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  • ||||||||||  cyclophosphamide / Generic mfg.
    Repurposing NSAIDs for chemo-immunotherapy: mechanisms beyond COX inhibition (Section 22; Poster Board #9) -  Mar 14, 2023 - Abstract #AACR2023AACR_8518;    
    Cyclophosphamide (CTX) is a widely used antineoplastic chemotherapeutic agent with immunostimulatory activities when used at low-medium doses...Other potential mechanisms, including modulation of chronic interferon signaling in tumor cells, have also been investigated. Altogether, our study sheds light on the multiple mechanisms underlying indomethacin
  • ||||||||||  cisplatin / Generic mfg., methotrexate / Generic mfg.
    Blockade of the cyclooxygenase-2 prevents chemotherapy-induced cognitive impairments (Section 14; Poster Board #30) -  Mar 14, 2023 - Abstract #AACR2023AACR_4916;    
    COX-2 inhibitors can be repurposed to enhance therapeutic benefits of PD-1/PD-L1 targeting agents in breast cancer patients. Similar as cisplatin treatment, the levels of COX-2 expression began to increase at 0.1
  • ||||||||||  ADT-007 / ADT Pharma, ChemomAb
    ADT-007 binds RAS and inhibits RAS signaling (Section 18; Poster Board #15) -  Mar 14, 2023 - Abstract #AACR2023AACR_3901;    
    Finally, ADT-007 demonstrated RAS-selective growth inhibition in isogenic pancreatic and colorectal cancer cell pairs (BxPC-3, HT29). Together, these experiments support further development of ADT-007 and related analogs for treatment of RAS-driven cancers.
  • ||||||||||  ADT-007 / ADT Pharma, ChemomAb
    Validation of a novel pan-Ras inhibitor, ADT-007, against lethal variants of prostate cancer (Section 17; Poster Board #28) -  Mar 14, 2023 - Abstract #AACR2023AACR_3883;    
    Finally, using PCa patient datasets, we showed that ADT-007 is potentially capable of reversing the expression of several genes associated with biochemical recurrence. Thus, our results show that ADT-007 is a novel drug candidate that circumvents subclonal aggressiveness, drug resistance, and stemness in lethal PCa through simultaneous inhibition of multiple oncogenic factors/pathways.
  • ||||||||||  ADT-030 / ADT Pharma
    ADT-030, a novel dual-acting RAS and ?-catenin inhibitor with robust antitumor activity (Section 17; Poster Board #23) -  Mar 14, 2023 - Abstract #AACR2023AACR_3878;    
    Thus, our results show that ADT-007 is a novel drug candidate that circumvents subclonal aggressiveness, drug resistance, and stemness in lethal PCa through simultaneous inhibition of multiple oncogenic factors/pathways. These results support further development of ADT-030, a novel inhibitor of RAS and ?-catenin signaling for the treatment of lung cancer and other RAS driven cancers, including those with co-occurring mutations in the Wnt/?-catenin pathway.
  • ||||||||||  ADT-030 / ADT Pharma
    A novel dual-acting RAS/?-catenin inhibitor activates antitumor immunity to potentiate cancer immunotherapy (Section 17; Poster Board #9) -  Mar 14, 2023 - Abstract #AACR2023AACR_2539;    
    Bulk and single-cell RNAseq is being conducted to determine the impact of ADT-030 on the cell compositions and transcriptomic changes in the TME. Altogether, our study provides insight into the mechanism of action of ADT-030 and underscores the potential of ADT-030 as a monotherapy or in combination with immunotherapies for RAS and Wnt/?-catenin driven cancers.
  • ||||||||||  indomethacin / Generic mfg., hydrocortisone / Generic mfg., paracetamol / Generic mfg.
    Journal:  Evaluation of Health-Related Values and Preferences of Adults Who Were Preterm Infants and Parents of Preterm Infants Concerning Use of Prophylactic Cyclooxygenase Inhibitor Drugs. (Pubmed Central) -  Mar 14, 2023   
    To explore the health-related values and preferences of adults who were preterm infants and families of preterm infants concerning the prophylactic use of indomethacin, ibuprofen, and acetaminophen initiated within the first 24 hours after birth...Relative importance of clinical outcomes, willingness to use each of the COX-Is when presented as the only option, preference for using prophylactic hydrocortisone vs indomethacin, willingness to use any of the COX-Is when all 3 options are available, and relative importance of having family values and preferences included in decision-making...The findings of this cross-sectional study of former preterm infants and parents of preterm infants suggest that there was minimal variability in how participants valued the main outcomes, with death and severe IVH being rated as the 2 most important undesirable outcomes. While indomethacin was the most preferred form of prophylaxis, variability was noted in the choice of COX-I interventions when participants were presented with the benefits and harms of each drug.
  • ||||||||||  rofecoxib (TRM-201) / Tremeau Pharma
    PK/PD data, Journal:  Modelling Adult COX-2 Cerebrospinal Fluid Pharmacokinetics to Inform Paediatric Investigation. (Pubmed Central) -  Mar 7, 2023   
    An additional transfer factor was required to account for passage across the blood-brain barrier. Use of a target concentration strategy for dose and consequent plasma (total and unbound) and CSF concentration prediction could be used to inform pediatric clinical studies.
  • ||||||||||  naproxen ER / Generic mfg.
    Clinical, Review, Journal, Surgery:  Current and Emerging COX inhibitors for Treating Postoperative Pain Following Oral Surgery. (Pubmed Central) -  Feb 27, 2023   
    Head-to-head and comparative studies do not show a clear-cut "optimal NSAID" in this setting, although ibuprofen, ketoprofen, dexketoprofen, and naproxen have gained most acceptance. Combination therapy with other analgesics or adjuvants is largely accepted.
  • ||||||||||  celecoxib oral / Generic mfg.
    Journal:  Selenocoxib-3, a novel anti-inflammatory therapeutic effectively resolves colitis. (Pubmed Central) -  Feb 27, 2023   
    The expression profiles of COX-1/2 demonstrated mitigation of pro-inflammatory mediators thereby promoting anti-inflammatory efficacy of Selenocoxib-3 when compared with Celecoxib. The current study suggests translational applicability of Se-containing novel class of COX inhibitors for efficiently managing inflammatory disorders such as UC.
  • ||||||||||  indomethacin / Generic mfg.
    Journal:  Piezo1 activation induces relaxation of the pudendal artery and corpus cavernosum. (Pubmed Central) -  Feb 27, 2023   
    In the CC, Yoda1 was also tested in the presence of indomethacin (non-selective COX inhibitor) and tetraethylammonium (TEA, non-selective potassium channel inhibitor)...In conclusion, our data demonstrate that Piezo1 is expressed and induced the relaxation of the pudendal artery and CC. Further studies are necessary to determine its role in penile erection and if erectile dysfunction is associated with Piezo1 deficiency.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg., celecoxib oral / Generic mfg.
    Anti-proliferative and anti-cancer properties of a novel class of cyclooxygenase inhibitors (Hall F-H (Indiana Convention Center)) -  Feb 14, 2023 - Abstract #ACSSp2023ACS_SP_4767;    
    Celecoxib and doxorubicin were used as reference molecules in COX inhibition and antiproliferative assays, respectively. If these compounds are potential inhibitors of the COX-2 isozyme and certain cancer cell lines, they may be of benefit for future cancer patients.
  • ||||||||||  Zolinza (vorinostat) / Merck (MSD)
    Journal, Epigenetic controller:  Solid-Phase Parallel Synthesis of Dual Histone Deacetylase-Cyclooxygenase Inhibitors. (Pubmed Central) -  Feb 12, 2023   
    The most promising dual inhibitors, C3 and C4, evoked antiproliferative effects in the low micromolar concentration range and caused a significant increase in apoptotic cells. In contrast to previous reports, the simultaneous inhibition of HDAC and COX activity by dual HDAC-COX inhibitors or combination treatments with vorinostat and celecoxib did not result in additive or synergistic anticancer activities.
  • ||||||||||  aspirin / Generic mfg.
    Leukogriene B4 Augmentation After The Administration Of Aspirin: Is A Cause Of Antiplatelet Activity Alteration Triggered By Cyclooxygenase Inhibition? (Hall F Poster Hall; LBP28) -  Feb 7, 2023 - Abstract #ISC2023ISC_858;    
    P=N/A
    We conducted a multi-center prospective cohort study (STRAPER study, ClinicalTrials.gov Identifier: NCT03823274; December 31, 2018-December 31, 2021) among 1,002 ischemic stroke patients to evaluate factors related to ischemic stroke recurrence after administering aspirin 100 mg and clopidogrel 75 mg for 12 weeks from the initial diagnosis. The LTB4 increase in patients having effective aspirin inhibition showed a possible mechanism that explains aspirin resistance occurred in secondary stroke prevention failure.
  • ||||||||||  Journal:  New Anti-Inflammatory β-Resorcylic Acid Lactones Derived from an Endophytic Fungus, Colletotrichum sp. (Pubmed Central) -  Jan 31, 2023   
    Mechanistically, compounds 5 and 6 significantly inhibited the protein expression of nuclear factor-κB, IκBα, IKKα/β, inducible nitric oxide synthase, and cyclooxygenase (COX)-2, whereas compound 1 only inhibited COX-2 expression. This study indicated that RAL-type compounds 1, 5, and 6 demonstrated potential anti-inflammatory activity by inhibiting the synthesis of pro-inflammatory cytokines.
  • ||||||||||  cisplatin / Generic mfg., naproxen / Generic mfg.
    Journal:  Biotinylated Pt(IV) prodrugs with elevated lipophilicity and cytotoxicity. (Pubmed Central) -  Jan 12, 2023   
    We have established that for Pt(IV) prodrugs with biotin and naproxen or stearate in axial position, the lipophilicity rather than biotin receptors expression is the main factor of cytotoxicity. We also monitored the reduction speed of Pt(IV) prodrug 3 with naproxen and biotin in axial positions in A549 cells using XANES and demonstrated that the prodrug gradually releases cisplatin within 20 hours of incubation.
  • ||||||||||  aspirin / Generic mfg.
    Journal:  Non-steroidal Anti-inflammatory Drugs and Cardiovascular Risk (Pubmed Central) -  Jan 5, 2023   
    Nonselective NSAIDs with a long half-life time are characterized by relatively stable plasma levels and thus a relatively stable platelet inhibition. Non-selective NSAIDs may additionally inhibit acetylsalicylic acid, which negatively affects its effect on platelet inhibition.
  • ||||||||||  Journal:  Carborane Analogues of Fenoprofen Exhibit Improved Antitumor Activity. (Pubmed Central) -  Dec 31, 2022   
    Furthermore, NSAIDs have shown promising cytotoxic properties. The structural modification of fenoprofen using bulky dicarba-closo-dodecaborane(12) (carborane) clusters and the biological evaluation of the carborane analogues for COX inhibition and antitumor potential showed that the carborane analogues exhibit stronger antitumor potential compared to their respective aryl-based compounds.
  • ||||||||||  Biomarker, Review, Journal:  Targeting cancer-related inflammation with non-steroidal anti-inflammatory drugs: Perspectives in pharmacogenomics. (Pubmed Central) -  Dec 23, 2022   
    Hence, a more comprehensive understanding in pharmacogenomic characteristics of NSAIDs and cancer-related inflammation would provide new insights into this appealing strategy. In this review, the up-to-date advances in clinical and experimental researches targeting cancer-related inflammation with NSAIDs are presented, and the potential of pharmacogenomics are discussed as well.
  • ||||||||||  indomethacin / Generic mfg.
    Journal:  Assessing the pyrogenicity of whole influenza virus particle vaccine in cynomolgus macaques. (Pubmed Central) -  Dec 18, 2022   
    Since WPV-induced fever was blunted by pretreatment with indomethacin (a cyclooxygenase inhibitor), the febrile response by WPV is considered to depend on the increase in prostaglandins synthesized by cyclooxygenase...Notably, sufficient antibody responses were acquired by half the amount of WPV without causing fever, suggesting that excessive immune responses to trigger the febrile response is not required for acquired immunity induction. Thus, we propose that WPV with a reduced antigen dose should be evaluated for potential clinical usage, especially in naïve populations.
  • ||||||||||  aspirin / Generic mfg.
    Journal:  Synthesis of new ester derivatives of salicylic acid and evaluation of their COX inhibitory potential. (Pubmed Central) -  Dec 16, 2022   
    In docking studies, the strongest inhibitor among the compounds synthesized was predicted to be MEST1, with the lowest binding energy. Docking studies revealed that MEST1 extends from the hydrophobic channel to the top of the cyclooxygenase active site, forming various interactions with residues in the binding pocket.
  • ||||||||||  meloxicam / Generic mfg.
    Review, Journal:  Meloxicam in Combating Clinical Mastitis: Nanotechnology-Driven Hope and Opportunities. (Pubmed Central) -  Dec 13, 2022   
    Therefore, in this review, we have highlighted the mechanism, biopharmaceutical challenges, and merits of meloxicam usage in dairy cattle mastitis. In addition, we also presented the integration of artificial neural network, in silico docking, and nanotechnology-driven topical drug delivery cargo as future opportunity for efficient delivery of meloxicam in the management of clinical mastitis.
  • ||||||||||  aspirin / Generic mfg.
    Journal:  C-Phycocyanin and Lycium barbarum Polysaccharides Protect against Aspirin-Induced Inflammation and Apoptosis in Gastric RGM-1 Cells. (Pubmed Central) -  Dec 12, 2022   
    Aspirin elevated nuclear factor-κB (NF-κB), extracellular signal-regulated kinase (ERK), p38, and c-Jun N-terminal kinase (JNK) activation, while CPC and/or LBP increased IL-10, and attenuated proinflammatory markers, Bax protein, NF-κB, and the activation of ERK and JNK. Therefore, CPC and/or LBP possess anti-inflammation by restraining the activation of the ERK signaling pathway, and LBP decreases apoptosis by suppressing the JNK signaling pathway activation in gastric RGM-1 cells with aspirin-induced epithelial damage.
  • ||||||||||  Preclinical, Journal:  Sex hormones and vascular reactivity: a temporal evaluation in resistance arteries of male rats. (Pubmed Central) -  Dec 9, 2022   
    Besides functional impairment, 18w animals showed morphological differences in third-order mesenteric arteries compared with the other groups. Our data show that time-dependent exposure to male sex hormones appears to play an important role in the development of vascular changes that can lead to impaired vascular reactivity in mesenteric arteries, which could be related to the onset of age-related cardiovascular changes in males.
  • ||||||||||  indomethacin / Generic mfg., celecoxib oral / Generic mfg.
    Preclinical, Journal:  Role of cyclooxygenase pathways in bowel fibrotic remodelling in a murine model of experimental colitis. (Pubmed Central) -  Dec 9, 2022   
    Colonic fibrosis is associated with altered bowel motility and induction of profibrotic factors driven by TGF-β signalling. COX-1 and COX-2 inhibition counteracts this fibrotic remodelling by the modulation of TGF-β/SMAD signalling, mainly via SMAD6 induction and reduction in SMAD2 phosphorylation.