Cited by 165Peroxisome Proliferator-Activated ReceptorsLipoproteins and Cardiovascular HealthDiabetes, Cardiovascular Risks, and Lipoproteins

Effects of Pemafibrate, a Novel Selective PPARα Modulator, on Lipid and Glucose Metabolism in Patients With Type 2 Diabetes and Hypertriglyceridemia: A Randomized, Double-Blind, Placebo-Controlled, Phase 3 Trial

Araki, Eiichi, Yamashita, Shizuya, Arai, Hidenori, Yokote, Koutaro, Satoh, Jo, Inoguchi, Toyoshi, Nakamura, Jiro, Maegawa, Hiroshi +5 more·2018·Diabetes Care

Abstract

OBJECTIVE: Type 2 diabetes is frequently complicated with atherogenic dyslipidemia. This study aimed to evaluate the efficacy and safety of pemafibrate (K-877) in patients with type 2 diabetes comorbid with hypertriglyceridemia. RESEARCH DESIGN AND METHODS: Patients were randomly assigned to three groups and received placebo (n = 57), 0.2 mg/day pemafibrate (n = 54), or 0.4 mg/day pemafibrate (n = 55) for 24 weeks (treatment period 1). Subsequently, the patients received follow-up treatment for another 28 weeks (treatment period 2), in which the placebo was switched to 0.2 mg/day pemafibrate. This article presents the results of treatment period 1, which were the primary objectives. RESULTS: The pemafibrate groups showed significantly reduced fasting serum triglyceride levels by ∼45% compared with the placebo group (P < 0.001). Additionally, the pemafibrate groups displayed significant decreases in non-HDL and remnant lipoprotein cholesterol, apolipoprotein (Apo) B100, ApoB48, and ApoCIII levels and significant increases in HDL cholesterol and ApoA-I levels. LDL cholesterol levels were not considerably altered in the pemafibrate groups. Furthermore, the 0.2 mg/day pemafibrate group showed a significantly reduced HOMA–insulin resistance score compared with the placebo group; however, no significant changes compared with placebo were found in fasting plasma glucose, fasting insulin, glycoalbumin, or HbA1c levels. The pemafibrate groups also showed significantly increased fibroblast growth factor 21 levels compared with the placebo group. All groups displayed comparable rates of adverse events and drug reactions. CONCLUSIONS: Pemafibrate significantly ameliorated lipid abnormalities and was well tolerated in patients with type 2 diabetes comorbid with hypertriglyceridemia.

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Registry

Crossref · 10.2337/dc17-1589

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38 of 38 references verified0 citation errors · 0 not checkable

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  • Pemafibrate reduces triglyceride levels and improves other lipid levels.

    “Pemafibrate, a selective peroxisome proliferator-activated receptor α modulator, reduces triglyceride levels and improves other lipid levels.”
  • Phase 2 studies showed that pemafibrate had greater triglyceride-lowering and HDL cholesterol-raising actions with fewer off-target effects than PPARα agonists such as fenofibrate.

    “Phase 2 studies have shown that, as compared with PPARα agonists such as fenofibrate, pemafibrate had greater triglyceride-lowering and HDL cholesterol-raising actions with fewer off-target effects. 9-14”

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Authors
Araki, E., Yamashita, S., Arai, H., Yokote, K., Satoh, J., Inoguchi, T., Nakamura, J., Maegawa, H., Yoshioka, N., Tanizawa, Y., Watada, H., Suganami, H., & Ishibashi, S.
Affiliations
  • Kumamoto University (JP)
  • Rinku General Medical Center (JP)
  • National Center for Geriatrics and Gerontology (JP)
  • Chiba University (JP)
  • Tohoku Medical and Pharmaceutical University Wakabayashi Hospital (JP)
  • Fukuoka Health Promotion Support Center, Fukuoka, Japan
  • Aichi Medical University (JP)
  • Shiga University of Medical Science (JP)
  • NTT Medical Center Sapporo (JP)
  • Yamaguchi University (JP)
  • Juntendo University (JP)
  • Kowa (Japan) (JP)
  • Jichi Medical University (JP)
Corresponding author
Araki, Eiichi
Venue
Diabetes Care
Published
2018-01-03
Volume
41
Issue
3
Pages
538-546
ISSN
  • 0149-5992 (ISSN-L)
  • 1935-5548
OpenAlex
W2782064714
Cited by
164
References
38
Citations by year
2026: 10 · 2025: 12 · 2024: 17 · 2023: 17 · 2022: 20 · 2021: 25 · 2020: 17 · 2019: 32 · 2018: 13 · 2017: 1
FWCI
7.75
Type
journal article
Language
en
Open access
closed
Locations
  • Diabetes Care (publishedVersion)
  • PubMed (publishedVersion)
Funders
Japan Society for the Promotion of Science (17K19643, 17H04201, 17H02100, 18K08482, 15H04849)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Peroxisome Proliferator-Activated Receptors
  • Health Sciences › Medicine › Surgery › Lipoproteins and Cardiovascular Health
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes, Cardiovascular Risks, and Lipoproteins
Keywords
pemafibrate, PPARα agonist, type 2 diabetes, hypertriglyceridemia, dyslipidemia, triglyceride lowering, remnant cholesterol, apolipoprotein B, apolipoprotein C-III, HDL cholesterol, apolipoprotein A-I, insulin resistance, FGF21, glucose metabolism, drug safety
MeSH terms
Aged, Benzoxazoles, Blood Glucose, Butyrates, Diabetes Mellitus, Type 2, Double-Blind Method, Female, Humans, Lipids, Male, Middle Aged, Placebos, Hypertriglyceridemia, PPAR alpha, Lipid Metabolism

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