ethacrynic acid / Generic mfg. 
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  • ||||||||||  Review, Journal:  Drugs for hypertension. (Pubmed Central) -  May 21, 2024   
    This work presents a promising strategy to enhance the efficacy of CHL in cancer therapy. No abstract available
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Review, Journal:  Pt(IV) Complexes in the Search for Novel Platinum Prodrugs with Promising Activity. (Pubmed Central) -  Feb 24, 2024   
    We have discussed the structure activity relationship (SAR) and the effects of the ligands on the biological activity of Pt(IV) complexes with cisplatin, oxaliplatin, carboplatin and the Pt core other than approved drugs. This literature work will help researchers to get an idea about Pt(IV) complexes that have been classified based on the aspects of their biological activity.
  • ||||||||||  furosemide / Generic mfg., bumetanide / Generic mfg.
    Sulfonamide Drug Reactions: Evidence for Limited Cross-Reactivity Between Furosemide and Bumetanide () -  Feb 20, 2024 - Abstract #AAD2024AAD_3316;    
    This is consistent with the literature which demonstrates minimal cross reactivity between classes of sulfa-containing drugs. Additionally, data analysis revealed the need for more specific and consistent coding measures in patients diagnosed with cutaneous drug eruptions.
  • ||||||||||  ethacrynic acid / Generic mfg.
    Preclinical, Journal:  Association between GSTP1 I105V polymorphisms and responses to GSTP1 inhibitor treatment: in silico and in (Pubmed Central) -  Jan 30, 2024   
    In this study, a silico model of GSTP1 I105V polymorphism was successfully established to predict the changes of binding model and binding affinity between GSTP1 I105(WT) or GSTP1 V105 and ethacrynic acid via molecular docking and molecular dynamics, and ultimately further evaluated for its anticancer effects...In summary, this study provides the first evidence that the GSTP1 I105V polymorphism may impact cancer cell sensitivity to its inhibitor through theoretical prediction. Furthermore, a comprehensive understanding of the correlation between GSTP1 I105V polymorphisms and responses to GSTP1 inhibitor treatment would offer valuable insights for future drug development targeting GSTP1 in cancer-related diseases.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  Henletor (torsemide) / Orchid
    Review, Journal:  Diuretic Strategies in Acute Decompensated Heart Failure: A Narrative Review. (Pubmed Central) -  Jan 11, 2024   
    PubMed, OVID, and Embase databases were searched from inception to December 22, 2022, with the following search terms: heart failure, acute heart failure, decompensated heart failure, furosemide, bumetanide, ethacrynic acid, hydrochlorothiazide, indapamide, metolazone, chlorthalidone, spironolactone, eplerenone, and acetazolamide...Trials involving torsemide, chlorothiazide, and tolvaptan were excluded...Heart failure with congestion can be managed with careful administration of high-dose loop diuretics, supported by thiazides and acetazolamide when necessary. Clinical trials are underway to further evaluate this strategy.
  • ||||||||||  ethacrynic acid / Generic mfg.
    Journal:  2(3H)-Dihydrofranolactone metabolites from Pleosporales sp. NUH322 as anti-amyotrophic lateral sclerosis drugs. (Pubmed Central) -  Oct 7, 2023   
    NUH322 culture media, and their protective activity against the excitotoxicity of ?-N-oxalyl-L-?,?-diaminopropionic acid (ODAP), an ?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamatergic agonist, was evaluated under low mitochondrial glutathione levels induced by ethacrynic acid (EA) and low sulfur amino acids using our developed ODAP-EA assay...The latter treatment significantly extended their lifespan (p?=?0.03) and delayed motor deterioration (p?=?0.001-0.01). Our result
  • ||||||||||  ethacrynic acid / Generic mfg.
    Journal:  A Switch-On Affinity-Based Iridium(III) Conjugate Probe for Imaging Mitochondrial Glutathione S-Transferase in Breast Cancer Cells. (Pubmed Central) -  Sep 26, 2023   
    Herein, we report a highly selective affinity-based luminescence probe 1 for GST in breast cancer cells through tethering a GST inhibitor, ethacrynic acid, to an iridium(III) complex...To the best of our knowledge, this probe is the first affinity-based iridium(III) imaging probe for the subcellular GST. Our work provides a valuable tool for unmasking the diverse roles of a subcellular GST in living systems, as well as for studying the heterogeneity of breast cancers.
  • ||||||||||  ethacrynic acid / Generic mfg., furosemide / Generic mfg., bumetanide / Generic mfg.
    Journal:  Role of Monovalent Ions in the NKCC1 Inhibition Mechanism Revealed through Molecular Simulations. (Pubmed Central) -  Dec 12, 2022   
    Consistent with experimental evidence, all drugs take advantage of the K/Na ions, which plastically respond to their binding. This study not only provides atomic-level insights useful for drug discovery campaigns of more selective/potent NKCC1 inhibitors aimed to tackle diseases related to deregulated Cl homeostasis, but it also supplies a paradigmatic example of the key importance of dynamical effects when drug binding is mediated by monovalent ions.
  • ||||||||||  Journal:  Anticancer ruthenium(II) tris(pyrazolyl)methane complexes with bioactive co-ligands. (Pubmed Central) -  Nov 18, 2022   
    The {Ru-tpm-PPh} assembly is stable in DO and in biological medium (DMEM) at 37 °C, with a tendency to slowly dissociate the pyridine ligand. The antiproliferative activity of the complexes was assessed on the cancerous A2780 and A2780cisR cell lines, and the nontumoral HEK 293T cell line; moreover inhibition assays were carried out on the complexes towards COX-2 and GSTP1 enzymes.
  • ||||||||||  Loop Diuretic-Induced Pancreatitis (Crown Ballroom) -  Sep 4, 2022 - Abstract #ACG2022ACG_3806;    
    Her medications included Prednisone, Plaquenil, and Eliquis...Bumetanide was held and later switched to ethacrynic acid with the resolution of symptoms...Nevertheless, our patient developed AP only with furosemide and bumetanide, indicating an added immune-mediated pathway involving sulfa metabolites likely contributing to AP, which also has been reported in the literature. Figure: CT abdomen from the time of initial ED presentation demonstrating edematous pancreas with minimal surrounding fat stranding and fluid in the region of the head and uncinate process, consistent with acute interstitial pancreatitis.
  • ||||||||||  ethacrynic acid / Generic mfg.
    Ethacrynic Acid-Associated Seronegative Enteropathy (Crown Ballroom) -  Sep 4, 2022 - Abstract #ACG2022ACG_1607;    
    Incorrect interpretation of the duodenal biopsies could have led to a misdiagnosis of CeD and an unnecessary gluten free diet. Figure: Figure 1: A: Duodenal biopsies showing villous blunting (H&E stain,100x magnification); B: Duodenal biopsies with arrows pointing to increased intraepithelial lymphocytes (H&E stain, 400x magnification)
  • ||||||||||  ethacrynic acid / Generic mfg.
    Journal:  Ethacrynic acid is an inhibitor of human factor XIIIa. (Pubmed Central) -  Jun 4, 2022   
    Phylogenetic tree confirms that BaGST2 belongs to the sigma class of GSTs superfamily. Overall, our studies indicate that EA inhibits the physiological function of human FXIIIa in vitro which may potentially contribute to the bleeding complications that were reported with the association of the parenteral administration of EA.
  • ||||||||||  veverimer (TRC101) / Tricida
    Journal:  Assessment of the Potential for Veverimer Drug-Drug Interactions. (Pubmed Central) -  Feb 16, 2022   
    The clinical relevance of in vitro binding and the transient increase in gastric pH was evaluated in human DDI studies using two drugs with the most binding to veverimer (furosemide, aspirin) and two additional drugs with pH-dependent solubility effecting absorption (dabigatran, warfarin)...The potential for DDIs with veverimer was evaluated based on the known site of action and physicochemical structure of the polymer, which restricts the compound to the gastrointestinal tract. Based on the findings from in vitro and human studies, we conclude that veverimer is unlikely to have clinically significant DDIs.
  • ||||||||||  ethacrynic acid / Generic mfg.
    Preclinical, Journal:  The Mechanism of N-acetyl-L-cysteine in Improving the Secretion of Porcine Follicle-Stimulating Hormone in Pichia pastoris. (Pubmed Central) -  Jan 28, 2022   
    These results indicated that NAC improved the secretion of HSA-pFSHβ by increasing the intracellular GSH content through its thiol activity rather than as a precursor for GSH synthesis. In conclusion, our results demonstrate, for the first time, that the secretion of recombinant HSA-pFSHβ in Pichia pastoris could be improved through thiol-reducing agent supplementation, and the mechanism of the effect NAC has on HSA-pFSHβ secretion is associated with improving the intracellular GSH content.
  • ||||||||||  ethacrynic acid / Generic mfg.
    Journal:  Ethacrynic acid targets GSTM1 to ameliorate obesity by promoting browning of white adipocytes. (Pubmed Central) -  Jan 18, 2022   
    In conclusion, our results demonstrate, for the first time, that the secretion of recombinant HSA-pFSHβ in Pichia pastoris could be improved through thiol-reducing agent supplementation, and the mechanism of the effect NAC has on HSA-pFSHβ secretion is associated with improving the intracellular GSH content. No abstract available
  • ||||||||||  Gilotrif (afatinib) / Boehringer Ingelheim
    Journal:  Ethacrynic Acid Enhances the Antitumor Effects of Afatinib in EGFR/T790M-Mutated NSCLC by Inhibiting WNT/Beta-Catenin Pathway Activation. (Pubmed Central) -  Dec 16, 2021   
    Our functional studies found that the antitumor mechanisms of afatinib when combined with EA mainly occurred by inhibiting WNT/β-catenin pathway activation and suppression of the secretion of anti-inflammatory factors. These results revealed that combination of afatinib with EA derivatives not only provided a new therapeutic approach for EGFR/T790M-mutated NSCLC patients but also offered a new idea for developing new drugs or optimizing the dose of afatinib in clinical use in future antitumor therapy.
  • ||||||||||  bumetanide / Generic mfg.
    Journal:  Loop Diuretics Inhibit Ischemia-Induced Intracellular Ca Overload in Neurons via the Inhibition of Voltage-Gated Ca and Na Channels. (Pubmed Central) -  Oct 5, 2021   
    Data suggest that loop diuretics effectively inhibit voltage-gated Ca and Na channels at clinically relevant concentrations, and block of these channels by these compounds likely contributes to their clinical effects. Importantly, inhibition of these channels, and not NKCC1, by loop diuretics reduces [Ca] overload in neurons during ischemia-acidosis, and thus BMN and EA could potentially be used therapeutically to lessen injury following ischemic stroke.
  • ||||||||||  ethacrynic acid / Generic mfg.
    Journal:  Marmoset glutathione transferases with ketosteroid isomerase activity. (Pubmed Central) -  Jul 22, 2021   
    Two residues differ in the H-site of the 91.4% sequence identical CjaGST A1-1 and CjaGST A3-3, and modeling of the structures suggests that the bulky phenyl ring of Phe111 in CjaGST A1-1 causes steric hindrance in the binding of the steroid substrate. Tributyltin acetate (IC=0.16 ± 0.004 μM) and ethacrynic acid (IC=3.3 ± 0.2 μM) were found to be potent inhibitors of CjaGST A3-3, as previously demonstrated with the human and equine orthologs.
  • ||||||||||  acetazolamide / Generic mfg., cyclosporine / Generic mfg.
    Clinical, Journal:  Acetazolamide-Associated Acute Kidney Injury in Critically Ill Pediatric Patients. (Pubmed Central) -  Jul 10, 2021   
    Synergic effects provided by specific combinations of metal and bioactive fragments were identified, pointing toward an optimal ethacrynic acid/flurbiprofen combination for both Ru(II) and Ir(III) complexes. Acute kidney injury occurs frequently in critically ill pediatric patients receiving intravenous acetazolamide.
  • ||||||||||  ethacrynic acid / Generic mfg.
    Journal:  Synthesis and Biological Evaluation of Ethacrynic Acid Derivatives Bearing Sulfonamides as Potent Anti-Cancer Agents. (Pubmed Central) -  Jun 22, 2021   
    These compounds displayed IC values in nanomolar range against A549, MCF7, PC3 and HCT116 cell lines, deducing the discovery that piperazine or 4-aminopiperidine is the linker's best choice to develop EA analogs with highly potent anti-proliferative activities own up to 24 nM. Besides, in terms of selectivity, those linkers are more suitable offering safety ratios of up to 63.8.
  • ||||||||||  Trial completion, Enrollment change:  ACEI or ARB and COVID-19 Severity and Mortality in US Veterans (clinicaltrials.gov) -  Apr 28, 2021   
    P=N/A,  N=22213, Completed, 
    Standardised, validated endpoints and pragmatic trial designs may allow investigators to determine the optimal diuretic, timing of initiation, dose, and interval to improve post-operative outcomes. Active, not recruiting --> Completed | N=10000 --> 22213