Bempedoic acid/Ezetimibe

The FDA approved label expansions for Esperion Therapeutics Nexletol and Nexlizet. Credit: grandbrothers via Shutterstock. Esperion Therapeutics declared that the US Food and Drug Administration (FDA) has approved a label expansion for two of its tablets, Nexletol (bempedoic acid) tablets and Nexlizet (bempedoic acid and ezetimibe). The two once-daily, oral tablets are now available for the reduction of cardiovascular risk and expanded low-density lipoprotein C (LDL-C) lowering in both primary and secondary prevention patients. The drugs can now also be used in combination with statins. The upgraded label also includes treatment for primary hyperlipidaemia, alone or in combination with a statin. The recent changes make Nexletol and Nexlizet the only approved LDL-C lowering non-statin drugs indicated for primary prevention patients, as per a 22 March company press release. The FDA first approved Nexletol in February 2020 for the treatment of hypercholesterolaemia based on data from two clinical trials (NCT02666664 and NCT02991118). The FDA approval was based on data from the Phase III CLEAR Outcomes study (NCT02993406), which assessed the use of the two bempedoic acid therapies on cardiovascular events. In the trial, data demonstrated that Nexletol and Nexlizet were both well-tolerated while reducing LDL-C by 20% and significantly reducing the risk of major adverse cardiovascular events compared to the placebo group. Esperion is also pursuing label expansions in Europe, recently receiving a positive recommendation from the European Medicines Agency’s (EMA) Committee for Medicinal Products for Human Use (CHMP) on 21 March. The Michigan-headquartered company forecasts an approval in Q2 2024. In the EU, Nexletol is under the brand name Nilemdo while Nexlizet is known as Nustendi. The EMA first approved the drug in January 2020. In addition, Esperion partnered with Daichi Sankyo for its EU development, amending their relationship earlier this year. See Also: Italfarmaco secures FDA approval for Duchenne muscular dystrophy drug Lisata clinches rare disease status for osteosarcoma drug The active ingredient of both therapies, bempedoic acid, is a prodrug that becomes activated in the liver. The drug lowers LDL-C through adenosine triphosphate-citrate lyase (ACL) inhibition.

Pictured: Gloved hand holding a specimen vial for an LDL-C test/iStock, Md Saiful Islam Khan Esperion secured broader-than-expected FDA labels for its cholesterol-busting drugs Friday, clearing the biotech to target 60 million more patients in the U.S. Shares of the company rose 23% to $2.82 in premarket trading. The previous labels for Nexletol (bempedoic acid) Tablets and Nexlizet (bempedoic acid and ezetimibe) limited use to the 10 million Americans with cardiovascular disease who are taking high-intensity statins but still need to lower their low-density lipoprotein cholesterol (LDL-C). Esperion filed to expand the label after generating data in an outcomes study. Esperion CEO Sheldon Koenig predicted last month that the label expansion could add 20 million patients to the population eligible for treatment with Nexletol and Nexlizet. The prediction was based on the belief that the FDA could authorize the drugs for use in patients who have diabetes, but not cardiovascular disease, who are on a low-dose statin and need further reductions in LDL-C. The labels given by the FDA support use in that population and another group of 40 million people. The third group covers people without cardiovascular disease who are unwilling to take statin therapy but need to lower their LDL-C. Collectively, the three groups cover 70 million patients, seven times as many people as Esperion was able to target under its old labels. Esperion compared the labels favorably to the restrictions on the use of the rival drugs Zetia (ezetimibe), Repatha (evolocumab), Praluent (alirocumab) and Leqvio (inclisiran). Nexletol and Nexlizet are the only drugs approved for use in the primary and secondary prevention of cardiovascular disease. Koenig said in a statement that the labels position the drugs as the “non-statins of first choice within the cardiovascular risk reduction treatment paradigm.” The next step is to leverage the expanded labels to drive sales. Esperion struggled to grow sales after winning approval in 2020, leading it to lay off 40% of its workforce in 2021. The expanded labels give the biotech a chance to relaunch the products in new patient populations and try to beat the $78.3 million in U.S. net product revenue it reported last year. Esperion is planning a “bold new consumer campaign” to activate its target patients and support growth of the products. The company also grew its sales team in anticipation of the label expansion. Koenig said last month that the addition of 60 new territory managers had grown the team to 150 representatives. Nick Paul Taylor is a freelance pharmaceutical and biotech writer based in London. He can be reached on LinkedIn.