Literature DB >> 28410749

Efficacy and safety of K-877, a novel selective peroxisome proliferator-activated receptor α modulator (SPPARMα), in combination with statin treatment: Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia.

Hidenori Arai1, Shizuya Yamashita2, Koutaro Yokote3, Eiichi Araki4, Hideki Suganami5, Shun Ishibashi6.   

Abstract

BACKGROUND AND AIMS: Substantial residual cardiovascular risks remain despite intensive statin treatment. Residual risks with high triglyceride and low high-density lipoprotein cholesterol are not the primary targets of statins. K-877 (pemafibrate) demonstrated robust efficacy on triglycerides and high-density lipoprotein cholesterol and a good safety profile as a monotherapy. The aim of these studies was to evaluate the efficacy and safety of K-877 add-on therapy to treat residual hypertriglyceridaemia during statin treatment.
METHODS: The objectives were investigated in two, multicentre, randomised, double-blind, placebo-controlled, parallel group comparison clinical trials: (A) K-877 0.1, 0.2, and 0.4 mg/day in combination with pitavastatin for 12 weeks in 188 patients, (B) K-877 0.2 (fixed dose) and 0.2 (0.4) (conditional up-titration) mg/day in combination with any statin for 24 weeks in 423 patients.
RESULTS: In both studies, we found a robust reduction in fasting triglyceride levels by approximately 50% in all combination therapy groups, which was significant compared to the statin-monotherapy (placebo) groups (p < 0.001). High-performance liquid chromatography analysis for lipoprotein subfractions revealed that atherogenic lipoprotein profiles were ameliorated by K-877 add-on therapy, i.e. small low-density lipoproteins decreased whereas larger ones increased, and larger high-density lipoproteins decreased whereas smaller ones increased. The incidence rates of adverse events and adverse drug reactions in K-877 combination therapy groups were comparable to those in statin-monotherapy groups without any noteworthy event in both studies.
CONCLUSIONS: These results strongly support the favourable benefit-to-risk ratio of K-877 add-on therapy in combination with statin treatment.
Copyright © 2017 The Authors. Published by Elsevier B.V. All rights reserved.

Entities:  

Keywords:  Combination therapy; Dyslipidaemia; K-877; Pemafibrate; SPPARMα; Statin; Triglyceride

Mesh:

Substances:

Year:  2017        PMID: 28410749     DOI: 10.1016/j.atherosclerosis.2017.03.032

Source DB:  PubMed          Journal:  Atherosclerosis        ISSN: 0021-9150            Impact factor:   5.162


  30 in total

1.  Triglyceride-Rich Lipoprotein Cholesterol, Small Dense LDL Cholesterol, and Incident Cardiovascular Disease.

Authors:  Edward K Duran; Aaron W Aday; Nancy R Cook; Julie E Buring; Paul M Ridker; Aruna D Pradhan
Journal:  J Am Coll Cardiol       Date:  2020-05-05       Impact factor: 24.094

Review 2.  Pemafibrate: First Global Approval.

Authors:  Hannah A Blair
Journal:  Drugs       Date:  2017-10       Impact factor: 9.546

Review 3.  Clinical Management of Hypertriglyceridemia in the Prevention of Cardiovascular Disease and Pancreatitis.

Authors:  Patricia Hernandez; Neena Passi; Taher Modarressi; Vivek Kulkarni; Meshal Soni; Fran Burke; Archna Bajaj; Daniel Soffer
Journal:  Curr Atheroscler Rep       Date:  2021-09-13       Impact factor: 5.113

4.  High Density Lipoproteins: Is There a Comeback as a Therapeutic Target?

Authors:  Arnold von Eckardstein
Journal:  Handb Exp Pharmacol       Date:  2022

5.  Small Dense Low-Density Lipoprotein Cholesterol and Cardiovascular Risk in Statin-Treated Patients with Coronary Artery Disease.

Authors:  Junnichi Ishii; Kosuke Kashiwabara; Yukio Ozaki; Hiroshi Takahashi; Fumihiko Kitagawa; Hideto Nishimura; Hideki Ishii; Satoshi Iimuro; Hideki Kawai; Takashi Muramatsu; Hiroyuki Naruse; Hiroshi Iwata; Sadako Tanizawa-Motoyama; Hiroyasu Ito; Eiichi Watanabe; Yutaka Matsuyama; Yoshihiro Fukumoto; Ichiro Sakuma; Yoshihisa Nakagawa; Kiyoshi Hibi; Takafumi Hiro; Seiji Hokimoto; Katsumi Miyauchi; Hiroshi Ohtsu; Hideo Izawa; Hisao Ogawa; Hiroyuki Daida; Hiroaki Shimokawa; Yasushi Saito; Takeshi Kimura; Masunori Matsuzaki; Ryozo Nagai
Journal:  J Atheroscler Thromb       Date:  2021-12-09       Impact factor: 4.394

Review 6.  High-Dose Omega-3 Fatty Acids in Cardiovascular Prevention: Finally Living Up to Their Potential?

Authors:  Adam J Nelson; Sam Mirzaee; Stephen J Nicholls
Journal:  Am J Cardiovasc Drugs       Date:  2020-02       Impact factor: 3.571

7.  Effects of a Novel Selective Peroxisome Proliferator-Activated Receptor α Modulator K-877 (Pemafibrate) on Postprandial hyperlipidemia.

Authors:  Yoshio Fujioka
Journal:  J Atheroscler Thromb       Date:  2017-10-18       Impact factor: 4.928

Review 8.  PPAR Agonists and Metabolic Syndrome: An Established Role?

Authors:  Margherita Botta; Matteo Audano; Amirhossein Sahebkar; Cesare R Sirtori; Nico Mitro; Massimiliano Ruscica
Journal:  Int J Mol Sci       Date:  2018-04-14       Impact factor: 5.923

Review 9.  Pemafibrate (K-877), a novel selective peroxisome proliferator-activated receptor alpha modulator for management of atherogenic dyslipidaemia.

Authors:  Jean-Charles Fruchart
Journal:  Cardiovasc Diabetol       Date:  2017-10-04       Impact factor: 9.951

Review 10.  Selective Peroxisome Proliferator-Activated Receptor Alpha Modulators (SPPARMα): New Opportunities to Reduce Residual Cardiovascular Risk in Chronic Kidney Disease?

Authors:  Jean-Charles Fruchart; Michel P Hermans; Jamila Fruchart-Najib
Journal:  Curr Atheroscler Rep       Date:  2020-07-15       Impact factor: 5.113

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