The selective peroxisome proliferator-activated receptor alpha modulator (SPPARMα) paradigm: conceptual framework and therapeutic potential : A consensus statement from the International Atherosclerosis Society (IAS) and the Residual Risk Reduction Initiative (R3i) Foundation

Cardiovasc Diabetol. 2019 Jun 4;18(1):71. doi: 10.1186/s12933-019-0864-7.

Abstract

In the era of precision medicine, treatments that target specific modifiable characteristics of high-risk patients have the potential to lower further the residual risk of atherosclerotic cardiovascular events. Correction of atherogenic dyslipidemia, however, remains a major unmet clinical need. Elevated plasma triglycerides, with or without low levels of high-density lipoprotein cholesterol (HDL-C), offer a key modifiable component of this common dyslipidemia, especially in insulin resistant conditions such as type 2 diabetes mellitus. The development of selective peroxisome proliferator-activated receptor alpha modulators (SPPARMα) offers an approach to address this treatment gap. This Joint Consensus Panel appraised evidence for the first SPPARMα agonist and concluded that this agent represents a novel therapeutic class, distinct from fibrates, based on pharmacological activity, and, importantly, a safe hepatic and renal profile. The ongoing PROMINENT cardiovascular outcomes trial is testing in 10,000 patients with type 2 diabetes mellitus, elevated triglycerides, and low levels of HDL-C whether treatment with this SPPARMα agonist safely reduces residual cardiovascular risk.

Keywords: Atherogenic dyslipidemia; Diabetes; Inflammation; PROMINENT; Pemafibrate (K-877); Remnant cholesterol; Residual cardiovascular risk; SPPARMalpha; Selective peroxisome proliferator-activated receptor alpha modulator; Triglycerides; Visceral obesity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Benzoxazoles / adverse effects
  • Benzoxazoles / therapeutic use*
  • Biomarkers / blood
  • Butyrates / adverse effects
  • Butyrates / therapeutic use*
  • Cardiovascular Diseases / blood
  • Cardiovascular Diseases / diagnosis
  • Cardiovascular Diseases / prevention & control*
  • Consensus
  • Dyslipidemias / blood
  • Dyslipidemias / diagnosis
  • Dyslipidemias / drug therapy*
  • Humans
  • Hypolipidemic Agents / adverse effects
  • Hypolipidemic Agents / therapeutic use*
  • Lipids / blood*
  • Molecular Targeted Therapy
  • PPAR alpha / agonists*
  • PPAR alpha / metabolism
  • Patient Safety
  • Risk Assessment
  • Risk Factors
  • Signal Transduction
  • Treatment Outcome

Substances

  • (R)-2-(3-((benzoxazol-2-yl-d4 (3-(4-methoxyphenoxy-d7)propyl)amino)methyl)phenoxy) butanoic acid
  • Benzoxazoles
  • Biomarkers
  • Butyrates
  • Hypolipidemic Agents
  • Lipids
  • PPAR alpha
  • PPARA protein, human