The Latest Medications to Lower LDL

Health Writer

Today’s drug research is informed by genomic advances that are contributing to the creation of personalized therapies for many disorders, including high LDL, the bad cholesterol that increases risk for heart attack and stroke. Statins have long been the drug of choice to reduce LDL cholesterol. While statins are effective for many people, they don’t work well for everyone. Some people experience unpleasant side effects and need an alternative to statins. The American College of Cardiology (ACC) and the American Heart Association (AHA) published a report on the use of newer non-statin LDL-reducing therapies that have emerged in the last decade. We’ve researched them, and we want to help you understand what they are, how they work, and what side effects might occur.


Ezetimibe inhibits the action of a specific protein, reducing the amount of cholesterol absorption in the small intestine. Ezetimibe can be taken alone or along with a statin. Adverse effects may include upper respiratory infection, diarrhea, joint pain, sinusitis, and pain in the hands and feet. If taken with a statin, side effects may include cold-like symptoms and muscle pain.

PCSK9 inhibitors

PCSK9 inhibitors are an injectable drug that blocks the receptors that pull LDL out of blood. Remember that oil (LDL) and water (blood) don’t mix. PCSK9 inhibitors, which allow receptors to pull LDL from blood, include evolocumab and alirocumab. They are given alone or along with statins. Adverse effects may include cold-like symptoms, upper respiratory infection, influenza, injection site reactions, and back pain. An advantage of the PCSK9 inhibitors is that they don’t cause the muscle problems experienced by some statin users.

Bile acid sequestrants (binders)

Bile-acid binders prevent them from entering into the bloodstream. As bile acids decrease, the liver generates more LDL receptors. That’s good because the receptors latch onto LDL and pull it out of the bloodstream. Bile acid binders include cholestyramine, colestipol, and colesevelam. They are given as an adjunct to improved diet and exercise, and the last one, colesevelam, may be used with a statin. Possible adverse effects are constipation, indigestion, and nausea.

Injectable drugs for people with HoFHPeople with high LDL may have a history of familial hypercholesterolemia (HoFH), which makes them eligible for two injectable medications.** Mipomersen** is injected weekly in people with confirmed HoFH. The drug targets a protein encoded by the APOB gene. Adverse effects may include injection site reactions, flu-like symptoms, nausea, headache, and elevated ALT, which can indicate liver injury.

Lomitapide is another injectable drug that is given as an adjunct to a low-fat diet for people with HoFH. The drug inhibits microsomal triglyceride transfer protein (MTP/MTTP), blocking components needed to make cholesterol. The result is less LDL in the bloodstream. Side effects may include diarrhea, nausea, vomiting, indigestion, and abdominal pain.

How do you decide what to take?

Start by consulting with a board-certified doctor to obtain cholesterol levels and determine risk for heart attack and stroke. The exam will include blood work and personal and family history. The doctor’s visit is the best time to ask questions, so make a list ahead of time and take notes during the consultation. Take prescribed medication as directed. If side effects occur, tell your doctor before stopping the medication.