Pemafibrate (Parmodia®) is a novel, highly selective peroxisome proliferator-activated receptor (PPAR)-α modulator (SPPARM). It acts by binding to PPAR-α and regulating the expression of target genes that modulate lipid metabolism, thereby decreasing plasma triglyceride levels and increasing high-density lipoprotein cholesterol levels. Developed by Kowa Company, Ltd., oral pemafibrate has been approved in Japan for the treatment of hyperlipidaemia (including familial hyperlipidaemia). This article summarizes the milestones in the development of pemafibrate leading to this first global approval for hyperlipidaemia.
The preparation of this review was not supported by any external funding. During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the author on the basis of scientific completeness and accuracy. H. A. Blair is a salaried employee of Adis, Springer SBM.
Additional information about this Adis Drug Review can be found at http://www.medengine.com/Redeem/B8FBF0603C57D013.
- 1.Kowa Co. PARMODIA® tab. 0.1 mg: prescribing information. 2017. www.kowa-souyaku.co.jp. Accessed 16 Aug 2017.
- 2.Takei K, Han SI, Murayama Y, et al. Selective peroxisome proliferator-activated receptor-alpha modulator K-877 efficiently activates the peroxisome proliferator-activated receptor-alpha pathway and improves lipid metabolism in mice. J Diabetes Investig. 2017;8(4):446–52.CrossRefPubMedPubMedCentralGoogle Scholar
- 3.Kowa Co Ltd. [The treatment of hyperlipidemia “Parmodia® tablets 0.1 mg” about acquiring manufacturing and marketing approval in Japan. First time high active and highly selective PPARα modulator in the world]. 2017. http://www.kowa.co.jp. Accessed 16 Aug 2017.
- 7.Sairyo M, Kobayashi T, Masuda D, et al. A novel selective PPARα modulator (SPPARMα), K-877 (pemafibrate), attenuates postprandial hypertriglyceridemia in mice. J Atheroscler Thromb. 2017. doi: 10.5551/jat.39693.
- 8.Yamashita S, Ishibashi S, Arai H, et al. Effect of K-877, a potent and selective PPAR alpha modulator (SPPARM alpha), on postprandial hyperlipidemia in dyslipidemic patients: a randomized cross-over study [abstract no. P5891]. Eur Heart J. 2016;37(Suppl 1):1204.Google Scholar
- 9.Yamashita S, Ishibashi S, Arai H, et al. Effect of K-877, a potent and selective PPAR alpha modulator (SPPARM alpha), on cholesterol efflux from macrophages in dyslipidemic patients [abstract no. P5982]. Eur Heart J. 2015;36(Suppl. 1):1047–8.Google Scholar
- 10.Araki E, Yamashita S, Arai H, et al. Effects of K-877, a novel selective PPARα modulator (SPPARMα), on lipid and glucose metabolism in fasting and postprandial states in type 2 diabetic patients with dyslipidaemia [abstract no. 1112]. Diabetologia. 2016;59(Suppl. 1):S531.Google Scholar
- 11.Ishibashi S, Yamashita S, Arai H, et al. Efficacy and safety of K-877, a potent and selective PPAR-α agonist, in Japanese patients with dyslipidemia [abstract no. 10718]. Circulation. 2013;128(22 Suppl. 1).Google Scholar
- 12.Yamashita S, Ishibashi S, Arai H, et al. Comparison of the novel peroxisome proliferator-activated receptor alpha agonist K-877 and fenofibrate on high-density lipoprotein subclass distribution determined by high-performance liquid chromatography in patients with dyslipidemia [abstract no. 15652]. Circulation. 2013;128(22 Suppl. 1).Google Scholar
- 13.Arai H, Yamashita S, Yokote K, et al. 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. Atherosclerosis. 2017;261:144–52.CrossRefPubMedGoogle Scholar
- 14.Kastelein JJP, Senko Y, Hounslow N, et al. K-877, a selective PPAR alpha modulator (SPPARM alpha), ameliorates dyslipidaemia in patients with well-controlled LDL cholesterol levels on statin therapy, without increases in serum creatinine [abstract no. P5983]. Eur Heart J. 2015;36(Suppl. 1):1048.Google Scholar
- 15.Kastelein JJP, Senko Y, Hounslow N, et al. K-877, a selective PPAR alpha modulator (SPPARM alpha), improves dyslipidaemia in statin-treated patients with type 2 diabetes mellitus [abstract no. P5985]. Eur Heart J. 2015;36(Suppl. 1):1048.Google Scholar