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New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease.
Expert Opin Pharmacother. 2014 Mar; 15(4):493-503.EO

Abstract

INTRODUCTION

Novel peroxisome proliferator-activated receptor (PPAR) modulators (selective PPAR modulators [SPPARMs]) and dual PPAR agonists may have an important role in the treatment of cardiometabolic disorders owing to lipid-modifying, insulin-sensitizing and anti-inflammatory effects.

AREAS COVERED

This review summarizes the efficacy of new PPAR agonists and SPPARMs that are under development for the treatment of atherogenic dyslipidemia and non-alcoholic fatty liver disease (NAFLD).

EXPERT OPINION

ABT-335 is a new formulation of fenofibrate that has been approved for concomitant use with statins. K-877, a SPPARM-α with encouraging preliminary results in modulating atherogenic dyslipidemia, and INT131, a SPPARM-γ with predominantly insulin-sensitizing actions, may also have favorable lipid-modifying effects. Although the development of dual PPAR-α/γ agonists (glitazars) and the SPPARM-δ GW501516 has been abandoned because of safety issues, another SPPARM-δ (MBX-8025) and a dual PPAR-α/δ agonist (GFT-505) have shown promising efficacy in decreasing plasma triglyceride and increasing high-density lipoprotein cholesterol concentrations, as well as improving insulin sensitivity and liver function. The beneficial effects of GFT-505 are complemented by preclinical findings that indicate reduction of hepatic fat accumulation, inflammation and fibrosis, making it a promising candidate for the treatment of NAFLD/nonalcoholic steatohepatitis (NASH). Long-term trials are required to test the efficacy and safety of these new PPAR agonists in reducing cardiovascular outcomes and treating NAFLD/NASH.

Authors+Show Affiliations

Biotechnology Research Center, Mashhad University of Medical Sciences , Mashhad , Iran.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

24428677

Citation

Sahebkar, Amirhossein, et al. "New Peroxisome Proliferator-activated Receptor Agonists: Potential Treatments for Atherogenic Dyslipidemia and Non-alcoholic Fatty Liver Disease." Expert Opinion On Pharmacotherapy, vol. 15, no. 4, 2014, pp. 493-503.
Sahebkar A, Chew GT, Watts GF. New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease. Expert Opin Pharmacother. 2014;15(4):493-503.
Sahebkar, A., Chew, G. T., & Watts, G. F. (2014). New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease. Expert Opinion On Pharmacotherapy, 15(4), 493-503. https://doi.org/10.1517/14656566.2014.876992
Sahebkar A, Chew GT, Watts GF. New Peroxisome Proliferator-activated Receptor Agonists: Potential Treatments for Atherogenic Dyslipidemia and Non-alcoholic Fatty Liver Disease. Expert Opin Pharmacother. 2014;15(4):493-503. PubMed PMID: 24428677.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease. AU - Sahebkar,Amirhossein, AU - Chew,Gerard T, AU - Watts,Gerald F, Y1 - 2014/01/16/ PY - 2014/1/17/entrez PY - 2014/1/17/pubmed PY - 2014/10/25/medline SP - 493 EP - 503 JF - Expert opinion on pharmacotherapy JO - Expert Opin Pharmacother VL - 15 IS - 4 N2 - INTRODUCTION: Novel peroxisome proliferator-activated receptor (PPAR) modulators (selective PPAR modulators [SPPARMs]) and dual PPAR agonists may have an important role in the treatment of cardiometabolic disorders owing to lipid-modifying, insulin-sensitizing and anti-inflammatory effects. AREAS COVERED: This review summarizes the efficacy of new PPAR agonists and SPPARMs that are under development for the treatment of atherogenic dyslipidemia and non-alcoholic fatty liver disease (NAFLD). EXPERT OPINION: ABT-335 is a new formulation of fenofibrate that has been approved for concomitant use with statins. K-877, a SPPARM-α with encouraging preliminary results in modulating atherogenic dyslipidemia, and INT131, a SPPARM-γ with predominantly insulin-sensitizing actions, may also have favorable lipid-modifying effects. Although the development of dual PPAR-α/γ agonists (glitazars) and the SPPARM-δ GW501516 has been abandoned because of safety issues, another SPPARM-δ (MBX-8025) and a dual PPAR-α/δ agonist (GFT-505) have shown promising efficacy in decreasing plasma triglyceride and increasing high-density lipoprotein cholesterol concentrations, as well as improving insulin sensitivity and liver function. The beneficial effects of GFT-505 are complemented by preclinical findings that indicate reduction of hepatic fat accumulation, inflammation and fibrosis, making it a promising candidate for the treatment of NAFLD/nonalcoholic steatohepatitis (NASH). Long-term trials are required to test the efficacy and safety of these new PPAR agonists in reducing cardiovascular outcomes and treating NAFLD/NASH. SN - 1744-7666 UR - https://www.unboundmedicine.com/medline/citation/24428677/New_peroxisome_proliferator_activated_receptor_agonists:_potential_treatments_for_atherogenic_dyslipidemia_and_non_alcoholic_fatty_liver_disease_ L2 - http://www.tandfonline.com/doi/full/10.1517/14656566.2014.876992 DB - PRIME DP - Unbound Medicine ER -