Genetics, Safety, Cost-Effectiveness, and Accessibility of Injectable Lipid-Lowering Agents: A Narrative Review
Table 1
Comparison of different lipid-lowering agents in terms of mode of action and safety consideration.
Drug class
Agent
Mechanism of action
Safety consideration
Cholesterol absorption inhibitor
Ezetimibe
Blocks the absorption of cholesterol and decreased delivery of intestinal cholesterol to the liver which results in increased cholesterol clearance
Generally well-tolerated with a low incidence of side effects Rare cases of serious allergic reactions have been reported
PCSK9 inhibitor
Alirocumab
Inhibits PCSK9 binding to LDL-Rs resulting in increased cholesterol clearance
Generally well-tolerated with a low incidence of side effects May cause injection-site reactions, such as redness or swelling In some patients, it may increase the risk of neurocognitive events, such as memory loss or confusion
Evolocumab
siRNA (small interfering RNA) therapy
Inclisiran
Targets the messenger RNA (mRNA) for PCSK9, reducing the amount of PCSK9 protein available to regulate LDL receptor levels. This results in lowered LDL cholesterol levels
Generally well-tolerated with a low incidence of side effects Injection-site reactions are the most commonly reported side effect May cause liver enzyme elevations, so liver function tests may need to be monitored periodically
Antisense oligonucleotide therapy
Mipomersen
Binds to and inhibits the production of apolipoprotein B-100, a protein that is an essential component of LDL cholesterol. This results in lowered levels of LDL cholesterol in the bloodstream
Can cause injection-site reactions, such as redness, swelling, or pain. May cause liver enzyme elevations and increase the risk of liver damage, so liver function tests may need to be monitored periodically. Can cause flu-like symptoms, such as fever, chills, and fatigue
Vaccines
Anti-PCSK9 vaccines
Stimulates the immune system to produce antibodies that target and neutralize PCSK9, resulting in lower LDL cholesterol levels
