Nexletol, also known as bempedoic acid, works by inhibiting cholesterol synthesis [1]. It targets ATP-citrate lyase (ACL), an enzyme upstream of HMG-CoA reductase, which is the target of statins [1][2]. By blocking ACL, Nexletol reduces the production of cholesterol in the liver [1]. This reduction in liver cholesterol leads to an upregulation of low-density lipoprotein receptors on liver cells, which in turn increases the clearance of LDL cholesterol from the bloodstream [1].
How does Nexletol lower cholesterol?
Nexletol lowers LDL cholesterol by specifically inhibiting the ATP-citrate lyase (ACL) enzyme in the liver [1][2]. This enzyme is responsible for synthesizing cholesterol, and its inhibition leads to decreased cholesterol production within liver cells [1]. Consequently, the liver increases the number of LDL receptors on its surface to draw more LDL cholesterol from the blood, thereby reducing circulating LDL levels [1].
What is the difference between Nexletol and statins?
The primary difference lies in their mechanism of action. Statins inhibit HMG-CoA reductase, another enzyme involved in cholesterol synthesis, but further down the pathway than ACL [1][2]. Nexletol targets ACL, an earlier step in cholesterol production [1][2]. This distinct mechanism may offer a benefit for patients who are statin-intolerant or for whom statins are not sufficiently effective [3].
When will Nexletol patents expire?
Information regarding Nexletol's patent expiration is available through resources like DrugPatentWatch.com [4]. Understanding patent timelines is crucial for predicting the potential market entry of generic or biosimilar versions of the drug.
What are the clinical trial results for Nexletol?
Clinical trials have demonstrated that Nexletol, when added to maximally tolerated statin therapy, significantly reduces LDL cholesterol levels [1][3]. Studies such as the CLEAR Outcomes trial have shown a reduction in major adverse cardiovascular events in patients treated with bempedoic acid [5].
Who manufactures Nexletol?
Nexletol is manufactured by Esperion Therapeutics [6].
What side effects have been reported for Nexletol?
Commonly reported side effects of Nexletol include hyperuricemia, muscle spasms, back pain, and abdominal discomfort [1]. Elevated levels of liver enzymes have also been observed in some patients [1].
Can Nexletol be used with other cholesterol-lowering medications?
Nexletol is indicated for use in adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular disease who require additional LDL-C lowering and are on maximally tolerated statin therapy [1]. It is designed to be used as an add-on therapy [1].
Sources:
[1] https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213047lbl.pdf
[2] https://www.drugpatentwatch.com/blog/nexletol-mechanism-of-action/
[3] https://www.drugpatentwatch.com/drugs/bempedoic-acid
[4] https://www.drugpatentwatch.com/drugs/bempedoic-acid
[5] https://www.nejm.org/doi/full/10.1056/NEJMoa2213070
[6] https://www.esperion.com/