Synthesis and Evaluation of Fenofibric Acid Ester Derivatives: Studies of Different Formulation with Their Bioavailability and Absorption Conditions
A series of fenofibric acid ester pro-drugs (JF-1-7) were synthesized. The pharmacokinetic properties of these pro-drugs were examined after oral administration to rats at a dose of 20 mg kg-1 to evaluate the relative bioavailability in rats. The bioavailability of the ester compounds, JF-1, 2, 3, 4, 5, 6, and 7, was significantly higher than that of fenofibrate. In particular, JF-2 proved to be most promising. The oral administration (20 mg kg-1) of JF-2 showed a relative bioavailability of approximately 272.8% compared to fenofibrate. (Source: Journal of the Brazilian Chemical Society)
Source: Journal of the Brazilian Chemical Society - January 20, 2020 Category: Chemistry Source Type: research

Canonical Wnt Signaling Promotes Neovascularization through Determination of Endothelial Progenitor Cell Fate via Metabolic Profile Regulation
This study found that EPC metabolic profile is a direct determinant of EPC fate. The Wnt signaling pathway regulates EPC metabolism, EPC fate and subsequently, new vessel formation. These findings reveal a new function of Wnt signaling in regulating mitochondrial function in EPC. This study also suggests a potential significance of EPC metabolic profile as a diagnostic marker and therapeutic target for diseases caused by abnormal blood vessel formation.© AlphaMed Press 2019 (Source: Stem Cells)
Source: Stem Cells - June 24, 2019 Category: Stem Cells Authors: Yan Shao, Jianglei Chen, Willard Freeman, Li ‐jie Dong, Zhi‐hui Zhang, Manhong Xu, Fangfang Qiu, Yanhong Du, Juping Liu, Xiao‐rong Li, Jian‐xing Ma Tags: Tissue ‐Specific Stem Cells Source Type: research

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 ineffect...
Source: Translational Oncology - May 8, 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 decarbox...
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...
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 exhi...
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, including 7 pho...
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 (a...
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) ...
Source: Xenobiotica - March 13, 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 11, 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.
ens F 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 fenofibrat...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 17, 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 12, 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

In  vitro metabolism of fenofibric acid by carbonyl reducing enzymes
Publication date: 25 October 2016 Source:Chemico-Biological Interactions, Volume 258 Author(s): Petra Malátková, Matthildi Kanavi, Milan Nobilis, Vladimír Wsól Fenofibric acid is a hypolipidemic drug that is used as an active ingredient per se or is administered in the form of fenofibrate that releases fenofibric acid after absorption. The metabolism of fenofibric acid is mediated primarily by glucuronidation. However, the other part of fenofibric acid is excreted as reduced fenofibric acid. Enzymes responsible for the formation of reduced fenofibric acid as well as their subcellular localizati...
Source: Chemico Biological Interactions - September 6, 2016 Category: Biochemistry Source Type: research

Absolute oral bioavailability of fenofibric acid and choline fenofibrate in rats determined by ultra-performance liquid chromatography tandem mass spectrometry.
Abstract Choline fenofibrate is the choline salt of fenofibric acid, which releasing free fenofibric acid in the gastrointestinal tract. To estimate the absolute oral bioavailability of fenofibric acid and choline fenofibrate, a novel and sensitive UPLC-MS/MS method with liquid-liquid extraction procedure was developed for the determination of fenofibric acid in rat plasma. The separation was achieved on a Phenomenex Kinetex C18 column (50 × 2.1 mm, 2.6 µm) containing 2mM ammonium acetate-methanol with a gradient elution program. Validations of this method including specificity, sensitivi...
Source: Biomedical Chromatography : BMC - September 4, 2016 Category: Biomedical Science Authors: Wei X, Li P, Liu M, Du Y, Wang M, Zhang J, Wang J, Liu H, Liu X Tags: Biomed Chromatogr Source Type: research

In vitro metabolism of fenofibric acid by carbonyl reducing enzymes
Publication date: Available online 4 September 2016 Source:Chemico-Biological Interactions Author(s): Petra Malátková, Matthildi Kanavi, Milan Nobilis, Vladimír Wsól Fenofibric acid is a hypolipidemic drug that is used as an active ingredient per se or is administered in the form of fenofibrate that releases fenofibric acid after absorption. The metabolism of fenofibric acid is mediated primarily by glucuronidation. However, the other part of fenofibric acid is excreted as reduced fenofibric acid. Enzymes responsible for the formation of reduced fenofibric acid as well as their subcellular loca...
Source: Chemico Biological Interactions - September 4, 2016 Category: Biochemistry Source Type: research

In vitro metabolism of fenofibric acid by carbonyl reducing enzymes.
M, Wsól V Abstract Fenofibric acid is a hypolipidemic drug that is used as an active ingredient per se or is administered in the form of fenofibrate that releases fenofibric acid after absorption. The metabolism of fenofibric acid is mediated primarily by glucuronidation. However, the other part of fenofibric acid is excreted as reduced fenofibric acid. Enzymes responsible for the formation of reduced fenofibric acid as well as their subcellular localization have remained unknown until now. We have found that the predominant site of fenofibric acid reduction is the human liver cytosol, whereas liver micros...
Source: Chemico-Biological Interactions - September 3, 2016 Category: Molecular Biology Authors: Malátková P, Kanavi M, Nobilis M, Wsól V Tags: Chem Biol Interact Source Type: research

Analytical methodologies based on LC –MS/MS for monitoring selected emerging compounds in liquid and solid phases of the sewage sludge
Publication date: 2016 Source:MethodsX, Volume 3 Author(s): C. Boix, M. Ibáñez, D. Fabregat-Safont, E. Morales, L. Pastor, J.V. Sancho, J.E. Sánchez-Ramírez, F. Hernández In this work, two analytical methodologies based on liquid chromatography coupled to tandem mass spectrometry (LC–MS/MS) were developed for quantification of emerging pollutants identified in sewage sludge after a previous wide-scope screening. The target list included 13 emerging contaminants (EC): thiabendazole, acesulfame, fenofibric acid, valsartan, irbesartan, salicylic acid, diclofenac, carbamazepin...
Source: MethodsX - July 21, 2016 Category: Science Source Type: research

Fenofibrate improves high-fat diet-induced and palmitate-induced endoplasmic reticulum stress and inflammation in skeletal muscle
Publication date: Available online 11 June 2016 Source:Life Sciences Author(s): Fang Dai, Tian Jiang, Ying-ying Bao, Guan-jun Chen, Li Chen, Qiu Zhang, Yun-xia Lu Aims Fenofibrate (FF) is commonly used clinically as a lipid-lowering drug, but whether it participates in endoplasmic reticulum (ER) stress and decreases inflammation in skeletal muscle is still unknown. The aim of this study is to determine whether FF treatment reduces insulin resistance (IR) by alleviating ER stress and downstream inflammation in skeletal muscle tissues and cells. Main methods Female SD rats were randomly divided into groups receivin...
Source: Life Sciences - June 11, 2016 Category: Biology Source Type: research

Comparisons of Pharmacokinetics and NO-releasing of Nitrofibriate and Fenofibrate after Oral Administration in Rats.
This study showed that nitrofibriate, as nitric oxide donor, could slowly release NO in vivo. This study provided biopharmaceutical basis for further study of nitrofibriate. This article is protected by copyright. All rights reserved. PMID: 27270950 [PubMed - as supplied by publisher] (Source: Biomedical Chromatography : BMC)
Source: Biomedical Chromatography : BMC - June 6, 2016 Category: Biomedical Science Authors: Yang Y, Cheng Q, Liu X, Liu Z, Li T, Jiang X, Wang L Tags: Biomed Chromatogr Source Type: research

Development and Validation of Bioanalytical UHPLC-UV Method for Simultaneous Analysis of Unchanged Fenofibrate and Its Metabolite Fenofibric Acid in Rat Plasma: Application to Pharmacokinetics
Publication date: Available online 26 May 2016 Source:Saudi Pharmaceutical Journal Author(s): Rayan G. Alamri, Kazi Mohsin, Ajaz Ahmad, Mohammad Raish, Fars K. Alanazi A simple, precise, selective and fast ultra-high performance liquid chromatography (UHPLC-UV) method has been developed and validated for the simultaneous determination of a lipid regulating agent fenofibrate and its metabolite fenofibric acid in rat plasma. The chromatographic separation was carried out on a reversed-phase Acquity® BEH C18 column using methanol-water (65:35, v/v) as the mobile phase. The isocratic flow was 0.3 ml/min with rapid r...
Source: Saudi Pharmaceutical Journal - May 27, 2016 Category: Drugs & Pharmacology Source Type: research

Analytical methodologies based on LC–MS/MS for monitoring selected emerging compounds in liquid and solid phases of the sewage sludge
Publication date: Available online 27 April 2016 Source:MethodsX Author(s): C. Boix, M. Ibáñez, D. Fabregat-Safont, E. Morales, L. Pastor, J.V. Sancho, J.E. Sánchez-Ramírez, F. Hernández In this work, two analytical methodologies based on liquid chromatography coupled to tandem mass spectrometry (LC–MS/MS) were developed for quantification of emerging pollutants identified in sewage sludge after a previous wide-scope screening. The target list included 13 emerging contaminants (EC): thiabendazole, acesulfame, fenofibric acid, valsartan, irbesartan, salicylic acid, diclofen...
Source: MethodsX - April 30, 2016 Category: Science Source Type: research

Analytical methodologies based on LC-MS/MS for monitoring selected emerging compounds in liquid and solid phases of the sewage sludge
Publication date: Available online 27 April 2016 Source:MethodsX Author(s): C. Boix, M. Ibáñez, D. Fabregat-Safont, E. Morales, L. Pastor, J.V. Sancho, J.E. Sánchez-Ramírez, F. Hernández In this work, two analytical methodologies based on liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) were developed for quantification of emerging pollutants identified in sewage sludge after a previous wide-scope screening. The target list included 13 emerging contaminants (EC): thiabendazole, acesulfame, fenofibric acid, valsartan, irbesartan, salicylic acid, diclofenac, ca...
Source: MethodsX - April 28, 2016 Category: Science Source Type: research

Effect of magnesium carbonate on the solubility, dissolution and oral bioavailability of fenofibric acid powder as an alkalising solubilizer.
Abstract To investigate the possibility of developing a novel oral pharmaceutical product using fenofibric acid instead of choline fenofibrate, the powder properties, solubility, dissolution and pharmacokinetics in rats of fenofibrate, choline fenofibrate and fenofibric acid were compared. Furthermore, the effect of magnesium carbonate, an alkalising agent on the solubility, dissolution and oral bioavailability of fenofibric acid was assessed, a mixture of fenofibric acid and magnesium carbonate being prepared by simple blending at a weight ratio of 2/1. The three fenofibrate derivatives showed different particle ...
Source: Archives of Pharmacal Research - March 18, 2016 Category: Drugs & Pharmacology Authors: Kim KS, Kim JH, Jin SG, Kim DW, Kim DS, Kim JO, Yong CS, Cho KH, Li DX, Woo JS, Choi HG Tags: Arch Pharm Res Source Type: research

Lack of an Effect of Ritonavir Alone and Lopinavir‐Ritonavir on the Pharmacokinetics of Fenofibric Acid in Healthy Volunteers
ConclusionIn contrast to a significant interaction between gemfibrozil and lopinavir‐ritonavir, neither lopinavir‐ritonavir nor ritonavir alone altered the pharmacokinetics of fenofibric acid in healthy volunteers. These data suggest that fenofibrate remains an important option in human immunodeficiency virus–infected patients receiving common ritonavir‐boosted therapy. (Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy)
Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy - January 21, 2016 Category: Drugs & Pharmacology Authors: Lori A. Gordon, Christine Y. Malati, Colleen Hadigan, Mary McLaughlin, Raul M. Alfaro, Mónica M. Calderón, Joseph A. Kovacs, Scott R. Penzak Tags: Original Research Article Source Type: research

A review on the rationale and clinical use of concomitant rosuvastatin and fenofibrate/fenofibric acid therapy.
Authors: Strain JD, Farver DK, Clem JR Abstract Mixed dyslipidemia, characterized by a lipid triad of elevated triglycerides (TG), elevated low-density lipoprotein-cholesterol (LDL-C) and reduced high-density lipoprotein-cholesterol (HDL-C), is a common and frequently difficult to manage condition. The use of combination medications is often needed to effectively treat the lipid triad. The co-administration of statins and fibrates may provide the desired endpoints but safety issues such as toxicity to the muscles, liver and kidneys are a concern. Given the potency of rosuvastatin to lower LDL-C and fenofibrate's ef...
Source: Clinical Pharmacology: Advances and Applications - November 29, 2015 Category: Allergy & Immunology Tags: Clin Pharmacol Source Type: research

Development and application of a UPLC-MS/MS method for simultaneous determination of fenofibric acid and berberine in rat plasma: Application to the drug-drug pharmacokinetic interaction study of fenofibrate combined with berberine after oral administration in rats.
This article is protected by copyright. All rights reserved. PMID: 26577601 [PubMed - as supplied by publisher] (Source: Biomedical Chromatography : BMC)
Source: Biomedical Chromatography : BMC - November 17, 2015 Category: Biomedical Science Authors: Li G, Yang F, Liu M, Su X, Zhao M, Zhao L Tags: Biomed Chromatogr Source Type: research

Nonstatin Therapies for Management of Dyslipidemia: A Review.
Abstract PURPOSE: Cardiovascular disease (CVD) is the leading cause of morbidity and mortality in the United States. Recently published cholesterol treatment guidelines emphasize the use of statins as the preferred treatment strategy for both primary and secondary prevention of CVD. However, the optimal treatment strategy for patients who cannot tolerate statin therapy or those who need additional lipid-lowering therapy is unclear in light of recent evidence that demonstrates a lack of improved cardiovascular outcomes with combination therapy. The purpose of this review is to summarize and interpret evidence that ...
Source: Clinical Therapeutics - September 24, 2015 Category: Drugs & Pharmacology Authors: Sando KR, Michelle Knight P Tags: Clin Ther Source Type: research

Beneficial Effects of Fenofibric Acid on Overexpression of Extracellular Matrix Components, COX-2, and Impairment of Endothelial Permeability Associated with Diabetic Retinopathy.
e; R, Roy S Abstract In the Fenofibric Acid (FA) Intervention and Event Lowering in Diabetes (FIELD) study, FA, a lipid-lowering drug, has been shown to significantly reduce macular edema in diabetic patients. In the present study, we investigated whether FA reduces vascular permeability by inhibiting cyclooxygenase-2 (COX-2), a critical mediator of inflammation, and reducing overexpression of fibronectin (FN) and collagen IV (Coll IV), two basement membrane (BM) components upregulated in diabetic retinopathy. Rat retinal endothelial cells (RRECs) were grown in normal (N:5 mM glucose) or high (HG:30 mM glucose) me...
Source: Experimental Eye Research - August 18, 2015 Category: Opthalmology Authors: Roy S, Kim D, Hernández C, Simó R, Roy S Tags: Exp Eye Res Source Type: research

Development of Omega-3 Phospholipid-based Solid Dispersion of Fenofibrate for the Enhancement of Oral Bioavailability.
Abstract This research aimed to develop the omega-3 phospholipids based solid dispersion to improve the oral bioavailability of fenofibrate. The omega-3 phospholipids based solid dispersion formulation (OPSD) was prepared by an antisolvent precipitation with immediate freeze-drying and the optimal composition of the formulation was determined as the ratios of sucrose to krill oil of 5:1 (w/w), krill oil to fenofibrate of 1.5:1 (w/w), and antisolvent to solvent of 6:4 (v/v). The developed OPSD formulation was characterized by using scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), and differentia...
Source: European Journal of Pharmaceutical Sciences - July 9, 2015 Category: Drugs & Pharmacology Authors: Yang L, Shao Y, Han HK Tags: Eur J Pharm Sci Source Type: research

Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs
In conclusion, this fenofibric acid-loaded controlled release pellet would be a potential alternative to the choline fenofibrate-loaded commercial product. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 8, 2015 Category: Drugs & Pharmacology Source Type: research

Transcriptome Analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα))-Regulated Genes in Primary Human Hepatocytes and the Mouse Liver.
CONCLUSION: These results indicate that changes in the gene expression induced by K-877 treatment are mainly mediated through PPARα activation. K-877 regulates the hepatic gene expression as a SPPARMα and thus may improve dyslipidemia as well as metabolic disorders, such as metabolic syndrome and type 2 diabetes, without untoward side effects. PMID: 26040752 [PubMed - as supplied by publisher] (Source: Journal of Atherosclerosis and Thrombosis)
Source: Journal of Atherosclerosis and Thrombosis - June 5, 2015 Category: Cardiology Tags: J Atheroscler Thromb Source Type: research

Fenofibrate prevents the disruption of the outer blood retinal barrier through downregulation of NF-κB activity
Conclusions Our findings suggest that the anti-inflammatory effects of FA through inhibition of NF-κB activity play a key role in the beneficial effect of fenofibrate for treating DME. (Source: Acta Diabetologica)
Source: Acta Diabetologica - May 5, 2015 Category: Endocrinology Source Type: research

Fenofibrate subcellular distribution as a rationale for the intracranial delivery through biodegradable carrier.
Authors: Grabacka M, Waligorski P, Zapata A, Blake DA, Wyczechowska D, Wilk A, Rutkowska M, Vashistha H, Ayyala R, Ponnusamy T, John VT, Culicchia F, Wisniewska-Becker A, Reiss K Abstract Fenofibrate, a well-known normolipidemic drug, has been shown to exert strong anticancer effects against tumors of neuroectodermal origin including glioblastoma. Although some pharmacokinetic studies were performed in the past, data are still needed about the detailed subcellular and tissue distribution of fenofibrate (FF) and its active metabolite, fenofibric acid (FA), especially in respect to the treatment of intracranial tumor...
Source: Journal of Physiology and Pharmacology - April 24, 2015 Category: Drugs & Pharmacology Tags: J Physiol Pharmacol Source Type: research

Effect of fenofibrate on retinal neurodegeneration in an experimental model of type 2 diabetes
Abstract There is now consistent evidence from two major clinical trials (the Fenofibrate Intervention and Event Lowering in Diabetes and the Action to Control Cardiovascular Risk in Diabetes Eye) that fenofibrate arrests the progression of diabetic retinopathy in type 2 diabetic patients. However, the underlying mechanisms of this beneficial effect remain to be elucidated. The aim of the study was to evaluate the potential effect of fenofibric acid (FA), the active metabolite of fenofibrate, in preventing retinal neurodegeneration in an experimental mouse model of type 2 diabetes. For this purpose, we evaluated ...
Source: Acta Diabetologica - February 1, 2015 Category: Endocrinology Source Type: research

Endoplasmic reticulum stress involved in high-fat diet and palmitic acid-induced vascular damages and fenofibrate intervention.
In this study, female Sprauge Dawley rats were divided into standard chow diets (SCD), high-fat diets (HFD) and HFD plus FF treatment group (HFD+FF) randomly. The rats of latter two groups were given HFD feeding for 5 months, then HFD+FF rats were treated with FF (30 mg/kg, once daily) via gavage for another 2 months. The pathological and tensional changes, protein expression of eNOS, and ER stress related genes in thoracic aorta were measured. Then impacts of palmitic acid (PA) and FF on EDV of thoracic aorta from normal female SD rats were observed. Ultimately the expression of ER stress related genes were assessed in pr...
Source: Biochemical and Biophysical Research communications - January 12, 2015 Category: Biochemistry Authors: Lu Y, Cheng J, Chen L, Li C, Chen G, Gui L, Shen B, Zhang Q Tags: Biochem Biophys Res Commun Source Type: research

The Lidose Hard Capsule Formulation of Fenofibrate is Suprabioavailable Compared to the Nanoparticle Tablet Formulation Under High-fat Fed Conditions.
CONCLUSION: Under high-fat fed conditions the extent of fenofibrate absorption was 37% higher for the 200 mg Lidose hard capsule compared to the 145 mg nanoparticle tablet, which is exactly as expected based on a mg-to-mg weight basis. The results of the present study underline the importance of assessing bioequivalence of fenofibrate formulations under identical fed conditions, and preferentially after a high-fat meal as this condition represents the worst-case scenario. Furthermore, the results of this study demonstrate that the 145 mg nanoparticle tablet is not bioequivalent to the 200 mg Lidose hard capsule when admini...
Source: J Pharm Pharm Sci - January 1, 2015 Category: Drugs & Pharmacology Authors: Verbeeck RK, Niet SD, Lebrun S, Tremege M, Rennie TW, Coffiner M, Streel B, Cahay B Tags: J Pharm Pharm Sci Source Type: research

Peroxisome Proliferator-Activated Receptors α and γ are Linked with Alcohol Consumption in Mice and Withdrawal and Dependence in Humans.
CONCLUSIONS: We provide convergent evidence using both mouse and human data for specific PPARs in alcohol action. Reduced EtOH intake in mice and the genetic association between AD or withdrawal in humans highlight the potential for repurposing FDA-approved PPARα or PPARγ agonists for the treatment of AD. PMID: 25516156 [PubMed - as supplied by publisher] (Source: Alcoholism, Clinical and Experimental Research)
Source: Alcoholism, Clinical and Experimental Research - December 16, 2014 Category: Addiction Authors: Blednov YA, Benavidez JM, Black M, Ferguson LB, Schoenhard GL, Goate AM, Edenberg HJ, Wetherill L, Hesselbrock V, Foroud T, Adron Harris R Tags: Alcohol Clin Exp Res Source Type: research

Peroxisome Proliferator‐Activated Receptors α and γ are Linked with Alcohol Consumption in Mice and Withdrawal and Dependence in Humans
ConclusionsWe provide convergent evidence using both mouse and human data for specific PPARs in alcohol action. Reduced EtOH intake in mice and the genetic association between AD or withdrawal in humans highlight the potential for repurposing FDA‐approved PPARα or PPARγ agonists for the treatment of AD. (Source: Alcoholism: Clinical and Experimental Research)
Source: Alcoholism: Clinical and Experimental Research - December 16, 2014 Category: Addiction Authors: Yuri A. Blednov, Jillian M. Benavidez, Mendy Black, Laura B. Ferguson, Grant L. Schoenhard, Alison M. Goate, Howard J. Edenberg, Leah Wetherill, Victor Hesselbrock, Tatiana Foroud, R. Adron Harris Tags: Original Article Source Type: research

Neuroprotective Potential of Peroxisome Proliferator Activated Receptor- α Agonist in Cognitive Impairment in Parkinson's Disease: Behavioral, Biochemical, and PBPK Profile.
In this study, we have investigated the effect of fenofibrate, a PPAR- α agonist in cognitive impairment model in PD. Bilateral intranigral administration of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) (100 µg/1 µL/side) produced significant cognitive dysfunctions. Fenofibrate treatment at 10, 30, and 100 mg/kg for twenty-five days was found to be neuroprotective and improved cognitive impairment in MPTP-induced PD model as evident from behavioral, biochemical (MDA, GSH, TNF- α , and IL-6), immunohistochemistry (TH), and DNA fragmentation (TUNEL positive cells) studies. ...
Source: PPAR Research - November 25, 2014 Category: Genetics & Stem Cells Tags: PPAR Res Source Type: research

Protective and Antioxidant Effects of PPAR{alpha} in the Ischemic Retina [Retina]
Conclusions. Peroxisome proliferator-activated receptor-alpha has a potent antiapoptotic effect in the ischemic retina. This protective effect may be mediated in part through downregulation of HIF-1α/Nox 4 and consequently alleviation of oxidative stress. (Source: Investigative Ophthalmology)
Source: Investigative Ophthalmology - July 23, 2014 Category: Opthalmology Authors: Moran, E., Ding, L., Wang, Z., Cheng, R., Chen, Q., Moore, R., Takahashi, Y., Ma, J.-x. Tags: Retina Source Type: research

PPAR{alpha} Regulates Mobilization and Homing of Endothelial Progenitor Cells Through the HIF-1{alpha}/SDF-1 Pathway [Retina]
Conclusions. Peroxisome proliferator-activated receptor alpha suppresses ischemia-induced EPC mobilization and homing through inhibition of the HIF-1α/SDF-1 pathway. This represents a novel molecular mechanism for PPARα's antiangiogenic effects. (Source: Investigative Ophthalmology)
Source: Investigative Ophthalmology - June 19, 2014 Category: Opthalmology Authors: Wang, Z., Moran, E., Ding, L., Cheng, R., Xu, X., Ma, J.-x. Tags: Retina Source Type: research

Comparison of Pharmacokinetics of Two Fenofibrate Tablet Formulations in Healthy Human Subjects.
CONCLUSIONS: Both fenofibrate tablet formulations demonstrated equivalent rates and extent of systemic absorption, and hence were considered bioequivalent. PMID: 24844853 [PubMed - as supplied by publisher] (Source: Clinical Therapeutics)
Source: Clinical Therapeutics - May 17, 2014 Category: Drugs & Pharmacology Authors: Chachad SS, Gole M, Malhotra G, Naidu R Tags: Clin Ther Source Type: research

Effects of Fenofibric Acid on Carotid Intima-Media Thickness in Patients With Mixed Dyslipidemia on Atorvastatin Therapy: Randomized, Placebo-Controlled Study (FIRST).
CONCLUSIONS: Compared with atorvastatin monotherapy, FA plus atorvastatin did not further decrease cIMT progression in high-risk patients with mixed dyslipidemia. PMID: 24743431 [PubMed - as supplied by publisher] (Source: Arteriosclerosis, Thrombosis and Vascular Biology)
Source: Arteriosclerosis, Thrombosis and Vascular Biology - April 17, 2014 Category: Cardiology Authors: Davidson MH, Rosenson RS, Maki KC, Nicholls SJ, Ballantyne CM, Mazzone T, Carlson DM, Williams LA, Kelly MT, Camp HS, Lele A, Stolzenbach JC Tags: Arterioscler Thromb Vasc Biol Source Type: research

Effect of ABT-335 (fenofibric acid) on meal-induced oxidative stress in patients with metabolic syndrome
Abstract: Objective: Examine the effect of ABT-335 (fenofibric acid) on postprandial lipemia and susceptibility of plasma lipoproteins to Cu++-mediated oxidation in patients with metabolic syndrome.Methods and results: This is a randomized double-blind, placebo-controlled study with cross-over and includes a 4-week wash-out period between the two treatment periods. At the end of each 8-week treatment period, subjects were challenged with a standardized mixed meal followed by blood collection over the ensuing 6 h. Plasma lipoproteins were isolated by a combination of ultracentrifugation and FPLC for the continuous moni...
Source: Atherosclerosis - November 26, 2013 Category: Cardiology Authors: Ngoc-Anh Le, Monica Farkas-Epperson, Mary Ellen Sweeney, Peter W.F. Wilson, W. Virgil Brown Tags: Clinical & Population Research - Epidemiology, Biomarkers, Nutrition Source Type: research