- |||||||||| ibuprofen / Generic mfg.
Review, Journal, Adverse events: Redesigning Ibuprofen for Improved Oral Delivery and Reduced Side Effects. (Pubmed Central) - May 21, 2025
Therefore, ongoing research is performed to improve the IBP's activity and treatment outcome, and one way to achieve such improvements is through reducing IBP's toxicity by designing less harmful but still effective novel IBP conjugates. The aim of this review is to summarize the latest achievements with IBP conjugation techniques that created such valuable IBP formulations less toxic than but as effective as the parent drug.
- |||||||||| Journal, Adverse events: Discovery of Safe COX-2 Inhibitors: Achieving Reduced Colitis Side Effects through Balanced COX Inhibition. (Pubmed Central) - May 21, 2025
The aim of this review is to summarize the latest achievements with IBP conjugation techniques that created such valuable IBP formulations less toxic than but as effective as the parent drug. As part of our ongoing research into the discovering novel and safer COX-2 inhibitors, we reported herein a highly potent and balanced COX-2 inhibitor 21d (IC50 value = 1.35
- |||||||||| nitroprusside / Generic mfg.
The role of CD38 in age-related vascular dysfunction: a sex-dependent factor (Station 11(Research Gateway)) - May 15, 2025 - Abstract #ESCWCC2025ESC_WCC_5253;
Moreover, CD38 inhibition alleviates age-dependent vascular dysfunction, at least in part, through enhanced eNOS activation. Therefore, targeting CD38 may be considered a potential therapeutic avenue in delaying vascular aging.
- |||||||||| aspirin / Generic mfg.
Clinical, Journal: Low-dose ASA therapy does not alter core or skin temperature during hot-dry or warm-humid heat stress (PSU HEAT project). (Pubmed Central) - May 12, 2025
Nearly 40% of US adults over the age of 50 use aspirin (ASA) therapy for the primary or secondary prevention of cardiovascular disease...Low-dose ASA attenuated FBF and forearm vascular conductance (all p???0.04) but had no effect on Tc or Tsk in either environment. In conclusion, low-dose ASA attenuates the skin blood flow response during minimal activity heat stress in both dry and humid environments but does not alter Tc.
- |||||||||| celecoxib oral / Generic mfg.
Journal: Gross Antioxidant Capacity and Anti-Inflammatory Potential of Flavonol Oxidation Products: A Combined Experimental and Theoretical Study. (Pubmed Central) - Apr 29, 2025
Additionally, BZF-OH compounds were analyzed as potential cyclooxygenase-2 (COX-2) inhibitors through docking and molecular dynamics simulations, where BZF-Quer-OH showed binding affinities comparable to celecoxib, a selective COX-2 inhibitor...In the case of the oxidation products, only the oxidation product of rhamnetin showed a reduction in COX-2 expression compared to the LPS-treated control. Together, these results highlight that flavonol-derived oxidation products not only retain significant antioxidant capacity but may also possess anti-inflammatory properties, opening new perspectives for the development of innovative therapies targeting oxidative stress and chronic inflammation.
- |||||||||| Journal: Bioactivity of Synthesized Trifluoromethyl Thioxanthone Analogues. (Pubmed Central) - Apr 27, 2025
This study highlights the significant biological activities of trifluoromethyl thioxanthene derivatives, positioning them as promising candidates for the treatment of cancer, metabolic disorders, and inflammation. These compounds demonstrated noteworthy antioxidant and enzyme inhibition properties, warranting further in vivo studies to confirm their therapeutic efficacy.
- |||||||||| hydroquinone / Generic mfg.
Journal: Cinerols L-R, Anti-inflammatory Meroterpenoids from the Marine Sponge Dysidea cinerea. (Pubmed Central) - Apr 27, 2025
Seven new sesquiterpene hydroquinone/quinone (SQ) meroterpenoids, cinerols L-R (1-7), along with four known analogues (8-11), were identified from a marine sponge, Dysidea cinerea, collected from the shore of the Xisha Islands in the South China Sea...Furthermore, the potent inhibitory activity on inflammatory cytokines of 4 prompted us to evaluate its effect on the nuclear factor-?B (NF-?B)/mitogen-activated protein kinase (MAPK) signaling pathway, a critical pathway that contributes to the inflammatory responses. Cinerol O (4) was unveiled to inhibit cyclooxygenase-2 (COX-2) expression and the production of inflammatory cytokines via suppressing the expression of NF-?B and MAPKs in LPS-induced RAW 264.7 macrophages.
- |||||||||| ibuprofen / Generic mfg.
Review, Journal: Clinical Benefits of Ibuprofen Arginine: A Narrative Review. (Pubmed Central) - Apr 27, 2025
By addressing both the inflammatory and nociceptive components of pain, IBA offers an effective and well-tolerated alternative in multimodal pain management strategies. This review explores the clinical benefits of IBA in pain management among various clinical settings.
- |||||||||| IMC001 / Immunofoco, OKN4395 / Owkin
INVOKE: A phase 1 study of OKN4395, a first-in-class EP2/EP4/DP1 triple prostanoid receptor antagonist, in patients with advanced solid tumors. (Hall A - Posters and Exhibits; Poster Bd #: 322b) - Apr 23, 2025 - Abstract #ASCO2025ASCO_926;
P1
INVOKE (OKN-4395-121; NCT06789172) is a Ph1a/1b, first-in-human study of OKN4395 (oral, BID) as monotherapy (mono) or in combination with pembrolizumab 200mg IV 3-weekly (combo), in patients with advanced solid tumors that have evidence of COX-associated immunosuppression...Trial data, paired pre- and on-treatment biopsies, and exploratory biomarkers will be used to enhance development using advanced agentic AI systems, including a synthetic digital twin control arm. Ph1a of the study is currently recruiting in the US, UK, and Australia.
- |||||||||| minocycline / Generic mfg.
Review, Journal: The (neuro)inflammatory system in anxiety disorders and PTSD: Potential treatment targets. (Pubmed Central) - Apr 13, 2025
Although exact identification of such immune subtypes of anxiety disorders and PTSD is still challenging, these patients will likely particularly benefit from therapeutic targeting of aspects of the inflammatory system. Different anti-inflammatory treatment approaches (microglia-directed treatments, pro-inflammatory cytokine inhibitors, COX-inhibitors, phytochemicals and a number of novel anti-inflammatory agents) have indeed shown some efficacy even in non-stratified anxiety patient groups and appear promising as novel alternative or complimentary therapeutic options in specific ("inflammatory") subtypes of anxiety disorder and PTSD patients.
- |||||||||| Journal: Unveiling a novel pyrazolopyrimidine scaffold as a dual COX-2/5-LOX inhibitor with immunomodulatory potential: Design, synthesis, target prediction, anti-inflammatory activity, and ADME-T with docking simulation. (Pubmed Central) - Apr 12, 2025
Different anti-inflammatory treatment approaches (microglia-directed treatments, pro-inflammatory cytokine inhibitors, COX-inhibitors, phytochemicals and a number of novel anti-inflammatory agents) have indeed shown some efficacy even in non-stratified anxiety patient groups and appear promising as novel alternative or complimentary therapeutic options in specific ("inflammatory") subtypes of anxiety disorder and PTSD patients. In this study, novel pyrazolo[1,5-a]pyrimidine derivatives were synthesized, developed, and screened for their ability to inhibit the cyclooxygenase-2 enzyme in vitro, with comparisons made to the established inhibitors Celecoxib and Meloxicam...Moreover, compound 5a exhibited 86
- |||||||||| flurbiprofen / Generic mfg., ibuprofen / Generic mfg., naproxen / Generic mfg.
Preclinical, Journal: Ibuprofen, Flurbiprofen or Naproxen Sodium Minimally Influences Musculoskeletal Adaptations to Treadmill Exercise in Rats. (Pubmed Central) - Apr 11, 2025
In this study, novel pyrazolo[1,5-a]pyrimidine derivatives were synthesized, developed, and screened for their ability to inhibit the cyclooxygenase-2 enzyme in vitro, with comparisons made to the established inhibitors Celecoxib and Meloxicam...Moreover, compound 5a exhibited 86 NSAIDs did not have a strong negative or positive effect on musculoskeletal adaptations to 6?weeks of treadmill running in young healthy male rodents.
- |||||||||| montelukast / Generic mfg., aspirin / Generic mfg., indomethacin / Generic mfg.
NSAIDs administration promotes allergic sensitization by altering the production of lipid mediators (Carron 1) - Mar 26, 2025 - Abstract #EAACI2025EAACI_577;
Method Balb/c mice were treated with either of two types of NSAIDs, aspirin (200 mg/L) or indomethacin (10 mg/L), in drinking water for 2 weeks...Administration of montelukast (16 mg/kg), a LTC 4 receptor inhibitor, suppressed aspirin-induced increase of sIgE level and aggravation of body temperature drop...Conclusion Our study revealed that NSAIDs administration promoted infiltration of mast cells and ILC2s in gastric mucosa. NSAIDS administration increased the level of LTC 4 and PGD 2 in gastric mucosa, which subsequently promoted antigen-specific IgE production via their receptors.
- |||||||||| indomethacin / Generic mfg.
Indomethacin in Arginine Vasopressin Deficiency () - Mar 13, 2025 - Abstract #NKFSCM2025NKF_SCM_673;
Although our patient had AVP-D , the response to adding indomethacin to DDAVP was similar, as it improved the effect of DDAVP on the collecting duct, as in AVP-R. Thus, it could be used as an adjunct medication in AVP-D with suboptimal response to DDAVP despite its ability to reduce urine output only by 25-50%.Conclusion The patient's recovery underscores the importance of individualized therapy and suggests that COX inhibitors can be valuable in cases with suboptimal DDAVP response.
- |||||||||| Biomarker, Journal: Role of arachidonic acid metabolism in osteosarcoma prognosis by integrating WGCNA and bioinformatics analysis. (Pubmed Central) - Mar 13, 2025
The study suggested that a high level of AAMRGs might serve as a biomarker for poor prognosis in osteosarcoma and offers a potential explanation for the role of cyclooxygenase inhibitors in cancer. The five biomarkers (CD36, CLDN11, EPYC, PANX3, and STOM) were screened to construct an AAMRGs risk model with prognostic value, providing a new reference for the prognosis and treatment of osteosarcoma.
- |||||||||| Journal, PD(L)-1 Biomarker, IO biomarker: Effect of perioperative analgesia on immunity in lung cancer. (Pubmed Central) - Mar 10, 2025
Furthermore, COX inhibitors are found to improve the efficacy of the immune checkpoint inhibitor anti-PD-L1. These results underscore the influence of perioperative COX inhibitors on tumor immunity and suggest potential new strategies for optimizing tumor immunotherapy.
- |||||||||| BLOOD-BRAIN BARRIER DYSFUNCTION IN ALZHEIMER (Hall C) - Mar 10, 2025 - Abstract #ADPD2025ADPD_786;
Using two ADxEpi rodent models (mouse and rat), we further show that LOX/COX inhibitors combined with a ROS scavenger attenuate barrier dysfunction in vivo. Conclusions Based on our data, we conclude that blocking A?/glutamate signaling by inhibiting NOX/LOX/COX repairs barrier dysfunction and has the potential to help reduce seizure burden and slow cognitive decline in AD with epilepsy.
- |||||||||| metformin / Generic mfg., ursodeoxycholic acid / Generic mfg.
SAFETY AND EFFICACY OF CHEMOPREVENTION FOR FAMILIAL ADENOMATOUS POLYPOSIS: A SYSTEMATIC REVIEW AND META-ANALYSIS (10 - SDCC) - Mar 8, 2025 - Abstract #DDW2025DDW_7688;
Metformin, ursodeoxycholic acid, non-selective COX inhibitors, and COX-2-specific inhibitors were the main drugs evaluated. These findings suggest that pharmacological interventions, particularly non-selective COX inhibitors, are associated with a reduction in polyp number, burden, and size, with a favorable safety profile.
- |||||||||| Journal: A One Stone Three Birds Paradigm of Photon-Driven Pyroptosis Dye for Amplifying Tumor Immunotherapy. (Pubmed Central) - Mar 6, 2025
This conjugate, with its highly precise ER imaging, embodies a trifunctional strategy: i) innovating an electron transfer mechanism, converting the hemicyanine moiety into an oxygen-independent type I photosensitizer, thereby navigating around the hypoxia constraints of traditional PDT; ii) executing precise ER-targeted PDT, amplifying caspase-1/GSDMD-mediated pyroptosis for ICD; 3) attenuating immunosuppressive pathways by inhibiting cyclooxygenase-2 downstream factors, including HIF-1?, PGE2, and VEGF. Indo-Cy's multimodal approach potently induces in vivo tumor pyroptosis and bolsters antitumor immunity, underscoring cyclooxygenase-2-targeted dyes' potential as a versatile oncotherapeutics.
- |||||||||| Visudyne (verteporfin) / Novartis
Journal: A Self-Amplifying Photodynamic Biomedicine for Cascade Immune Activation Against Triple-Negative Breast Cancer. (Pubmed Central) - Mar 4, 2025
Notably, the self-amplifying photodynamic biomedicine significantly inhibited primary tumors, distal tumors, lung metastases, and post-operative recurrence while maintaining high biocompatibility. To sum up, the work provides a viable cascade stimulation approach and an efficient biomedical nanoplatform, offering a novel strategy for photodynamic immunotherapy of TNBC in the clinic.
- |||||||||| ketorolac / Generic mfg.
Journal: Oral Contraceptive Pill Phase Alters Mechanisms Contributing to Cutaneous Microvascular Function in Response to Local Heating. (Pubmed Central) - Mar 3, 2025
Endothelium-dependent dilation was assessed in the cutaneous microvasculature via local heating at four intradermal microdialysis sites treated with: 1) lactated Ringer's (control), 2) 10 mM ketorolac (Keto, COX inhibitor), 3) 50 mM tetraethylammonium (TEA, calcium-activated potassium channel inhibitor), and 4) 10 mM ketorolac + 50 mM TEA (Keto + TEA)...Within-participant differences between control and Keto sites support a phase-dependent restraint of NO activity via COX pathways (p=0.01). These findings demonstrate that the OCP phase affects underlying mechanistic pathways contributing to cutaneous microvascular endothelial function.
- |||||||||| Preclinical, Journal: In Vitro COX Inhibitory Activity, LC-MS Analysis and Molecular Docking Study of Silene vulgaris and Stellaria media. (Pubmed Central) - Mar 1, 2025
Also, the availability of chrysin in HFSM and rhamnetin in HFSV exhibited good docking scores i.e., 115.092, and 112.341 with a selective affinity towards COX-2. The findings of in-vitro COX Inhibitory Activity and molecular docking studies highlighted the impressive anti-inflammatory properties of S. vulgaris and S. media, and require further investigations to establish them as therapeutic candidates in the management of inflammation and related issues.
- |||||||||| ibuprofen / Generic mfg.
Preclinical, Journal: Prostaglandin D2 delays CD8+ T-cell responses and respiratory syncytial virus clearance in geriatric cotton rats. (Pubmed Central) - Feb 25, 2025
Treatment with the cyclooxygenase (COX) inhibitor ibuprofen restores RSV clearance, indicating that inflammation contributes to impaired clearance in geriatric cotton rats...We show that inhibiting this inflammatory pathway in geriatric cotton rats improves immune parameters and speeds clearance of RSV. These results contribute to our understanding of delayed RSV clearance in elderly individuals with possible applications for improving immune responses to RSV in clinical settings.
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