Chemically Modified Variants of Fenofibrate with Antiglioblastoma Potential.
Abstract
Anticancer effects of a common lipid-lowering drug, fenofibrate, have been described in the literature for a quite some time; however, fenofibrate has not been used as a direct anticancer therapy. We have previously reported that fenofibrate in its unprocessed form (ester) accumulates in the mitochondria, inhibits mitochondrial respiration, and triggers a severe energy deficit and extensive glioblastoma cell death. However, fenofibrate does not cross the blood brain barrier and is quickly processed by blood and tissue esterases to form the PPARα agonist fenofibric acid, which is practically ineff...
Source: Translational Oncology - May 7, 2019 Category: Cancer & Oncology Authors: Stalinska J, Zimolag E, Pianovich NA, Zapata A, Lassak A, Rak M, Dean M, Ucar-Bilyeu D, Wyczechowska D, Culicchia F, Marrero L, Del Valle L, Sarkaria J, Peruzzi F, Jursic BS, Reiss K Tags: Transl Oncol Source Type: research
Pharmacokinetics and bioequivalence of two fenofibrate choline formulations in healthy subjects under fed and fasted condition
.
CONCLUSION: The reference and the test formulations of 135 mg choline fenofibrate show comparable pharmacokinetic profiles of fenofibric acid under both fed and fasted conditions and are considered bioequivalent.
.
PMID: 30802201 [PubMed - as supplied by publisher] (Source: International Journal of Clinical Pharmacology and Therapeutics)
Source: International Journal of Clinical Pharmacology and Therapeutics - February 26, 2019 Category: Drugs & Pharmacology Tags: Int J Clin Pharmacol Ther Source Type: research
Expanded Table: Lipid-Lowering Drugs (online only)
Date: February 11, 2019
Issue #:
1565Summary:
View the Expanded Table: Lipid-Lowering Drugs (Source: The Medical Letter)
Source: The Medical Letter - February 1, 2019 Category: Drugs & Pharmacology Authors: admin Tags: alirocumab Altoprev Antara Atorvastatin Cholesterol Cholestyramine Colesevelam Colestid Colestipol Crestor Epanova Ezetimibe ezetimibe/simvastatin Fenofibrate Fenofibric acid Fenoglide Fibricor Fish oil Flolipid Fluva Source Type: research
Lipid-Lowering Drugs
Date: February 11, 2019
Issue #:
1565Summary:
Cholesterol management guidelines from the American
College of Cardiology/American Heart Association Task
Force have recently been published. See Table 1 for a
brief summary of their recommendations. (Source: The Medical Letter)
Source: The Medical Letter - January 8, 2019 Category: Drugs & Pharmacology Authors: admin Tags: alirocumab Altoprev Antara Atorvastatin Bezafibrate Bezalip Cholesterol Cholestyramine Colesevelam Colestid Colestipol Crestor Epanova evolucumab Ezetimibe ezetimibe/simvastatin Ezetrol Fenofibrate Fenofibric acid Fen Source Type: research
Unveiling the Important Roles of Coexisting Contaminants on Photochemical Transformations of Pharmaceuticals: Fibrate Drugs as a Case Study
In this study, the roles of coexisting contaminants on the phototransformation of pharmaceuticals were unveiled with the fibrate drugs gemfibrozil (GMF), fenofibrate (FNF), and fenofibric acid (FNFA) as model compounds. GMF undergoes initial concentration dependent photodegradation due to the involvement of singlet oxygen (1O2) initiated self-sensitized photolysis, and undergoes pH dependent photodegradation due to dissociation and hydroxyl radical (•OH) generation. The decarboxylated intermediates of GMF and coexisting FNFA significantly accelerated the photodegradation of GMF. The promotional effects of the decarboxyla...
Source: Journal of Hazardous Materials - July 12, 2018 Category: Environmental Health Source Type: research
Comparative Evaluation of Gemcabene and Peroxisome Proliferator–Activated Receptor Ligands in Transcriptional Assays of Peroxisome Proliferator–Activated Receptors: Implication for the Treatment of Hyperlipidemia and Cardiovascular Disease
Abstract:
Gemcabene, a late-stage clinical candidate, has shown efficacy for LDL-C, non-HDL cholesterol, apoB, triglycerides, and hsCRP reduction, all risk factors for cardiovascular disease. In rodents, gemcabene showed changes in targets, including apoC-III, apoA-I, peroxisomal enzymes, considered regulated through peroxisome proliferator–activated receptor (PPAR) gene activation, suggesting a PPAR-mediated mechanism of action for the observed hypolipidemic effects observed in rodents and humans. In the current study, the gemcabene agonist activity against PPAR subtypes of human, rat, and mouse were compared with kno...
Source: Journal of Cardiovascular Pharmacology - July 1, 2018 Category: Cardiology Tags: Original Article Source Type: research
Anti-inflammatory activity of anti-hyperlipidemic drug, fenofibrate, and its phase-I metabolite fenofibric acid: in silico , in vitro , and in vivo studies
Abstract
Fenofibrate, an anti-hyperlipidemic drug and its phase-I biotransformed metabolite fenofibric acid, was studied for COX-1 (PDB ID: 3N8Y) and COX-2 (PDB ID: 1PXX) inhibition potentials in silico and in vitro for their effects on human recombinant COX-2 enzyme isolated from aBaculovirus expression system in sf21 cells (EC 1.14.99.1) using a conventional spectrophotometric assay. Furthermore, the compounds were also screened for their anti-inflammatory potentials in vivo using carrageenan-induced paw oedema method in Wistar rats. The test compounds fenofibric acid, fenofibrate, and the standard drug diclofenac exh...
Source: Inflammopharmacology - December 13, 2017 Category: Drugs & Pharmacology Source Type: research
Enzymatic reactive oxygen species assay to evaluate phototoxic risk of metabolites.
Abstract
The present study aimed to verify the feasibility of an enzymatic reactive oxygen species (eROS) assay to evaluate the phototoxic risk of compounds after their metabolization. The eROS assay was designed based on the combined use of an in vitro drug metabolism system and a ROS assay. The incubation time of compounds with human hepatic S9 fractions was optimized with the use of fenofibrate (FF), a typical phototoxicant with metabolite-related phototoxicity, and the reproducibility and robustness of the eROS assay were examined using FF. The eROS assay was applied to 12 phototoxic compounds, includi...
Source: Toxicology Letters - July 8, 2017 Category: Toxicology Authors: Kato M, Ohtake H, Sato H, Seto Y, Onoue S Tags: Toxicol Lett Source Type: research
Determination of Fenofibric Acid in Rat Plasma and its Application to a Comparative Pharmacokinetic Study of JW322 and Fenofibrate
In this study, a sensitive and reliable method for the quantitation of fenofibric acid in rat plasma was developed and validated using high performance liquid chromatography (HPLC). The plasma samples were prepared by deproteinization, and sildenafil was used as an internal standard. Chromatographic separation was achieved using a reversed-phase (C18) column. The mobile phase, 0.02 M ammonium acetate buffer:acetonitrile (35:65, v/v), was run at a flow rate of 1.0 mL/min, and the column eluent was monitored using an ultraviolet detector at 280 nm at room temperature. The retention times of sildenafil (an internal stan...
Source: Drug Research - May 30, 2017 Category: Drugs & Pharmacology Authors: Kim, Tae Kon Tags: Original Article Source Type: research
The Effect of Fenofibric Acid on the Pharmacokinetics and Pharmacodynamics of Warfarin in Rats.
Abstract
1. Case reports have shown that coadministration of fenofibric acid (FA) could increase bleeding risks of warfarin, but the mechanisms remained unknown. We therefore investigated the pharmacokinetic and pharmacodynamic interaction between warfarin and FA in rats. 2. Rats received warfarin alone (2 mg/kg) or coadministered with FA (100 mg/kg). FA significantly increased the exposure to warfarin, and decreased that to 7-hydroxywarfarin in rats nearly by two-fold, meanwhile increased Cmax and prolonged t1/2 of warfarin. Anticoagulant activity significantly increased, with prothrombin time (PT) up...
Source: Xenobiotica - March 12, 2017 Category: Research Authors: Guo C, Xue S, Zheng X, Yang L, Zhao D, Chen X, Li N Tags: Xenobiotica Source Type: research
Molecules, Vol. 21, Pages 1708: Zerumbone, a Bioactive Sesquiterpene, Ameliorates Diabetes-Induced Retinal Microvascular Damage through Inhibition of Phospho-p38 Mitogen-Activated Protein Kinase and Nuclear Factor-κB Pathways
In conclusion, treatment of diabetic rats with zerumbone attenuates the severity of retinal inflammation and angiogenesis, via inhibition of p38 MAPK and NF-κB signaling pathways. These benefits of zerumbone for DR appear to be linked to its antihyperglycemic and antihyperlipidemic effects. (Source: Molecules)
Source: Molecules - December 10, 2016 Category: Chemistry Authors: Wayne Liu Thing-Fong Tzeng I-Min Liu Tags: Article Source Type: research
Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man.
Abstract
Formulating poorly water soluble drugs using ordered mesoporous silica materials is an emerging approach to tackle solubility-related bioavailability problems. The current study was conducted to assess the bioavailability-enhancing potential of ordered mesoporous silica in man. In this open-label, randomized, two-way cross-over study, 12 overnight fasted healthy volunteers received a single dose of fenofibrate formulated with ordered mesoporous silica or a marketed product based on micronized fenofibrate. Plasma concentrations of fenofibric acid, the pharmacologically active metabolite of fenofibr...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 16, 2016 Category: Drugs & Pharmacology Authors: Bukara K, Schueller L, Rosier J, Martens MA, Daems T, Verheyden L, Eelen S, Van Speybroeck M, Libanati C, Martens JA, Van Den Mooter G, Frérart F, Jolling K, De Gieter M, Bugarski B, Kiekens F Tags: Eur J Pharm Biopharm Source Type: research
C/EBP ‐β Is Differentially Affected by PPARα Agonists Fenofibric Acid and GW7647, but does not Change Apolipoprotein A‐I Production During ER‐Stress and Inflammation
This article is protected by copyright. All rights reserved (Source: Journal of Cellular Biochemistry)
Source: Journal of Cellular Biochemistry - September 11, 2016 Category: Biochemistry Authors: Sophie E. van der Krieken, Herman E. Popeijus, Maurice Konings, Stefan P.J. Dullens, Ronald P. Mensink, Jogchum Plat Tags: Article Source Type: research
A Cross-Reactivity of Fenofibric Acid With MDMA DRI Assay.
CONCLUSION: Fenofibrate's interference with MDMA immunoassay was confirmed. Fenofibrate being widely prescribed, physicians had to be alerted that this treatment could lead to false-positive results.
PMID: 27612346 [PubMed - as supplied by publisher] (Source: Military Medicine)
Source: Military Medicine - September 10, 2016 Category: Global & Universal Tags: Mil Med Source Type: research
