SPPARMαへの期待

出版社: フジメディカル出版
著者:
発行日: 2019-06-10
分野: 臨床医学:内科  >  循環器一般
ISBN: 9784862701725
電子書籍版: 2019-06-10 (初版第1刷)
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選択的PPARαモジュレータ―(SPPARMα)という新たな概念に基づいて創薬されたペマフィブラート。フィブラートを超えた新たなPPARαアゴニストとしての期待は大きい。
その開発の経緯,遺伝子発現解析,作用機序,適応疾患(高TG血症・低HDL-C血症)と使い方,スタチンとの併用療法,安全性(副作用,相互作用)など,新薬の特性を国内屈指の執筆順が詳解。
「脂質異常症」の診療に携わる臨床医必備の1冊。

目次

  • 表紙
  • 執筆者一覧
  • 目次
  • カラー図譜
  • 本書をご覧いただくにあたって
  • イントロダクション
  • 1 SPPARMαとは ?
  • 1) パルモディア ( R ) はいかに開発されたか : PPAR薬の革新への2つのイノベーション
  • 2) 遺伝子発現解析からみた有用性
  • 3) 作用メカニズム - 構造の特徴から作用特性まで
  • 4) 世界におけるSPPARMα開発の最先端
  • 2 SPPARMαの臨床
  • 1) 高TG血症に対して ( 高レムナント血症, small dense LDLも含めて )
  • 2) 低HDL - C血症に対して
  • 3) スタチンとの併用
  • 4) 動脈硬化性疾患予防におけるポジショニング
  • 3 SPPARMαの安全性
  • 1) 副作用
  • 2) 薬物動態と薬物相互作用
  • 4 SPPARMαの幅広い使い方
  • 1) 腎機能低下例
  • 2) NASH
  • 3) 肥満・メタボリックシンドローム
  • 4) 2型糖尿病合併例
  • 5) 高齢者
  • 5 SPPARMαのエビデンス
  • 1) フィブラートのRCTの歴史
  • 2) PROMINENTの意義・概要
  • 6 トピックス
  • topic 1) 冠動脈疾患発症における中性脂肪の関わり
  • topic 2) 食後高中性脂肪血症管理の重要性
  • topic 3) 遺伝子多型から考えるトリグリセライドリスク
  • topic 4) 血管炎症におけるPPARαの関わり SPPARMαによる血管慢性炎症抑制のメカニズムと効果への期待
  • topic 5) 褐色脂肪細胞およびベージュ脂肪細胞の分化・機能制御におけるPPARαの関わり
  • 7 SPPARMαの展望 - まとめに代えて
  • 索引
  • 奥付

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参考文献のリンクは、リンク先の都合等により正しく表示されない場合がありますので、あらかじめご了承下さい。

本参考文献は電子書籍掲載内容を元にしております。

イントロダクション

P.27 掲載の参考文献
6) Rubins HB et al : Gemfibrozil for the secondary prevention of coronary heart disease in men with low levels of high-density lipoprotein cholesterol. Veterans Affairs High-Density Lipoprotein Cholesterol Intervention Trial Study Group. N Engl J Med 341 : 410-418, 1999
16) Fruchart JC : Selective peroxisome proliferator-activated receptor α modulators (SPPARMα) : the next generation of peroxisome proliferator-activated receptor α-agonists. Cardiovasc Diabetol 12 : 82, 2013
19) Takizawa T et al : Abstract 12867 : The mechanism of K-877, a highly potent and selective PPARalpha modulator, on regulation of synthesis, secretion and metabolism of triglycerides and cholesterol. Circulation 128 : A12867, 2013 [AHA2013 Abstract]
21) Raza-Iqbal S et al : Transcriptome Analysis of K-877 (a Novel Selective PPARalpha Modulator (SPPARMα)) -Regulated Genes in Primary Human Hepatocytes and the Mouse Liver. J Atheroscler Thromb 22 : 754-772, 2015
22) Yamamoto Y et al : Molecular association model of PPARα and its new specific and efficient ligand, pemafibrate : Structural basis for SPPARMα. Biochem Biophys Res Commun 499 : 239-245, 2018
23) 日本動脈硬化学会 : 動脈硬化性疾患予防のための脂質異常症診療ガイド 2018年版
24) Ishibashi S et al : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, active- and placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
26) Ishibashi S et al : Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor αmodulator, in patients with dyslipidemia : Results from a 24-week, randomized, double blind, active-controlled, phase 3 trial. J Clin Lipidol 12 : 173-184, 2018
37) Sairyo M et al : A Novel Selective PPARalpha Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice. J Atheroscler Thromb 25 : 142-152, 2018
38) Takei K et al : Effects of K-877, a novel selective PPARα modulator, on small intestine contribute to the amelioration of hyperlipidemia in low-density lipoprotein receptor knockout mice. J Pharmacol Sci 133 : 214-222, 2017
42) Araki M et al : The Peroxisome Proliferator-Activated Receptorα (PPARα) Agonist Pemafibrate Protects Against Diet-Induced Obesity in Mice. Int J Mol Sci 19. pii : E2148, 2018
45) Yamashita S et al : Effects of selective PPARαmodulator K-877 on particle numbers of lipoprotein subclasses in dyslipidemic patients : Analysis by GP-HPLC and NMR lipoprofile 2 and 3. Atherosclerosis Supplements 32 : 62-63, 2018 [ISA2018 Abstract]
49) Arai H et al : Efficacy and safety of K-877, a novel selective peroxisome proliferatoractivated receptor α modulator (SPPARMα), in combination with statin treatment : Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia. Atherosclerosis 261 : 144-152, 2017
53) Yokote K et al, on behalf of the K-877 Study Group : Long-term efficacy and safety of pemafibrate, a novel selective peroxisome proliferator-activated receptor α-modulator (SPPARMα), in dyslipidemic patients with renal impairment. Int J Mol Sci 20 : pii : E706, 2019

1 SPPARMαとは ?

P.40 掲載の参考文献
7) Raza-Iqbal S et al : Transcriptome Analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα)) -Regulated Genes in Primary Human Hepatocytes and the Mouse Liver. J Atheroscler Thromb 22 : 754-772, 2015
9) Ishibashi S et al ; K-877-04 Study Group : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, activeand placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
10) Arai H et al ; K-877 Study Group : 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 261 : 144-152, 2017
12) Araki E et al : 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. Diabetes Care 41 : 538-546, 2018
13) Ishibashi S et al ; K-877 Study Group : Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor α modulator, in patients with dyslipidemia : Results from a 24-week, randomized, double blind, active-controlled, phase 3 trial. J Clin Lipidol 12 : 173-184, 2018
P.49 掲載の参考文献
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2) Fruchart JC : Peroxisome proliferator-activated receptor-α (PPARα) : at the crossroads of obesity, diabetes and cardiovascular disease. Atherosclerosis 205 : 1-8, 2009
3) Fruchart JC : Selective peroxisome proliferator-activated receptor α modulators (SPPARMα) : the next generation of peroxisome proliferator-activated receptor α-agonists. Cardiovasc Diabetol 12 : 82, 2013
4) Raza-Iqbal S et al : Transcriptome Analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα)) -Regulated Genes in Primary Human Hepatocytes and the Mouse Liver. J Atheroscler Thromb 22 : 754-772, 2015
5) Ishibashi S et al, K-877-04 Study Group : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, activeand placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
8) Gao Y et al : Upregulation of hepatic VLDLR via PPARα is required for the triglyceride-lowering effect of fenofibrate. J Lipid Res 55 : 1622-1633, 2014
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P.60 掲載の参考文献
1) Fruchart JC : Selective peroxisome proliferator-activated receptor α modulators (SPPARMα) : the next generation of peroxisome proliferator-activated receptor α-agonists. Cardiovasc Diabetol 12 : 82, 2013
2) Takei K et al : Selective peroxisome proliferator-activated receptor-α modulator K-877 efficiently activates the peroxisome proliferator-activated receptor-α pathway and improves lipid metabolism in mice. J Diabetes Investig 8 : 446-452, 2017
3) Raza-Iqbal S et al : Transcriptome Analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα)) -Regulated Genes in Primary Human Hepatocytes and the Mouse Liver. J Atheroscler Thromb 22 : 754-772, 2015
4) Takei K et al : Effects of K-877, a novel selective PPARα modulator, on small intestine contribute to the amelioration of hyperlipidemia in low-density lipoprotein receptor knockout mice. J Pharmacol Sci 133 : 214-222, 2017
5) Araki M et al : The Peroxisome Proliferator-Activated Receptor α (PPARα) Agonist Pemafibrate Protects against Diet-Induced Obesity in Mice. Int J Mol Sci 19 : 2148, 2018
6) Yamamoto Y et al : Molecular association model of PPARα and its new specific and efficient ligand, pemafibrate : Structural basis for SPPARMα. Biochem Biophys Res Commun 499 : 239-245, 2018
P.63 掲載の参考文献
2) Yamamoto Y et al : Molecular association model of PPARα and its new specific and efficient ligand, pemafibrate : Structural basis for SPPARMα. Biochem Biophys Res Commun 499 : 239-245, 2018
3) Raza-Iqbal S et al : Transcriptome Analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα)) -Regulated Genes in Primary Human Hepatocytes and the Mouse Liver. J Atheroscler Thromb 22 : 754-772, 2015
4) Hennuyer N et al : The novel selective PPARα modulator (SPPARMα) pemafibrate improves dyslipidemia, enhances reverse cholesterol transport and decreases inflammation and atherosclerosis. Atherosclerosis 249 : 200-208, 2016
6) Ishibashi S et al : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, active- and placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
7) Ishibashi S et al : Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor α modulator, in patients with dyslipidemia : Results from a 24-week, randomized, double blind, active-controlled, phase 3 trial. J Clin Lipidol 12 : 173-184, 2018
9) Matsuba I et al : Effects of a novel selective peroxisome proliferator-activated receptor-α modulator, pemafibrate, on hepatic and peripheral glucose uptake in patients with hypertriglyceridemia and insulin resistance. J Diabetes Investig 9 : 1323-1332, 2018
10) Araki E et al : 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. Diabetes Care 41 : 538-546, 2018
11) Arai H et al : Efficacy and safety of K-877, a novel selective peroxisome proliferatoractivated receptor α modulator (SPPARMα), in combination with statin treatment : Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia. Atherosclerosis 261 : 144-152, 2017

2 SPPARMαの臨床

P.75 掲載の参考文献
2) Arai H et al, K-877 Study Group : 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 261 : 144-152, 2017
16) Ishibashi S et al : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, active- and placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
P.84 掲載の参考文献
3) Ko KW et al : Triglyceride transfer is required for net cholesteryl ester transfer between lipoproteins in plasma by lipid transfer protein. Evidence for a hetero-exchange transfer mechanism demonstrated by using novel monoclonal antibodies. J Biol Chem 269 : 28206-28213, 1994
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9) Colin S et al : Activation of intestinal peroxisome proliferator-activated receptor-α increases high-density lipoprotein production. Eur Heart J 34 : 2566-2574, 2013
10) Hennuyer N et al : The novel selective PPARα modulator (SPPARMα) pemafibrate improves dyslipidemia, enhances reverse cholesterol transport and decreases inflammation and atherosclerosis. Atherosclerosis 249 : 200-208, 2016
11) Raza-Iqbal S et al : Transcriptome Analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα)) -Regulated Genes in Primary Human Hepatocytes and the Mouse Liver. J Atheroscler Thromb 22 : 754-772, 2015
12) Ishibashi S et al : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, active- and placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
13) Ishibashi S et al ; K-877 Study Group : Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor αmodulator, in patients with dyslipidemia : Results from a 24-week, randomized, double blind, active-controlled, phase 3 trial. J Clin Lipidol 12 : 173-184, 2018
14) Arai H et al ; K-877 Study Group : 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 261 : 144-152, 2017
P.90 掲載の参考文献
1) Arai H et al ; K-877 Study Group : Efficacy and safety of K-877, a novel selective rator-activated receptor α modulator (SPPARMα), in combination with statin treatment : Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia. Atherosclerosis 261 : 144-152, 2017
P.101 掲載の参考文献

3 SPPARMαの安全性

P.110 掲載の参考文献
1) Fruchart JC : Selective peroxisome proliferator-activated receptor α modulators (SPPARMα) : the next generation of peroxisome proliferator-activated receptor α-agonist. Cardiovasc Diabetol 12 : 82, 2013
3) パルモディア錠インタビューフォーム
4) Ishibashi S et al : Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor α modulator, in patients with dyslipidemia : Results from a 24-week, randomized, double blind, active-controlled, phase 3 trial. J Clin Lipidol 12 : 173-184, 2018
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8) Arai H et al : Efficacy and Safety of K-877, a novel selective peroxisome proliferatoractivated receptor α modulator (SPPARMα), in combination with statin treatment : Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidemia. Atherosclerosis 261 : 144-152, 2017
P.118 掲載の参考文献

4 SPPARMαの幅広い使い方

P.126 掲載の参考文献
2) Fruchart JC : Selective peroxisome proliferator-activated receptor α modulators (SPPARMα) : the next generation of peroxisome proliferator-activated receptor α-agonists. Cardiovasc Diabetol 12 : 82, 2013
3) Ishibashi S et al : Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor α modulator, in patients with dyslipidemia : Results from a 24-week, randomized, double blind, active-controlled, phase 3 trial. J Clin Lipidol 12 : 173-184, 2018
4) Araki E et al : 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. Diabetes Care 41 : 538-546, 2018
5) 医薬品インタビューフォーム 高脂血症治療剤パルモディア錠
9) Hong YA et al : Fenofibrate improves renal lipotoxicity through activation of AMPKPGC-1α in db/db mice. PLoS One 9 : e96147, 2014
10) Maki T et al : Renoprotective effect of a novel selective PPARα modulator K-877 in db/db mice : A role of diacylglycerol-protein kinase C-NAD (P) H oxidase pathway. Metabolism 71 : 33-45, 2017
11) Yokote K et al ; Of The K-Study Group OB : Long-Term Efficacy and Safety of Pemafibrate, a Novel Selective Peroxisome Proliferator-Activated Receptor-α Modulator (SPPARMα), in Dyslipidemic Patients with Renal Impairment. Int J Mol Sci 20 : pii : E706, 2019
P.137 掲載の参考文献
2) Ip E et al : Central role of PPARα-dependent hepatic lipid turnover in dietary steatohepatitis in mice. Hepatology 38 : 123-132, 2003
5) Larter CZ et al : Peroxisome proliferator-activated receptor-α agonist, Wy 14,643, improves metabolic indices, steatosis and ballooning in diabetic mice with non-alcoholic steatohepatitis. J Gastroenterol Hepatol 27 : 341-350, 2012
12) Fruchart JC : Selective peroxisome proliferator-activated receptor α modulators (SPPARMα) : the next generation of peroxisome proliferator-activated receptor α-agonists. Cardiovasc Diabetol 12 : 82, 2013
14) Ishibashi S et al : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, active- and placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
P.146 掲載の参考文献
2) Fruchart JC : Selective peroxisome proliferator-activated receptor α modulators (SPPARMα) : the next generation of peroxisome proliferator-activated receptor α-agonists. Cardiovasc Diabetol 12 : 82, 2013
14) Ishibashi S et al : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, active- and placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
16) Ishibashi S et al : Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor α modulator, in patients with dyslipidemia : Results from a 24-week, randomized, double blind, active-controlled, phase 3 trial. J Clin Lipidol 12 : 173-184, 2018
17) Arai H et al : Efficacy and safety of K-877, a novel selective peroxisome proliferatoractivated receptor α modulator (SPPARMα), in combination with statin treatment : Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia. Atherosclerosis 261 : 144-152, 2017
18) Araki E et al : 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. Diabetes Care 41 : 538-546, 2018
P.155 掲載の参考文献
2) その他のリスク合併時の管理 糖尿病. 動脈硬化性疾患予防のための脂質異常症診療ガイド 2018年版, 日本動脈硬化学会編, 2018, pp77-78
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4) Araki E et al : 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. Diabetes Care 41 : 538-546, 2018
5) Matsuba I et al : Effects of a novel selective peroxisome proliferator-activated receptor-α modulator, pemafibrate, on hepatic and peripheral glucose uptake in patients with hypertriglyceridemia and insulin resistance. J Diabetes Investig 9 : 1323-1332, 2018
P.160 掲載の参考文献
1) Fujioka Y : Effects of a Novel Selective Peroxisome Proliferator-Activated Receptor α Modulator K-877 (Pemafibrate) on Postprandial Hyperlipidemia. J Atheroscler Thromb 25 : 126-127, 2018
2) Sairyo M et al : A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice. J Atheroscler Thromb 25 : 142-152, 2018
3) Ye P et al : Age-related decrease in expression of peroxisome proliferator-activated receptor alpha and its effects on development of dyslipidemia. Chin Med J (Engl) 118 : 1093-1098, 2005
4) Hennuyer N et al : The novel selective PPARα modulator (SPPARMα) pemafibrate improves dyslipidemia, enhances reverse cholesterol transport and decreases inflammation and atherosclerosis. Atherosclerosis 249 : 200-208, 2016
5) Raza-lqbal S et al : Transcriptome analysis of K-877 (a Novel Selective PPARα Modulator (SPPARMα)) -Regulated Genes in Primary Human Hepatocytes and the Mouse Liver. J Atheroscler Thromb 22 : 754-772, 2015
6) Ishibashi S et al : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, active- and placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
12) Roy A, Pahan K : PPARα signaling in the hippocampus : crosstalk between fat and memory. J Neuroimmune Pharmacol 10 : 30-34, 2015

5 SPPARMαのエビデンス

P.169 掲載の参考文献
1) Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease : the Scandinavian Simvastatin Survival Study (4S). Lancet 344 : 1383-1389, 1994
8) Rubins HB et al : Gemfibrozil for the secondary prevention of coronary heart disease in men with low levels of high-density lipoprotein cholesterol. Veterans Affairs High-Density Lipoprotein Cholesterol Intervention Trial Study Group. N Engl J Med 341 : 410-418, 1999
P.178 掲載の参考文献
13) Ishibashi S et al : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, active- and placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
14) Arai H et al : Efficacy and safety of K-877, a novel selective peroxisome proliferatoractivated receptor α modulator (SPPARMα), in combination with statin treatment : Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia. Atherosclerosis 261 : 144-152, 2017

6 トピックス

P.183 掲載の参考文献
P.190 掲載の参考文献
1) 日本動脈硬化学会編 : 動脈硬化性疾患予防ガイドライン 2017年版, 日本動脈硬化学会, 2017
10) Ishibashi S et al ; K-877-04 Study Group : Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients : A randomized, double blind, activeand placebo-controlled, phase 2 trial. Atherosclerosis 249 : 36-43, 2016
11) Sairyo M et al : A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice. J Atheroscler Thromb 25 : 142-152, 2018
P.197 掲載の参考文献
P.204 掲載の参考文献
5) Fruchart JC : Selective peroxisome proliferator-activated receptor α modulators (SPPARMα) : the next generation of peroxisome proliferator-activated receptor α-agonists. Cardiovasc Diabetol 12 : 82, 2013
7) Hennuyer N et al : The novel selective PPARα modulator (SPPARMα) pemafibrate improves dyslipidemia, enhances reverse cholesterol transport and decreases inflammation and atherosclerosis. Atherosclerosis 249 : 200-208, 2016
9) Yokote K et al : Long-Term Efficacy and Safety of Pemafibrate, a Novel Selective Peroxisome Proliferator-Activated Receptor-α Modulator (SPPARMα), in Dyslipidemic Patients with Renal Impairment. Int J Mol Sci 20 : pii : E706, 2019
19) Ishibashi S et al : Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor α modulator, in patients with dyslipidemia : Results from a 24-week, randomized, double blind, active-controlled, phase 3 trial. J Clin Lipidol 12 : 173-184, 2018
P.213 掲載の参考文献
5) Hiraike Y et al : NFIA co-localizes with PPARγ and transcriptionally controls the brown fat gene program. Nat Cell Biol 19 : 1081-1092, 2017
6) Ohno H et al : PPARγ agonists induce a white-to-brown fat conversion through stabilization of PRDM16 protein. Cell Metab 15 : 395-404, 2012
14) Valmaseda A et al : Opposite regulation of PPAR-α and -γ gene expression by both their ligands and retinoic acid in brown adipocytes. Mol Cell Endocrinol 154 : 101-109, 1999
15) Hondares E et al : Peroxisome proliferator-activated receptor α (PPARα) induces PPARγ coactivator 1α (PGC-1α) gene expression and contributes to thermogenic activation of brown fat : involvement of PRDM16. J Biol Chem 286 : 43112-43122, 2011
20) Defour M et al : The Peroxisome Proliferator-Activated Receptor α is dispensable for cold-induced adipose tissue browning in mice. Mol Metab 10 : 39-54, 2018
22) Araki M et al : The Peroxisome Proliferator-Activated Receptor α (PPARα) Agonist Pemafibrate Protects against Diet-Induced Obesity in Mice. Int J Mol Sci 19 : pii : E2148, 2018

7 SPPARMαの展望 - まとめに代えて

P.220 掲載の参考文献
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16) Takizawa T et al : Pharmacological effects of K-877, a potent and selective PPAR alpha modulator (SPPARM alpha) -Controlling the plasma HDL-C and triglycerides, and prevention of atherosclerosis in experimental animals. Eur Heart J 36 : 257-258, 2015 [ESC2015 Abstract]
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18) Konishi H et al : Abstract 15623 : Effect of pemafibrate (K-877), a novel selective peroxisome proliferator-activated receptor α modulator (SPPARMα), in atherosclerosis model using low density lipoprotein receptor knock-out swine with balloon injury. Circulation 136 : A15623, 2017 [AHA2017 Abstract]
19) Kockx M et al : Fibrates suppress fibrinogen gene expression in rodents via activation of the peroxisome proliferator-activated receptor-alpha. Blood 93 : 2991-2998, 1999

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