DAIICHI-SANKYO

Daiichi Sankyo Europe GmbH (hereafter, ‘Daiichi Sankyo’) today announced results from two pooled analyses from four Phase 3 clinical trials for bempedoic acid and separate results from a Phase 2 study of the bempedoic acid / ezetimibe fixed dose combination (FDC). The data were presented at the American College of Cardiology’s 69^th Scientific Sessions Together with World Congress of Cardiology virtual experience (ACC.20/WCC).

The 12-week Phase 2 bempedoic acid / ezetimibe FDC study (also known as Study 058) enrolled adult patients with type 2 diabetes mellitus (T2DM) at high risk of cardiovascular disease.⁶ The bempedoic acid / ezetimibe FDC reduced LDL-C by 40% compared to placebo with no increase in glycated haemoglobin (HbA1c), indicating that glycaemic control was not adversely affected.⁶ The bempedoic acid / ezetimibe FDC was well tolerated in Study 058, and the incidence of adverse events rates were generally comparable to placebo.⁶

The first pooled analysis of four Phase 3 clinical trials investigating bempedoic acid in adult patients with hypercholesterolaemia demonstrated that bempedoic acid resulted in a significant lowering of LDL-C, in addition to other lipid measurements (total cholesterol, non-high-density lipoprotein cholesterol (HDL-C) apoliopoprotein B, HDL-C), regardless of the presence of background ezetimibe.⁷ The use of bempedoic acid with or without background ezetimibe therapy, was in the same range for overall incidence of treatment emergent adverse events (TEAEs) in both study arms.⁷

The second pooled analysis showed that bempedoic acid lowers high sensitivity C-reactive protein (hsCRP), a key marker of inflammation associated with cardiovascular disease, by 42% at 12 weeks in patients with hypercholesterolaemia, regardless of the presence or intensity of background statin therapy.⁸

“We are encouraged by all the data presented today that continue to demonstrate the potential benefit of bempedoic acid for adult patients who need to reduce their LDL-C levels in order to reduce their risk of a cardiovascular event such as a heart attack or stroke,” said Wolfgang Zierhut, MD, Head of Antithrombotic and Cardiovascular Medical Affairs Department at Daiichi Sankyo Europe. “There is a need to reduce LDL-C levels as identified in the most recent ESC/EAS guidelines and the Phase 2 data presented today showing the potential to lower LDL-C for people at particularly high risk due to their diabetes without impacting glycaemic control is promising to see, however we will need validation from larger studies. Additional lipid-lowering treatments are badly needed to support patients, and we hope to be able to make bempedoic acid available in Europe soon.”

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About bempedoic acid

With a unique mechanism of action, bempedoic acid is being developed as a first-in-class, affordable, oral treatment which lowers cholesterol, and which can be combined with other oral treatments to help lower cholesterol even further.^1,2,3,4 Bempedoic acid inhibits ATP citrate lyase (ACL), an enzyme which is involved in the production of cholesterol in the liver.^1,2,3,4

Bempedoic acid has received a positive CHMP recommendation for use in adults with primary hypercholesterolaemia (heterozygous familial and non-familial) or mixed dyslipidaemia, as an adjunct to diet:^1,2,3,4

• 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.

Bempedoic acid 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.⁹ Due to its novel mechanism of action, bempedoic acid is not activated in skeletal muscle.⁹

About bempedoic acid / ezetimibe

Bempedoic acid / ezetimibe is being developed as an oral treatment which combines two complementary ways of reducing cholesterol in a convenient once-daily tablet.⁵ Bempedoic acid / ezetimibe is a fixed dose combination tablet.⁵

Bempedoic acid / ezetimibe has received a positive CHMP recommendation 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 bempedoic acid and bempedoic acid / ezetimibe 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.

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¹ 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.
² Ray KK, et al . Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol. N Engl J Med . 2019; 380:1022–32.
³ 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.
⁴ 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.
⁵ 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.
⁶ Bays, HE, et al . Bempedoic acid 180 mg + ezetimibe 10 mg fixed dose combination drug product vs ezetimibe alone or placebo in patients with type 2 diabetes and hypercholesterolemia. Poster presentation at American College of Cardiology’s 69th Scientific Sessions Together with World Congress of Cardiology virtual experience (ACC.20/WCC). March 2020.
⁷ Catapano, AL, et al . Bempedoic acid efficacy and safety in patients at high-risk for CVD treated with or without ezetimibe: pooled analysis of 4 phase 3 clinical trials. Poster presentation at American College of Cardiology’s 69th Scientific Sessions Together with World Congress of Cardiology virtual experience (ACC.20/WCC). March 2020.
⁸ Stroes, ESG, et al . Factors influencing bempedoic acid-mediated reductions in high sensitivity c-reative protein: analysis of pooled patient-level data from 4 phase 3 clinical trials. Poster presentation at American College of Cardiology’s 69th Scientific Sessions Together with World Congress of Cardiology virtual experience (ACC.20/WCC). March 2020.
⁹ 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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