The Italian Medicines Agency has approved the reimbursement of the first-in-class treatment (first of its kind with this mechanism of action) of bempedoic acid and the fixed-dose combination of bempedoic acid and ezetimibe, for the treatment of adult patients whose blood LDL-cholesterol (C-Ld) levels remain too high despite taking such as statins and other lipid-lowering therapies. In Italy, bempedoic acid and its fixed-dose association with ezetimibe can be prescribed under a reimbursement regime through a prescription form. This was announced by Daiichi Sankyo, the Group that developed and marketed the new drug presented in Rome during the press conference “Add to reduce: bempedoic acid for those who do not reach the LDL-C targets”, held at the Luigi Sturzo Institute.
Up to 80% of patients affected by hypercholesterolemia – it emerged from the meeting – he fails to reach the Lld cholesterol targets recommended by the new international guidelines, despite taking lipid-lowering therapies, and remains at a greater risk of developing events such as heart attack or stroke. Hence the motto: “The lower the better: the lower a person’s LDL-C level, the lower their cardiovascular risk”.
The most recent guidelines for the management of dyslipidemia (ESC/EAS 2019) – reports a note – have revised the C-Ldl objectives indicating a target of <55mg/dL in very high risk patients and <70mg/dL for high risk patients. More than 80% of patients do not reach their LDL-C target despite taking treatments such as statins and other lipid-lowering therapies, resulting in an increase in risk of heart attack or stroke, responsible for 85% of deaths caused by atherosclerotic cardiovascular disease. In clinical trials involving over 4,000 patients at high and very high risk of cardiovascular events, bempedoic acid and its fixed-dose combination with ezetimibe have consistently demonstrated significant LDL-C reductions with a good tolerability profile. . Due to its specific mechanism of action, bempedoic acid is not activated in skeletal muscle, thus reducing the potential for muscle-related side effects such as myalgias.
“The accumulation of lipids in the blood vessel walls, especially those transported by LDL (the atherogenic lipoproteins par excellence) – he explains Marcello Arca, Past president of the Italian Society for the study of atherosclerosis (Sisa) – is capable of causing inflammation of the vessel, a process known as atherosclerosis. Atherosclerosis causes the formation of plaques, which become complicated and limit the flow of blood to the heart or brain, with consequences that can be fatal in some cases. The evidence is now clear and indisputable: LDL cholesterol is a direct and proven cause of events such as heart attacks, strokes and, therefore, also and death from ischemic cardiovascular disease. Consequentially, the latest ESC guidelines call for reducing LDL-C, the so-called bad cholesterol, as much as possible in high-risk people. The availability of bempedoic acid and the fixed combination of bempedoic acid and ezetimibe in Italy will provide important new treatment options to help patients achieve their LDL cholesterol goals.”
Bempedoic acid is a new oral treatment, first-in-class (first of its kind with this mechanism of action), to be taken once a day – details the note – which can be associated with other lipid-lowering treatments to further reduce C-LDL levels. The drug provides patients with an additional 17 to 28% reduction in LDL-C on top of maximally tolerated statins, with or without other oral lipid-lowering therapies. It has been observed in clinical trials an approximately 18% reduction in LDL-C with high-intensity statins and up to a 28% reduction in LDL-C in patients not taking statins. In contrast, the bempedoic acid/ezetimibe fixed combination demonstrated an approximately 38% reduction in LDL-C compared with placebo, when added to background lipid-lowering therapy.
It’s about a prodrug – it was reaffirmed during the presentation – that it acts on the well-known cholesterol synthesis process, upstream of the hepatic target of statins, by inhibiting a new molecular target: ATP citrate lyase (ACL), an enzyme involved in the production of cholesterol in the liver. The fixed-dose combination of bempedoic acid and ezetimibe is a new once-daily oral treatment that combines two complementary methods of lowering cholesterol into a single once-daily oral tablet. Bempedoic acid inhibits the production of cholesterol in the liver, while ezetimibe reduces the absorption of dietary cholesterol in the intestine. Due to its specific mode of action, bempedoic acid is not active in skeletal muscle, therefore it is not expected to cause muscle related undesirable effects such as myalgias.
Cardiovascular diseases are now the first cause of death in the world, with an estimated 17.9 million deaths each year, 85% of which are caused by heart attack or stroke. In Italy, cardiovascular diseases are responsible for 35.8% of all deaths (32.5% in men and 38.8% in women), exceeding 230,000 cases per year. In 2017 alone, 47,000 of deaths due to CVD were attributed to hypercholesterolemia.
“Daiichi Sankyo is pleased to make bempedoic acid and its fixed-dose combination with ezetimibe available to those who cannot get their LDL cholesterol levels under control,” he said. Joanne Jervis, Vice President European Customer Experience Daiichi Sankyo -. A unique treatment of its kind, to respond as always to the unsatisfied treatment needs, especially those of patients at the highest cardiovascular risk”, he concluded “But we continue to lavish our commitment also on campaigns and initiatives aimed at increasing patient awareness and specialists, because we deeply believe that to achieve our mission of improving patients’ quality of life, issues such as therapeutic adherence, primary and secondary prevention, are just as crucial as the development of innovative drugs”.
This drug – concludes the note – is subject to additional monitoring. Healthcare professionals are asked to report any suspected adverse reactions.