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DRUG CLASS:

Cholesterol absorption inhibitor

15d
Ezetimibe Normalizes Dietary Cholesterol-Induced Exacerbation of Liver Injury in Alcohol-Fed Mice. (PubMed, Biomolecules)
Moreover, mice fed a diet containing both cholesterol and alcohol exhibited increased expression of monocyte chemoattractant protein 1 (Mcp1) and tumor necrosis factor alpha (Tnfα) in the distal small intestine. Collectively, our findings indicate that ezetimibe effectively mitigates the adverse effects of dietary cholesterol and alcohol consumption on hepatic lipid accumulation and liver injury.
Preclinical • Journal
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TNFA (Tumor Necrosis Factor-Alpha) • CCL2 (Chemokine (C-C motif) ligand 2)
20d
Investigation of the nitric oxide signaling pathway induced by ezetimibe on renal injury in streptozotocin-induced diabetic rat: role of anti-oxidative and anti-inflammatory effects. (PubMed, Immunopharmacol Immunotoxicol)
Sixty rats were used in the study, divided into the following groups: a control group (healthy rats), a diabetic control group, a diabetic group treated with metformin, a diabetic group treated with ezetimibe, a diabetic group treated with ezetimibe plus L-NAME, and a diabetic group treated with ezetimibe plus L-arginine. However, the beneficial effects of ezetimibe were reversed by L-NAME. Ezetimibe protected the kidney against diabetic injury mainly by activating the nitric oxide signaling pathway, enhancing antioxidant enzyme activity, and reducing inflammation, suggesting that its nephroprotective effects are NO-dependent.
Preclinical • Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • CAT (Catalase)
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metformin
1m
Moderate-Intensity Statin Plus Ezetimibe in CKD and ASCVD (clinicaltrials.gov)
P=N/A, N=1952, Not yet recruiting, Yonsei University
New trial
1m
The SCD1 inhibitor aramchol interacts with regorafenib and metformin to kill tumor cells. (PubMed, Oncotarget)
Knock down of SCD1 enhanced the percentage of dead cells in vehicle control treated cells but did not alter the abilities of drugs to kill tumor cells. Our data demonstrates that UM cells are killed by treatment with aramchol plus regorafenib plus metformin via enhanced autophagic flux and that this combination may have the potential to control UM tumors that have metastasized to the liver.
Journal
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ATG5 (Autophagy Related 5) • BECN1 (Beclin 1) • LAMP2 (Lysosomal Associated Membrane Protein 2) • SCD (Stearoyl-CoA Desaturase)
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Stivarga (regorafenib) • metformin • Aramchol (aramchol meglumine)
2ms
Enrollment closed
2ms
Single and Multiple Dose Pharmacokinetics (PK) of Aramchol From an Aramchol Meglumine Tablet (clinicaltrials.gov)
P1, N=32, Recruiting, Galmed Pharmaceuticals Ltd | Not yet recruiting --> Recruiting
Enrollment open
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Aramchol (aramchol meglumine)
2ms
Ezetimibe counteracts lipopolysaccharide-induced liver injury in mice via modulating TLR4-mediated MYD88/TRAF-6/NF-kB signaling pathway. (PubMed, Toxicol Appl Pharmacol)
Additionally, myeloid differentiation primary-response protein 88 (MYD88), TNF Receptor Associated Factor 6 (TRAF-6) and IL-6 were markedly reduced in the liver by EZE. Collectively, EZE may be a promising candidate in sepsis-related liver injury following further clinical studies.
Preclinical • Journal • IO biomarker
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MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • NFKB1 (Nuclear factor of kappa light polypeptide gene enhancer in B-cells 1) • TLR4 (Toll Like Receptor 4) • TRAF6 (TNF Receptor Associated Factor 6)
3ms
New trial