The first oral non statins cholesterol lowering drug in recent 20 years! Esperion's first ACL inhibitor, nexletol, has been approved by the US FDA!

The US Food and Drug Administration (FDA) has approved a new cholesterol lowering drug, nexletol (bempedoic), according to esperion therapeutics Acid, tablet), an oral, once-a-day, non statins, LDL-C-lowering drug, specific indications: as an adjuvant therapy of diet and maximum tolerated dose of statins, it is used to treat adult patients with heterozygous familial hypercholesterolemia (hefh) and atherosclerotic cardiovascular disease requiring further reduction of "bad" cholesterol (LDL-C) Adult patients with disease (ASCVD) Nexletol will be available in the US on March 30, 2020 In terms of medication, the recommended dose of nexletol is 180mg (1 tablet), which can be taken with or without food once a day After starting the treatment, the patients should analyze the blood lipid level within 8 to 12 weeks In particular, nexletol is the first oral, once a day, non statins cholesterol lowering drug approved in the United States in the past 20 years, which has a new mechanism of action in reducing LDL-C Currently, despite standard care (including statins), many patients are unable to achieve LDL-C goals The launch of nexletol will provide an important treatment option for patients with increased risk of cardiovascular disease due to hefh and ASCVD patients with increased LDL-C level LDL-C is a waxy fat like substance existing in human body Elevated LDL-C promotes the accumulation of LDL-C in arteries and may lead to cardiovascular events, including heart attacks and strokes Despite standard care, including statins, it is estimated that nearly 15 million patients (about a quarter of the patients) in the United States do not reach the LDL-C level recommended by the guidelines Nexletol is a first in class ATP citrate lyase (ACL) inhibitor It can reduce LDL-C by reducing cholesterol biosynthesis and up regulating LDL receptor Bempedoic acid is a synthetic dicarboxylic acid derivative, which is a precursor drug and needs the activation of acsvl1 Studies have shown that acsvl1 is absent in skeletal muscle Therefore, bempedoic acid will not be activated in skeletal muscle, which can avoid the muscular toxicity related to statins The approval of nexletol is supported by a global critical phase III clinical project The project includes a number of phase III clinical studies, involving more than 3000 patients In these studies, nexletol reduced LDL-C levels by 18% compared to placebo when combined with the most tolerable dose of statins Nexletol reduced LDL-C levels by 28% compared with placebo in patients with statin intolerance In addition, at the 12th week of treatment, nexletol also reduced the level of high-sensitivity C-reactive protein (hs CRP) by 19% - 22% relative to the baseline, which is a key marker of cardiovascular disease-related inflammation In patients with diabetes, nexletol reduced HbA1c by 0.2% compared with placebo In clinical studies, nexletol was well tolerated and the incidence of the most common adverse events was approximately the same as placebo The impact of Nexletol on incidence rate and mortality of cardiovascular disease has not been determined Esperion is conducting a global cardiovascular outcomes study clear outcomes, which is expected to obtain cardiovascular risk reduction data in 2022 At present, esperion's second cholesterol lowering drug bempedoic acid / ezetimibe is under review by the US FDA, and the results will be obtained on February 26 In January 2019, the first three companies purchased the commercial rights of bempedoic acid and bempedoic acid / ezymab compound tablets in Europe with a total of US $900 million At the end of January this year, the European Drug Administration (EMA) Committee on human pharmaceutical products (CHMP) issued a positive review, recommending approval of the two drugs for the treatment of hypercholesterolemia and mixed dyslipidemia CHMP's comments have been submitted to the European Commission (EC) for review, which will make a final review decision in April 2020.