Cholesterol lowering injectable medications
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Overview of Injectable Cholesterol-Lowering 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 of cardiovascular disease or with inherited forms of high cholesterol 128.
Types of Injectable Cholesterol-Lowering Drugs
PCSK9 Inhibitors: Evolocumab and Alirocumab
PCSK9 inhibitors, such as evolocumab and alirocumab, are monoclonal antibodies that block the PCSK9 protein, which normally reduces the number of LDL receptors in the liver. By blocking PCSK9, these drugs increase the liver’s ability to remove LDL cholesterol from the blood. They are approved for patients with familial hypercholesterolemia and those with cardiovascular disease who need additional cholesterol lowering 128. Clinical trials show these drugs can lower LDL cholesterol by 30–50% and are generally well tolerated, with side effects mostly limited to mild injection-site reactions, nasopharyngitis, joint pain, and back pain 12.
Small Interfering RNA (siRNA) Therapy: Inclisiran
Inclisiran is a newer injectable drug that uses small interfering RNA to block the production of PCSK9 in the liver. It is given as a subcutaneous injection twice a year after two initial doses. Inclisiran is approved for adults with atherosclerotic cardiovascular disease or heterozygous familial hypercholesterolemia who need further LDL cholesterol reduction despite maximally tolerated statin therapy 56910. Clinical trials have shown that inclisiran can reduce LDL cholesterol by about 40–52% compared to placebo, with a safety profile similar to placebo except for mild injection-site reactions 56910. Long-term safety and effects on cardiovascular outcomes are still being studied 910.
Other Injectable Agents
Other injectable agents include antisense oligonucleotides (such as mipomersen) and drugs targeting angiopoietin-like protein 3 (like evinacumab). These are less commonly used and have less extensive safety data, especially in patients with other health conditions or those taking multiple medications . Mipomersen, for example, can cause liver-related side effects and injection-site reactions .
Physician and Patient Preferences
Physicians, especially cardiologists, often prefer injectable therapies for patients who have trouble adhering to daily oral medications. Less frequent dosing, such as twice-yearly injections with inclisiran, is seen as an advantage for improving adherence in real-world practice . Efficacy in lowering LDL cholesterol is the most important factor for prescribers, but cost and side effects are also considered .
Safety and Tolerability
Overall, injectable cholesterol-lowering drugs like PCSK9 inhibitors and inclisiran have shown favorable safety and tolerability profiles in clinical trials. The most common side effects are mild and include injection-site reactions, with serious side effects being rare 12910. Long-term safety data are still being collected, especially for newer agents like inclisiran 910.
Conclusion
Injectable cholesterol-lowering medications, including PCSK9 inhibitors and inclisiran, offer effective and generally well-tolerated options for patients who need additional LDL cholesterol reduction beyond what oral medications can provide. These drugs are especially valuable for high-risk patients and those with adherence challenges, and ongoing studies will further clarify their long-term safety and impact on cardiovascular outcomes 125678910.
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