Joicela (lumiracoxib) / Novartis 
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 23 Diseases   1 Trial   1 Trial   58 News 
  • ||||||||||  Joicela (lumiracoxib) / Novartis
    Cell-Type Specific Induction of Cyclo-Oxygenase-2 in Layer II/III Prefrontal Cortical Neurons Mediates Stress-Induced Anxiety Phenotypes in Mice (Grand Saguaro) -  Oct 31, 2022 - Abstract #ACNP2022ACNP_457;    
    Using a pharmacological approach, we found that systemic lumiracoxib, a selective Ptgs2-inhibitor, led to a significant reduction in fear expression (2-way ANOVA, Drug effect, p=0.03)... Together these findings suggest that Ptgs2 is expressed in a dynamic, cell-type specific way in Layer II/III Penk+ neurons in mPFC, and that its role in prostaglandin and /or endocannabinoid regulation within these neurons may be an important mediator of stress-related anxiety behavior.
  • ||||||||||  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.
  • ||||||||||  tolcapone / Generic mfg.
    Clinical, Journal:  Safety data and withdrawal of hepatotoxic drugs. (Pubmed Central) -  Nov 25, 2021   
    Preclinical safety data are not sufficient to allow early prediction of DILI in humans and post-marketing safety monitoring and signal detection still should be used to identify potential serious cases of DILI. However, it seems that changes in Pharmacovigilance legislation with a closer management of drug safety may have contributed to the improvement of the risk minimization.
  • ||||||||||  Joicela (lumiracoxib) / Novartis
    Journal:  Cyclooxygenase-2 inhibition prevents stress induced amygdala activation and anxiety-like behavior. (Pubmed Central) -  Apr 28, 2021   
    Here, we examined the effects of pharmacological inhibition of COX-2 with the highly selective inhibitor Lumiracoxib (LMX) on anxiety-like behavior and in vivo basolateral amygdala (BLA) neural activity in response to acute restraint stress exposure...In addition, in vivo fiber photometry studies showed that acute stress increased calcium transients and the predicted action potential frequency of BLA neurons, which was also normalized by acute LMX pretreatment. These findings indicate pharmacological inhibition of COX-2 can prevent acute stress-induced increase in BLA cellular activity and anxiety-like behavior and provides insights into the neural mechanisms by which COX-2 inhibition could affect anxiety domain symptoms in patients with affective disorders.
  • ||||||||||  Joicela (lumiracoxib) / Novartis
    Journal:  Bioactivation of Lumiracoxib in Human Liver Microsomes: Formation of GSH- and Amino Adducts Through Acyl Glucuronide. (Pubmed Central) -  Apr 1, 2021   
    In addition to reaction with GSH, the formed 1-O-acylglucuronides were chemically unstable (T = 1.5 h in phosphate buffer) and rearranged to 2-, 3-, and/or 4-isomers, which further underwent ring-openning to form aldehyde derivatives and then reacted with NAL to yield Schiff bases derivatives (M5-M8). The present study provides a clear bioactivation profile of lumiracoxib through acyl glucuronidation, which would be one of the mechanisms attributed to the liver injury caused by lumiracoxib.
  • ||||||||||  Prexige (lumiracoxib) / Novartis, indomethacin / PLx Pharma Inc, Generic mfg.
    [VIRTUAL] A novel protective role of prostaglandin D2 in antigen-induced bronchoconstriction (Pre-congress content) -  Jul 15, 2020 - Abstract #ERS2020ERS_2155;    
    In GPT, challenge with OVA (100 µg/mL) induced a constrition (Emax of 54±6%) that was enhanced by the unselective COX inhibitor indomethacin (Emax:94±2%; p<0.05)...Selective inhibition of COX-2 by lumiracoxib did not inhibit release of PGD2 or TXA2... Endogenous PGD2 is generated via COX-1 and mediates a previously unknown inhibitory effect of the antigen-induced bronchoconstriction via DP1 receptors inhibiting mast cell release.
  • ||||||||||  Prexige (lumiracoxib) / Novartis, Zelboraf (vemurafenib) / Roche
    Journal:  Metabolic targeting synergizes with MAPK inhibition and delays drug resistance in melanoma. (Pubmed Central) -  Nov 4, 2019   
    Furthermore the addition of NSAIDs delayed the onset of RAF inhibitor resistance, most likely by counteracting the upregulation of MITF. Our data suggest that selected NSAIDs could be a promising combination partner for MAPK pathway inhibitors in the treatment of BRAF mutated melanomas.
  • ||||||||||  Prexige (lumiracoxib) / Novartis
    Journal:  Cyclooxygenase-2 inhibition reduces anxiety-like behavior and normalizes enhanced amygdala glutamatergic transmission following chronic oral corticosterone treatment. (Pubmed Central) -  Aug 31, 2019   
    ...Treatment with the highly selective COX-2 inhibitor Lumiracoxib (LMX) reversed anxiety-like behavior induced by chronic CORT...Ex vivo electrophysiology studies revealed that repeated LMX treatment normalized chronic CORT-induced increases in spontaneous excitatory glutamatergic currents recorded from anterior, but not posterior, basolateral amygdala neurons. These data indicate COX-2 inhibition can reverse chronic CORT-induced increases in anxiety-like behaviors and amygdala glutamatergic signaling, and support further clinical investigation of selective COX-2 inhibitors for the treatment of affective and stress-related psychiatric disorders.
  • ||||||||||  Joicela (lumiracoxib) / Novartis
    Trial termination:  Safety Study of Renal Function in Patients With Chronic Kidney Failure Taking Lumiracoxib or Diclofenac for Arthralgia (clinicaltrials.gov) -  Feb 10, 2013   
    P2,  N=28, Terminated, 
    These data indicate COX-2 inhibition can reverse chronic CORT-induced increases in anxiety-like behaviors and amygdala glutamatergic signaling, and support further clinical investigation of selective COX-2 inhibitors for the treatment of affective and stress-related psychiatric disorders. Recruiting --> Terminated; Interim analysis shows harma to one of the study arms.