[1] When in the bloodstream, 99.3% of the substance are bound to plasma proteins. [1], In the EU, bempedoic acid is indicated in adults with primary hypercholesterolaemia (heterozygous familial and non familial) or mixed dyslipidaemia, as an adjunct to diet in combination with a statin or statin with other lipid-lowering therapies in patients unable to reach LDL C goals with the maximum tolerated dose of a statin; or alone or in combination with other lipid-lowering therapies in patients who are statin intolerant, or for whom a statin is contraindicated. Lowering "bad" cholesterol may help to decrease the risk of heart … Nexletol (Bempedoic acid) is a prescription medicine used, along with diet and other lipid-lowering medicines, in the treatment of adults with heterozygous familial hypercholesterolemia (HeFH). [13], There were two clinical trials that evaluated the benefits and side effects of bempedoic acid. [3][2], In the US, bempedoic acid is indicated for the treatment of hypercholesterolemia in combination with diet and the highest tolerated statin therapy in adults with heterozygous familial hypercholesterolemia, or with established atherosclerotic cardiovascular disease, who need additional lowering of LDL cholesterol. [email protected] [1] Of ESP15228, 99.2% are bound to plasma proteins. [3][10][11][12] The U.S. Food and Drug Administration (FDA) granted the approval of Nexletol to Esperion Therapeutics. [13] The trials were conducted in United States, Canada, and Europe. [1], Bempedoic acid has a biological half-life of 21±11 hours. Copyright © 2003 - 2020 Canadian Pharmacy King. [1], The FDA approved bempedoic acid based on evidence from two clinical trials (Trial 1/ NCT02666664 and Trial 2/NCT02991118) of 3009 subjects with high LDL cholesterol and known atherosclerotic cardiovascular disease or HeFH. [13] The trial designs were similar. It is activated to the thioester with coenzyme A by the enzyme SLC27A2 in the liver. By inhibiting ACL, bempedoic acid suppresses cholesterol synthesis, 8 thereby triggering the upregulation of LDL receptor expression in the liver, resulting in increased clearance of LDL particles and lowering of LDL-cholesterol in the blood. [13], 8-Hydroxy-2,2,14,14-tetramethylpentadecanedioic acid, InChI=1S/C19H36O5/c1-18(2,16(21)22)13-9-5-7-11-15(20)12-8-6-10-14-19(3,4)17(23)24/h15,20H,5-14H2,1-4H3,(H,21,22)(H,23,24), Committee for Medicinal Products for Human Use, "Nexletol- bempedoic acid tablet, film coated", "Bempedoic Acid (ETC-1002): An Investigational Inhibitor of ATP Citrate Lyase", "Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol", "Bempedoic Acid a Small Molecule Drug Process and Synthesis, Innovation And /Or Advantages, Development Status And /Or Regulatory Status", "Esperion Announces FDA Approval of Nexletol (bempedoic acid) Tablet, an Oral, Once-Daily, Non-Statin LDL-Cholesterol Lowering Medicine", "FDA Approves Drug That Lowers Cholesterol in a New Way", "FDA approves first non-statin pill to treat high cholesterol in almost two decades", Magnesium pyridoxal 5-phosphate glutamate, https://en.wikipedia.org/w/index.php?title=Bempedoic_acid&oldid=984339755, Articles containing unverified chemical infoboxes, Articles containing potentially dated statements from March 2019, All articles containing potentially dated statements, Creative Commons Attribution-ShareAlike License, This page was last edited on 19 October 2020, at 16:13. This medication works in the liver by blocking an enzyme needed to make LDL. [2], Bempedoic acid was approved for use in the United States in February 2020, and for use in the European Union in April 2020. PHARMACY MANAGER: Mohammed Hassan [2], Common adverse effects in clinical trials were muscle spasms (3.6% of treated patients, as compared to 2.3% under placebo), pain in the back (3.3% versus 2.2%) or in a limb (3.0% versus 1.7%), gout (1.5% versus 0.4%), and gastrointestinal problems such as diarrhea. [1] About a fifth of the substance is reversibly converted by an aldo-keto reductase enzyme to a metabolite (called ESP15228) that is also pharmacologically active in form of its coenzyme A–thioester. Bempedoic acid was approved for use in the United States in February 2020, and for use in the European Union in April 2020. Bempedoic acid, sold under the brand name Nexletol among others, is a medication for the treatment of hypercholesterolemia. [1], In a study, it reduced LDL cholesterol by about 20 mg/dl compared to placebo and had no more side effects than placebo, although a higher percentage of drug receiving subjects dropped out of the study because of side effects (11% vs. 7% under placebo). Bempedoic acid is used along with a proper diet and other medications to help lower "bad" cholesterol (such as LDL) in the blood. [1], Bempedoic acid does not interact with the cytochrome P450 enzyme system in the liver and only weakly inhibits the transporter proteins SLCO1B1, SLCO1B3 and SLC22A7 (the latter possibly being responsible for the increase of uric acid in the blood, and therefore the adverse effect gout). If you have any question, please call our customer Nexletol (Bempedoic Acid) is used along with a proper diet and other lipid-lowering medications to treat high cholesterol. Can I take NEXLETOL with other medicines? HeFH is an inherited condition that causes high levels of “bad” cholesterol called low density lipoprotein (LDL).