Comparison of Pharmacokinetics of Two Fenofibrate Tablet Formulations in Healthy Human Subjects

Chachad, Siddharth; Gole, Milind; Malhotra, Geena; Naidu, Raghu

doi:10.1016/j.clinthera.2014.04.017

Cited by 9 publications

(10 citation statements)

References 18 publications

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“…In the present study, the SREBP-1 mRNA level was positively related to mRNA levels of lipogenic genes such as FAS, ACCα and ACCβ, which further supported the notion. It is worth pointing out that fenofibrate is a prodrug of the active chemical moiety fenofibric acid, and that fenofibrate is converted by ester hydrolysis in the liver to fenofibric acid, which is the active constituent in the circulation [50]. Fig.…”

Section: Discussionmentioning

confidence: 99%

Dietary Fenofibrate Reduces Hepatic Lipid Deposition by Regulating Lipid Metabolism in Yellow Catfish Pelteobagrus fulvidraco Exposed to Waterborne Zn

Zheng

Luo

et al. 2015

Lipids

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Fenofibrate is known to possess lipid-lowering effects by regulation of gene transcription involved in lipid metabolism. Waterborne Zn exposure induces lipid deposition in yellow catfish Pelteobagrus fulvidraco. Thus, the present working hypothesis is that dietary fenofibrate addition will reduce hepatic lipids in yellow catfish exposed to waterborne Zn. To this end, juvenile yellow catfish were exposed to 0.04 (control), 0.35 mg/L waterborne Zn, 0.15% dietary fenofibrate, and 0.35 mg Zn/l + 0.15% dietary fenofibrate for 8 weeks. Growth performance, lipid deposition and metabolism in the liver were determined. Dietary fenofibrate promoted growth performance and reduced hepatic lipid content of yellow catfish exposed to waterborne Zn. However, these effects did not appear in fish in normal water. The lipid-lowering effect of fenofibrate on fish exposed to waterborne Zn was associated with increased lipolysis, as indicated by increased CPT I activities and expression of lipolytic genes PPARα, CPT IA, ATGL and HSL, and with reduced lipogenesis as indicated by reduced activities of G6PD, 6PGD, ME and ICDH. Dietary fenofibrate significantly increased mRNA levels of FAS, LPL and ACCα, but reduced mRNA levels of ACCβ and PPARγ in fish exposed to waterborne Zn. Pearson correlations between transcriptional factors expression, and activities and expression of several enzymes were observed, indicating that changes at the molecular and enzymatic levels may underlie the patterns of lipid metabolism and accordingly affect hepatic fat storage. Taken together, our results suggest that the lipid-lowering effect of fenofibrate was attributed, in part, to the down-regulation of lipogenesis and up-regulation of fatty acid oxidation.

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Section: Discussionmentioning

confidence: 99%

Dietary Fenofibrate Reduces Hepatic Lipid Deposition by Regulating Lipid Metabolism in Yellow Catfish Pelteobagrus fulvidraco Exposed to Waterborne Zn

Zheng

Luo

et al. 2015

Lipids

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show abstract

“…This active material induces 24 reductions in total cholesterol, apolipoprotein B, total triglycerides, 25 low density lipoproteins and very low density lipoproteins 26 (Filippatos and Elisaf, 2011). Fenofibrate had been used commer- 27 cially under the brand name Tricor 1 (Green Cross Co., South Korea) 28 (Chachad et al, 2014;Zhang et al, 2012). However, its use is 29 considerably limited because it has very low bioavailability, chiefly 30 under fasting conditions, due to its poor water solubility and 31 lipophilic nature.…”

mentioning

confidence: 97%

Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs

Kim

Jin

Mustapha

et al. 2015

International Journal of Pharmaceutics

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“…Fenofibrate is an oral prodrug that is converted by esterases into its active metabolite, fenofibric acid [125], which is one of the most widely lipid-lowering agent and usually combines with a statin [126]. Fenofibrate has been used commercially under the brand name Tricor ® [127,128] but its use is considerably limited because it has very low bioavailability, chiefly under fasting conditions, due to its poor water solubility and lipophilic nature [129]. Trilipix ® (choline fenofibrate, ABT-335) is the newest formulation of a fibric acid derivative approved by the FDA.…”

Section: Ppar Ligand Therapeutics In Lipid Metabolism Disordermentioning

confidence: 99%

The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development

Hong

Zhai

2018

IJMS

112

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Peroxisome proliferator-activated receptors (PPARs) are a well-known pharmacological target for the treatment of multiple diseases, including diabetes mellitus, dyslipidemia, cardiovascular diseases and even primary biliary cholangitis, gout, cancer, Alzheimer’s disease and ulcerative colitis. The three PPAR isoforms (α, β/δ and γ) have emerged as integrators of glucose and lipid metabolic signaling networks. Typically, PPARα is activated by fibrates, which are commonly used therapeutic agents in the treatment of dyslipidemia. The pharmacological activators of PPARγ include thiazolidinediones (TZDs), which are insulin sensitizers used in the treatment of type 2 diabetes mellitus (T2DM), despite some drawbacks. In this review, we summarize 84 types of PPAR synthetic ligands introduced to date for the treatment of metabolic and other diseases and provide a comprehensive analysis of the current applications and problems of these ligands in clinical drug discovery and development.

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Comparison of Pharmacokinetics of Two Fenofibrate Tablet Formulations in Healthy Human Subjects

Cited by 9 publications

References 18 publications

Dietary Fenofibrate Reduces Hepatic Lipid Deposition by Regulating Lipid Metabolism in Yellow Catfish Pelteobagrus fulvidraco Exposed to Waterborne Zn

Dietary Fenofibrate Reduces Hepatic Lipid Deposition by Regulating Lipid Metabolism in Yellow Catfish Pelteobagrus fulvidraco Exposed to Waterborne Zn

Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs

The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development

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