2017
DOI: 10.1007/s40265-017-0818-x View full text |Buy / Rent full text
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Abstract: 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 th… Show more

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“…The biphasic dose response, which was not clear in fenofibrate treatment to the best of our knowledge, may be related to the fact that LY518674 and pemafibrate are both more potent and selective PPARa agonists than fenofibrate (16,27). Pemafibrate is primarily eliminated via the liver, whereas fenofibrate and gemfibrozil are eliminated via kidneys (26,28). The above-mentioned differences may be, at least in part, associated with different responses in several clinical laboratory tests.…”
Section: Discussionmentioning
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“…The biphasic dose response, which was not clear in fenofibrate treatment to the best of our knowledge, may be related to the fact that LY518674 and pemafibrate are both more potent and selective PPARa agonists than fenofibrate (16,27). Pemafibrate is primarily eliminated via the liver, whereas fenofibrate and gemfibrozil are eliminated via kidneys (26,28). The above-mentioned differences may be, at least in part, associated with different responses in several clinical laboratory tests.…”
Section: Discussionmentioning
“…no. NCT03071692) (26). The biphasic dose response, which was not clear in fenofibrate treatment to the best of our knowledge, may be related to the fact that LY518674 and pemafibrate are both more potent and selective PPARa agonists than fenofibrate (16,27).…”
Section: Discussionmentioning
“…However, a SPPARMα, pemafibrate, is mainly metabolized in the liver and almost exclusively excreted from the liver, with only 14.5% excretion in the urine [91]. The main metabolites of pemafibrate in plasma are benzyl oxidized oxidant and a mixture of glucuronic acid conjugate and N-dealkylated dicarboxylic acid [92]. Excretion rate of unmetabolized pemafibrate into urine is < 0.5%, and almost all the metabolized compounds excreted in the urine have no PPARα agonist activity.…”
Section: Pemafibrate For Patients With Chronic Kidney Disease (Ckd)mentioning
“…Pemafibrate (formerly known as K-877) is one of the newest members of the selective PPAR-α modulators, being >2000-fold more selective for PPAR-α vs. either PPAR-γ or -δ (delta) [ 72 ]. Pemafibrate has been recently approved in Japan for the treatment of hyperlipidemias, with a recommended dosage of 0.1 mg bid with the possibility of reaching a maximum of 0.2 mg bid [ 73 ].…”
Section: Ppar-α: Fibrates and Omega-3 Fatty Acids In The Metabolicmentioning