Ezetimibe |
Inhibition of intestine cholesterol absorption |
- |
[24] |
Mipomersen |
ApoB synthesis inhibition |
Injection site reactions; Influenza-like symptoms; Fatty liver |
[61] |
Lomitapide |
Reduced secretion of apoB-containing lipoproteins by MTP inhibition |
Gastrointestinal tract diarrhea, nausea, vomiting, and dyspepsia; Fatty liver |
[70,71] |
Statins |
Reduced hepatic cholesterol synthesis and increased LDLR expression by blocking hepatic 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) |
Statin-associated muscle symptoms (myalgia, myopathy, and myositis with elevated creatinine kinase rhabdomyolysis) |
[62,69] |
Anti-PCSK9 monoclonal antibodies (mAbs) |
Blockade of circulating PCSK9 interaction with LDLR |
Injection site reactions |
[63] |
Bempedoic acid |
Reduced hepatic cholesterol synthesis and increased LDLR expression by blocking ATP-citrate lyase (ACLY) |
Elevated uric acid levels; Tendon rupture; Increased serum creatinine |
[59] |
Bile acid sequestrants |
Reduced bile acid reabsorption and increased fecal elimination |
Gastrointestinal side effects: constipation, bloating, abdominal discomfort, and aggravation of hemorrhoids |
[64,72] |
CETP inhibitors |
Inhibition of CETP |
Increase of plasma aldosterone and blood pressure |
[60] |
Squalene synthase inhibitors |
Reduced hepatic cholesterol synthesis and increased LDLR expression by blocking squalene synthase |
Acidosis; Elevation of alanine aminotransferase and total bilirubin |
[66,73] |
ASBT inhibitors |
Reduced bile acid reabsorption |
Abdominal pain and diarrhea |
[67] |