Esperion Announces Publication Of Definitive Paper On Bempedoic Acid Mechanism Of Action In Nature Communications
ANN ARBOR, Mich., Nov. 28, 2016 (GLOBE NEWSWIRE) -- Esperion Therapeutics, Inc. (NASDAQ:ESPR), a pharmaceutical company focused on developing and commercializing oral therapies for the treatment of patients with elevated low density lipoprotein cholesterol (LDL-C), today announced the publication of "Liver-specific ATP-citrate lyase inhibition by bempedoic acid decreases LDL-C and attenuates atherosclerosis," by Stephen L. Pinkosky et al. in Nature Communications, available at: http://www.nature.com/articles/ncomms13457. The paper systematically outlines the experiments and analyses undertaken by Esperion and its collaborators to fully understand the mechanism of action for how bempedoic acid reduces LDL-C.
Bempedoic acid is a pro-drug that requires activation to the CoA form to inhibit adenosine triphosphate (ATP) citrate lyase, an important enzyme on the cholesterol biosynthesis pathway. The specific enzyme required for this activation was identified as acetyl-CoA synthetase long chain 1 (ACSVL1), found in the liver but not found in skeletal muscle. Since bempedoic acid has no activity in skeletal muscle there is minimal risk for the muscle-related adverse events that have been associated with the use of statins.
Importantly, ATP citrate lyase (ACL) inhibition, mediated by bempedoic acid, results in decreased cholesterol biosynthesis, up regulation of LDL receptors, and reduction in LDL-C levels. In addition, bempedoic acid also reduced the progression of atherosclerosis in preclinical models.
"We are pleased that the research conducted by our scientific team on the liver-specific mechanism of action for bempedoic acid has been recognized in Nature Communications, a journal whose prestige speaks to the high quality of our science and research. Bempedoic acid targets ACL, the key differentiating feature of the molecule and has also been shown to complement the effects of statins, which target HMG-CoA reductase," said Tim Mayleben, president and chief executive officer of Esperion Therapeutics. "The publication of these results will provide the scientific and medical communities information to better understand both how bempedoic acid reduces elevated LDL-C, and why bempedoic acid appears to be associated with minimal risk for the muscle-related adverse events that have been associated with the use of statins."
About Bempedoic Acid
Bempedoic acid is a first-in-class ACL inhibitor that reduces cholesterol biosynthesis and lowers elevated levels of LDL-C by up-regulating the LDL receptor, but with reduced potential for muscle-related side effects. Completed Phase 1 and 2 studies in more than 800 patients treated with bempedoic acid have produced clinically relevant LDL-C lowering results of up to 30 percent as monotherapy, approximately 50 percent in combination with ezetimibe, and an incremental 20 to 22 percent when added to stable statin therapy.
Esperion's Commitment to Patients with Hypercholesterolemia
In the United States, 78 million people, or more than 20 percent of the population, have elevated LDL-C; an additional 73 million people in Europe and 30 million people in Japan also live with elevated LDL-C. Esperion's mission is to provide patients and physicians with a new oral therapy to significantly reduce elevated levels of LDL-C in patients inadequately treated with current lipid-modifying therapies. Esperion-discovered and developed, bempedoic acid is an oral LDL-C lowering therapy in Phase 3 development. The Company plans to develop bempedoic acid as a monotherapy as well as a fixed dose combination (FDC) with ezetimibe, with a particular focus on patients inadequately treated with current lipid-modifying therapies. It is estimated that approximately 5-20 percent of patients who are prescribed statins are only able to tolerate less than the lowest approved daily starting dose of their statin ("statin intolerant").
About Esperion Therapeutics
Esperion Therapeutics, Inc. is a pharmaceutical company focused on developing and commercializing oral therapies for the treatment of patients with elevated LDL-C. Through scientific and clinical excellence, and a deep understanding of cholesterol biology, the team at Esperion is committed to developing new LDL-C lowering therapies that will make a substantial impact on reducing global cardiovascular disease; the leading cause of death around the world. Bempedoic acid, the Company's lead product candidate, significantly reduces elevated LDL-C levels in patients with hypercholesterolemia, including patients inadequately treated with current lipid-modifying therapies. For more information, please visit www.esperion.com and follow us on Twitter at https://twitter.com/EsperionInc.
Bempedoic acid is a pro-drug that requires activation to the CoA form to inhibit adenosine triphosphate (ATP) citrate lyase, an important enzyme on the cholesterol biosynthesis pathway. The specific enzyme required for this activation was identified as acetyl-CoA synthetase long chain 1 (ACSVL1), found in the liver but not found in skeletal muscle. Since bempedoic acid has no activity in skeletal muscle there is minimal risk for the muscle-related adverse events that have been associated with the use of statins.
Importantly, ATP citrate lyase (ACL) inhibition, mediated by bempedoic acid, results in decreased cholesterol biosynthesis, up regulation of LDL receptors, and reduction in LDL-C levels. In addition, bempedoic acid also reduced the progression of atherosclerosis in preclinical models.
"We are pleased that the research conducted by our scientific team on the liver-specific mechanism of action for bempedoic acid has been recognized in Nature Communications, a journal whose prestige speaks to the high quality of our science and research. Bempedoic acid targets ACL, the key differentiating feature of the molecule and has also been shown to complement the effects of statins, which target HMG-CoA reductase," said Tim Mayleben, president and chief executive officer of Esperion Therapeutics. "The publication of these results will provide the scientific and medical communities information to better understand both how bempedoic acid reduces elevated LDL-C, and why bempedoic acid appears to be associated with minimal risk for the muscle-related adverse events that have been associated with the use of statins."
About Bempedoic Acid
Bempedoic acid is a first-in-class ACL inhibitor that reduces cholesterol biosynthesis and lowers elevated levels of LDL-C by up-regulating the LDL receptor, but with reduced potential for muscle-related side effects. Completed Phase 1 and 2 studies in more than 800 patients treated with bempedoic acid have produced clinically relevant LDL-C lowering results of up to 30 percent as monotherapy, approximately 50 percent in combination with ezetimibe, and an incremental 20 to 22 percent when added to stable statin therapy.
Esperion's Commitment to Patients with Hypercholesterolemia
In the United States, 78 million people, or more than 20 percent of the population, have elevated LDL-C; an additional 73 million people in Europe and 30 million people in Japan also live with elevated LDL-C. Esperion's mission is to provide patients and physicians with a new oral therapy to significantly reduce elevated levels of LDL-C in patients inadequately treated with current lipid-modifying therapies. Esperion-discovered and developed, bempedoic acid is an oral LDL-C lowering therapy in Phase 3 development. The Company plans to develop bempedoic acid as a monotherapy as well as a fixed dose combination (FDC) with ezetimibe, with a particular focus on patients inadequately treated with current lipid-modifying therapies. It is estimated that approximately 5-20 percent of patients who are prescribed statins are only able to tolerate less than the lowest approved daily starting dose of their statin ("statin intolerant").
About Esperion Therapeutics
Esperion Therapeutics, Inc. is a pharmaceutical company focused on developing and commercializing oral therapies for the treatment of patients with elevated LDL-C. Through scientific and clinical excellence, and a deep understanding of cholesterol biology, the team at Esperion is committed to developing new LDL-C lowering therapies that will make a substantial impact on reducing global cardiovascular disease; the leading cause of death around the world. Bempedoic acid, the Company's lead product candidate, significantly reduces elevated LDL-C levels in patients with hypercholesterolemia, including patients inadequately treated with current lipid-modifying therapies. For more information, please visit www.esperion.com and follow us on Twitter at https://twitter.com/EsperionInc.