New mechanism cholesterol lowering drugs! FDA approved two innovative drugs (nexletol, nexlizet) of esperion in one week!

February 27, 2020 / BIOON / -- expression therapeutics recently announced that the U.S Food and Drug Administration (FDA) has approved nexlizet (bexpedoic acid / ezetimibe, 180mg / 10mg, tablet), which is the FDA obtained by the company after nexletol (bexpedoic acid, 180mg, tablet) last week A second approved cholesterol lowering drug, both oral, once a day, non statins, LDL-C lowering drugs, with the same indications: as an adjuvant therapy of diet and maximum tolerated dose of statins, for the treatment of adults with heterozygous familial hypercholesterolemia (hefh), and for further reduction of "bad" cholesterol (LDL-C) levels Adult patients with atherosclerotic cardiovascular disease (ASCVD) The two drugs will be launched in the United States on March 30, 2020 It is recommended to take one tablet daily, with or without food It is worth mentioning that nexlizet is the first non statins and cholesterol lowering (LDL-C) compound drug approved by the regulatory authority; nexletol is the first oral, once a day, non statins and cholesterol lowering (LDL-C) drug approved by the regulatory authority 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 these two drugs 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 The active components of nexlizet are bempedoic acid and ezetimibe, which can reduce LDL-C by inhibiting the complementary mechanism of liver cholesterol synthesis and intestinal absorption 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 approval of nexlizet was supported by a phase III clinical project of fixed combination drug products, as well as the safety data from nexletol global key phase III project and the existing safety data of ezemeb The study showed that nexlizet reduced LDL-C by 38% (95% CI: - 47%, - 30%; P < 0.001) compared with placebo when combined with the maximum tolerated dose of statins The impact of Nexletol and Nexlizet 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 In January 2019, the first three acquired the commercialized rights of nexletol and nexlizet in Europe for 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 (bio Com) original source: assertion announcements FDA approval of the nexsize (bempedoic acid and ezetimibe) tablet, an oral, once daily, non station LDL cholesterol lowing medicine