these findings, the theoretical binding affinities and mode of interactions of two naphthalene-based NSAIDs such as naproxen (NAP) and nabumetone (NAB) were studied through molecular modeling...The study brings out a potential scaffold for the designing of broad spectrum PLA inhibitors which can be used for inflammation or envenomation.
  • ||||||||||  Relafen (nabumetone) / GSK
    Journal:  Probing the Interplay between Amorphous Solid Dispersion Stability and Polymer Functionality. (Pubmed Central) -  Jun 26, 2019   
    ...The kinetics of the crystallization of the nonsteroidal anti-inflammatory drug nabumetone from amorphous solid dispersions containing each functionalized polymer were interpreted on the basis of two interactions: hydrogen bonding between the drug and the polymer and the solubility of the polymer in the amorphous drug...Furthermore, factors, such as the glass transition temperature of pure polymers, were uncorrelated with isothermal nucleation rates. These findings inform a framework relating polymer functionality and stability deconvoluted from the polymer chain length or backbone chemistry with the potential to aid in the design of polymers to inhibit the crystallization of hydrophobic drugs from amorphous solid dispersions.
  • ||||||||||  Trial completion, Trial primary completion date:  To Compare the Efficacy and Safety of LAYLA in Osteoarthritis Patients of the Knee (clinicaltrials.gov) -  Sep 19, 2017   
    P4,  N=134, Completed, 
    These findings inform a framework relating polymer functionality and stability deconvoluted from the polymer chain length or backbone chemistry with the potential to aid in the design of polymers to inhibit the crystallization of hydrophobic drugs from amorphous solid dispersions. Recruiting --> Completed | Trial primary completion date: Dec 2014 --> May 2015