New first-in-class cholesterol-lowering treatment NILEMDO® and its combination with ezetimibe NUSTENDI® approved in Europe

Daiichi Sankyo Europe GmbH (hereafter, ‘Daiichi Sankyo’) today announced that the European Commission (EC) has approved both NILEMDO^® (bempedoic acid) and NUSTENDI^®(bempedoic acid / ezetimibe) for use in adults with primary hypercholesterolaemia or mixed dyslipidaemia in Europe.^4,5 Bempedoic acid has a unique mechanism of action which is complementary to statins and other lipid-lowering therapies (LLTs) allowing additional LDL-C lowering on top of other LLTs compared to placebo.⁶ Both approvals were supported by data from the CLEAR trial programme conducted in more than 4,000 high- and very high-risk patients.^6-10

“Across Europe, cardiovascular disease is one of the major causes of death killing more than four million people every year. High LDL-C is one of the major causes for heart attacks, strokes and other events that can lead to death,” said Professor Alberico L. Catapano, Chairperson of the guidelines Task Force and Professor of Pharmacology at the Department of Pharmacological and Biomolecular Sciences, University of Milan, Italy. “ESC/EAS Guidelines recommend intensively lowering LDL-C to reduce cardiovascular risk. The approval of bempedoic acid and its fixed dose combination with ezetimibe gives us important new treatment options that can be combined with other lipid-lowering treatments to help reduce LDL-C in people at risk of events like heart attacks and strokes.”

NILEMDO^® is a new, first-in-class, affordable, oral treatment which lowers cholesterol, and can be combined with other oral treatments to help lower cholesterol even further. It provides additional LDL-C lowering of up to 28% on top of other lipid-lowering therapies, compared to placebo by inhibiting ATP Citrate Lyase (ACL), an enzyme in the well-known cholesterol synthesis pathway, upstream of the statin target in the liver.^4,9

NUSTENDI^®is a fixed dose combination tablet of bempedoic acid and ezetimibe which combines two complementary ways of reducing cholesterol in a convenient, once-daily, oral treatment with the potential to support adherence to treatment by reducing pill burden for patients. Bempedoic acid inhibits cholesterol production in the liver while ezetimibe reduces absorption of dietary cholesterol in the gut.^8,11 In a Phase 3 clinical trial NUSTENDI^® reduced LDL-C by 38% compared to placebo in high-risk patients already taking maximum-tolerated statin therapy.⁸

A combined safety analysis in more than 3,600 patients confirms that bempedoic acid is well tolerated, and overall adverse event rates were similar to placebo.¹² Due to its novel mechanism of action, NILEMDO^® is not activated in skeletal muscle which decreases the potential for muscle-related adverse effects.^4,13

Up to 80% of patients do not reach guideline-recommended LDL-C goals despite receiving treatments such as statins, and are at increased risk of a heart attack or stroke.^1,2,3

“Due to the limitations of existing lipid-lowering therapies, the need for additional add-on treatments remains to help people reach their LDL-C goals and to reduce cardiovascular risk,” said Benoit Creveau, Head of Cardiovascular Marketing at Daiichi Sankyo Europe. “NILEMDO^® and NUSTENDI^® can be added to existing, oral lipid-lowering therapies and will help HCPs and their patients at high- and very high-risk to take back control. The approval of NILEMDO^® and NUSTENDI^® in Europe is a key milestone for us at Daiichi Sankyo Europe and reflects our ongoing commitment to reducing the burden of cardiovascular disease.”

- ENDS –

About NILEMDO^®
With a unique mechanism of action, NILEMDO^® is a new, first-in-class, affordable, oral treatment which lowers cholesterol, and which can be combined with other oral treatments to help lower cholesterol even further.⁴ Bempedoic acid inhibits ATP citrate lyase (ACL), an enzyme which is involved in the production of cholesterol in the liver.⁴

NILEMDO^® has been approved for use in adults with primary hypercholesterolaemia (heterozygous familial and non-familial) or mixed dyslipidaemia, as an adjunct to diet:⁴

• 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.

NILEMDO^® acts on the well-known cholesterol synthesis pathway, upstream of the statin target in the liver, with a unique mechanism of action which allows additional LDL-C lowering when added to statin treatment.⁴ Due to its novel mechanism of action, NILEMDO^® is not activated in skeletal muscle.⁴

About NUSTENDI^®
NUSTENDI^® is a new oral treatment which combines two complementary ways of reducing cholesterol in a convenient once-daily tablet. NUSTENDI^® is a fixed dose combination tablet containing bempedoic acid (the active pharmaceutical ingredient in NILEMDO^®) and ezetimibe.⁵

NUSTENDI^® has been approved for use in adults with primary hypercholesterolaemia (heterozygous familial and non-familial) or mixed dyslipidaemia, as an adjunct to diet:⁵

• in combination with a statin in patients unable to reach LDL-C goals with the maximum tolerated dose of a statin in addition to ezetimibe,
• alone in patients who are either statin-intolerant or for whom a statin is contraindicated, and are unable to reach LDL-C goals with ezetimibe alone,
• in patients already being treated with the combination of bempedoic acid and ezetimibe as separate tablets with or without a statin.

Daiichi Sankyo Europe has licensed exclusive commercialisation rights to these products in the European Economic Area and Switzerland from Esperion. Through scientific and clinical excellence, and a deep understanding of cholesterol biology, the experienced Lipid Management Team at Esperion is committed to developing new LDL-C lowering medicines that will make a substantial impact on reducing global cardiovascular disease, the leading cause of death around the world.

About Daiichi Sankyo
Daiichi Sankyo Group is dedicated to the creation and supply of innovative pharmaceutical therapies to improve standards of care and address diversified, unmet medical needs of people globally by leveraging our world-class science and technology. With more than 100 years of scientific expertise and a presence in more than 20 countries, Daiichi Sankyo and its 15,000 employees around the world draw upon a rich legacy of innovation and a robust pipeline of promising new medicines to help people. In addition to a strong portfolio of medicines for cardiovascular diseases, under the Group’s 2025 Vision to become a “Global Pharma Innovator with Competitive Advantage in Oncology,” Daiichi Sankyo is primarily focused on providing novel therapies in oncology, as well as other research areas centred around rare diseases and immune disorders. For more information, please visit: www.daiichisankyo.com.

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1 ESC/EAS Guidelines for the management of dyslipidaemias. Eur Heart J. 2020 Jan 1;41(1):111-188 doi:10.1093/eurheartj/ehz455.

2 Fox KM, et al. Treatment patterns and low-density lipoprotein cholesterol (LDL-C) goal attainment among patients receiving high- or moderate-intensity statins. Clin Res Cardiol 2018; 107: 380–388.

3 Kotseva K, et al. Lifestyle and impact on cardiovascular risk factor control in coronary patients across 27 countries: Results from the European Society of Cardiology ESC-EORP EUROASPIRE V registry. Eur J Prev Cardio. 2019;26(8):824–835.

4 European Medicines Agency. Nilemdo® Summary of Product Characteristics. March 2020.

5 European Medicines Agency. Nustendi® Summary of Product Characteristics. March 2020.

6 Laufs U, et al. Efficacy and Safety of Bempedoic Acid in Patients with Hypercholesterolemia and Statin Intolerance. J Am Heart Assoc. 2019;8(7):e011662.

7 Goldberg AC, et al. Effect of Bempedoic Acid vs Placebo Added to Maximally Tolerated Statins on Low-Density Lipoprotein Cholesterol in Patients at High Risk for Cardiovascular Disease. The CLEAR Wisdom Randomized Clinical Trial. JAMA. 2019;322(18):1780–1788. doi:10.1001/jama.2019.16585.

8 Ballantyne, CM, et al. Bempedoic acid plus ezetimibe fixed-dose combination in patients with hypercholesterolemia and high CVD risk treated with maximally tolerated statin therapy. Eur J Prev Cardiol. 2019; doi 10.1177/2047487319864671.

9 Ballantyne CM, et al. Efficacy and safety of bempedoic acid added to ezetimibe in statin-intolerant patients with hypercholesterolemia: A randomized, placebo-controlled study. Atherosclerosis. 2018;277:195–203.

10 Ray KK, et al. Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol. N Engl J Med. 2019; 380:1022–32.

11 Phan BAP et al. Ezetimibe therapy: mechanism of action and clinical update. Vascular Health and Risk Management 2012:8 415–427.

12 Ballantyne, CM, et al. Safety profile of bempedoic acid: pooled analysis of 4 phase 3 clinical trials. Abstract: P5364.

13 Pinkosky SL, et al. Liver- specific ATP-citrate lyase inhibition by bempedoic acid decreases LDL-C and attenuates atherosclerosis. Nature Communications. 2016; 7:13457. DOI:10.1038/ncomms13457.

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Contact information

Lydia Worms (Europe)
Daiichi Sankyo Europe GmbH
Communications & Product PR Europe
+49 (89) 7808751