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Review
. 2018 Apr 6;9(9):1527-1537.
doi: 10.7150/jca.24488. eCollection 2018.

Anticancer Properties of Fenofibrate: A Repurposing Use

Xin Lian  1   2 , Gang Wang  1 , Honglan Zhou  1 , Zongyu Zheng  1   2 , Yaowen Fu  1 , Lu Cai  1   2   3
Affiliations
Review

Anticancer Properties of Fenofibrate: A Repurposing Use

Xin Lian et al. J Cancer. .

Abstract

Cancer is a leading cause of death throughout the world, and cancer therapy remains a big medical challenge in terms of both its therapeutic efficacy and safety. Therefore, to find out a safe anticancer drug has been long goal for oncologist and medical scientists. Among clinically used medicines with no or little toxicity, fenofibrate is a drug of the fibrate class that plays an important role in lowering the levels of serum cholesterol and triglycerides while elevating the levels of high-density lipoproteins. Recently, several studies have implied that fenofibrate may exert anticancer effects via a variety of pathways involved in apoptosis, cell-cycle arrest, invasion, and migration. Given the great potential that fenofibrate may have anticancer effects, this review was to investigate all published works which directly or indirectly support the anticancer activity of fenofibrate. These studies provide evidence that fenofibrate exerted antitumor effects in several human cancer cell lines, such as breast, liver, glioma, prostate, pancreas, and lung cancer cell lines. Among these studies some have further confirmed the possibility and efficacy of fenofibrate anticancer in xenograft mouse models. In the last part of this review, we also discuss the potential mechanisms of action of fenofibrate based on the available information. Overall, we may repurpose fenofibrate as an anticancer drug in cancer treatment, which urgently need further and comprehensively investigated.

Keywords: fenofibrate, lipid-lowering, anticancer drug; repurposing.

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Conflict of interest statement

Competing Interests: The authors have declared that no competing interest exists.

Figures

Figure 1
Figure 1
Chemical structure of fenofibrate. Fenofibrate is 2-4[(4-chlorobenzoyl) phenoxy]-2-methylpropanoic acid, 1-methylethyl ester.
Figure 2
Figure 2
Lowering lipid mechanisms of fenofibrate. Fenifibrate activates PPARα, and forms a heterodimer with RXR, then interacts with PPRE, leading to the activation of target gene transcription of lipid metabolism regulation genes. PPARα: peroxisome proliferator-activated receptor α; RXR: retinoid X receptor; PPRE: peroxisome proliferator response element; Apo: apolipoprotein; HDL: high-density lipoprotein; VLDL: very-low-density lipoprotein; TG: triglyceride.
Figure 3
Figure 3
Key signaling mechanisms involved in anticancer activities of fenofibrate. Fenofibrate inhibited multiple cancers by regulation of apoptosis, cell cycle arrest, invasion and migration through different pathways. ROS: reactive oxygen species; NF-κB: nuclear factor kappa-light-chain-enhancer of activated B cells; FoxO3A: Fork-head box O3A; FoxO1: Fork-head box O1; ERK: extracellular-signal-regulated kinase; AMPK: 5' adenosine monophosphate-activated protein kinase; Bax: Bcl-2-associated X protein; Bim: Bcl-2-like protein 11; Bcl-2: B-cell lymphoma 2; bcl-xL: B-cell lymphoma-extra large; MMPs: Matrix metalloproteinases.
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