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Bempedoic acid to lower LDL Cholesterol

Posted on Friday March 29, 2024 in Heart Health

As a cardiologist, one of the most common challenges I encounter is managing high cholesterol levels in patients who are intolerant to statins due to muscle aches or other side effects. This has led to a significant need for alternative treatments that can effectively reduce cholesterol with fewer  associated peripheral side effects. Enter Bempedoic acid, a promising new player in the field of cholesterol-lowering medications which gets included in our locally developed pathways we use to guide treatment for patients who have  had a heart attack, acute coronary syndrome, stent, bypass operation or whose CT / FAI shows higher risk coronary heart disease.

Understanding Bempedoic Acid

Bempedoic acid, dosed at 180 mg once daily, represents a new frontier in the fight against high cholesterol. Unlike statins, which are the traditional go-to medications for lowering cholesterol, Bempedoic acid operates exclusively in the liver, avoiding the muscle-related side effects that some patients experience with statins. Bempedoic acid is part of a class of medicines known as adenosine triphosphate-citrate lyase (ACL) inhibitors. It’s a prodrug, meaning it’s activated only once it reaches the liver, transforming into its active form without affecting the muscles. This specificity allows Bempedoic acid to lower the production of cholesterol in the liver, akin to how statins work, but without the unwanted muscle interactions.

The Mechanism: How Does Bempedoic Acid Work?

The drug functions by inhibiting the enzyme adenosine triphosphate-citrate lyase (ACL). This inhibition leads to an increase in the expression of LDL receptors, enhancing the clearance of low-density lipoproteins (LDL-C) from the bloodstream. In simpler terms, it helps the liver pull more LDL cholesterol out of the blood, thereby lowering overall levels. Furthermore, Bempedoic acid, like statins, has an anti-inflammatory effect, primarily achieved through the activation of the AMPK pathway in immune cells. This action leads to a reduction in plasma levels of C-reactive protein, a marker of inflammation that is often elevated in cardiovascular diseases.

Clinical Benefits and Safety

In clinical trials, Bempedoic acid has shown a notable ability to reduce LDL cholesterol levels by approximately 20% when used alone. When combined with other lipid-lowering therapies like statins, ezetimibe, or PCSK9 inhibitors, it can help patients achieve their LDL cholesterol targets more effectively. The safety profile of Bempedoic acid is encouraging, with phase III clinical trials indicating that it is generally well-tolerated, whether used alone or in combination with other cholesterol-lowering medications. This is particularly significant for patients who are unable to tolerate statins or are seeking additional ways to control their cholesterol levels.

In summary, Bempedoic acid offers a new avenue for patients who require an alternative to statins for managing high cholesterol. Its liver-specific action and promising safety profile make it a valuable addition to the array of treatments available to combat high cholesterol levels and reduce the risk of cardiovascular diseases.

FAQ

What are the risks of bempedoic acid?

This medicine may increase the uric acid levels in the blood (hyperuricemia), which can lead to gout. This can occur within 4 weeks of using this medicine. Check with your doctor right away if you have joint pain, stiffness, or swelling, lower back, side, or stomach pain, or swelling of the feet or lower legs.
Bempedoic acid is associated with a low rate of mild, asymptomatic and self-limited serum aminotransferase elevations during therapy and to rare instances of clinically apparent acute liver injury. 

Does bempedoic acid cause weight gain?

Although bempedoic acid/ezetimibe has been shown to lower LDL-C levels, it will not help you lose weight, nor should you gain weight

References

  1. A Century of Cholesterol and Coronaries: From Plaques to Genes to Statins
  2. Bempedoic acid. Mechanism of action and pharmacokinetic and pharmacodynamic properties
  3. Mechanism of action and therapeutic use of bempedoic acid in atherosclerosis and metabolic syndrome
  4. Bempedoic Acid: Statin Alternative Helped Reduce Bad Cholesterol By 21%

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