Cholesterol-lowering injectable medications
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Overview of Cholesterol-Lowering Injectable Medications
Injectable cholesterol-lowering drugs have become important options for patients who cannot reach their cholesterol goals with oral medications like statins, or for those who are statin intolerant. These medications are especially useful for people at high risk for cardiovascular disease or with inherited cholesterol disorders 12.
Types of Injectable Cholesterol-Lowering Drugs
PCSK9 Inhibitors: Evolocumab, Alirocumab, and Ongericimab
PCSK9 inhibitors are monoclonal antibodies that block the PCSK9 protein, which leads to more LDL receptors on liver cells and greater removal of LDL cholesterol from the blood. Evolocumab and alirocumab are well-studied PCSK9 inhibitors. They are given as subcutaneous injections, usually every two weeks or once a month, and can lower LDL cholesterol by about 50-60% when added to statin therapy 1210. Ongericimab, a newer anti-PCSK9 antibody, has also shown strong LDL cholesterol reductions of over 70% in clinical trials, with a good safety profile .
Small Interfering RNA (siRNA) Therapy: Inclisiran
Inclisiran is a first-in-class siRNA therapy that works by blocking the production of PCSK9 in the liver. It is given as a subcutaneous injection twice a year after two initial doses. Clinical trials have shown that inclisiran can reduce LDL cholesterol by about 50% in patients with atherosclerotic cardiovascular disease or familial hypercholesterolemia, even when they are already on statins 4589. The most common side effect is mild injection site reactions, and overall safety is similar to placebo 489.
Antisense Oligonucleotides and Other Emerging Injectables
Other injectable drugs, such as mipomersen, volanesorsen, and drugs targeting angiopoietin-like protein 3 (like evinacumab), are being studied for their cholesterol-lowering effects. These drugs are less widely used and have less safety data, especially in patients with other health conditions . Mipomersen, for example, can cause liver-related side effects and injection site reactions .
Safety and Tolerability of Injectable Cholesterol-Lowering Drugs
PCSK9 inhibitors (evolocumab, alirocumab, and ongericimab) and inclisiran have shown good safety and tolerability in clinical trials. The most common side effects are mild injection site reactions, nasopharyngitis, joint pain, and back pain. Serious side effects are rare 127910. Mipomersen and similar drugs may have more side effects, such as liver enzyme increases and flu-like symptoms, and require more long-term safety data 12.
Physician and Patient Preferences
Physicians value the strong LDL cholesterol-lowering effect of injectable therapies, especially for patients who have trouble taking daily pills or have not reached their cholesterol goals with oral medications. Less frequent dosing, such as every six months with inclisiran, is preferred for patients with adherence issues . Cardiologists are more likely than primary care doctors to prefer injectable therapies over oral options .
Conclusion
Injectable cholesterol-lowering medications, including PCSK9 inhibitors (evolocumab, alirocumab, ongericimab) and siRNA therapy (inclisiran), offer effective and generally well-tolerated options for patients who need additional LDL cholesterol reduction beyond what statins can provide. These drugs are especially valuable for high-risk patients and those who struggle with daily medication adherence. Ongoing research will further clarify their long-term safety and impact on cardiovascular outcomes 12478910.
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