Injectable cholesterol lowering drugs
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Overview of Injectable Cholesterol Lowering Drugs
Injectable cholesterol-lowering drugs have become important options for patients who cannot reach their cholesterol goals with statins alone or who are statin intolerant. These drugs are especially useful for people at high risk for cardiovascular disease or with inherited forms of high cholesterol 126.
Types of Injectable Lipid-Lowering Therapies
PCSK9 Inhibitors: Evolocumab, Alirocumab, and Ongericimab
PCSK9 inhibitors, such as evolocumab and alirocumab, are monoclonal antibodies that block the PCSK9 protein, which leads to increased removal of LDL cholesterol from the blood. These drugs are approved for patients with familial hypercholesterolemia and those with cardiovascular disease who need additional cholesterol lowering 126. Ongericimab, another anti-PCSK9 antibody, has shown significant LDL cholesterol reduction (over 70%) and is well tolerated, with similar safety profiles whether administered by prefilled syringe or autoinjector .
Small Interfering RNA (siRNA) Therapies: Inclisiran
Inclisiran is a novel siRNA drug that reduces the production of PCSK9 in the liver, leading to lower LDL cholesterol levels. It is administered as a subcutaneous injection twice a year after two initial doses 45810. Clinical trials have shown that inclisiran can reduce LDL cholesterol by 40–51% in patients with atherosclerotic cardiovascular disease or familial hypercholesterolemia, with a safety profile similar to placebo 4510. Common side effects include injection site reactions, joint stiffness, and mild infections 45.
Antisense Oligonucleotides: Mipomersen and Others
Mipomersen is an antisense oligonucleotide that targets apolipoprotein B100 mRNA, reducing LDL cholesterol. However, its use is associated with liver-related side effects, such as increased liver fat and elevated liver enzymes, as well as injection site reactions and flu-like symptoms. Long-term safety data are still needed 12.
Other Emerging Injectable Agents
Other injectable drugs targeting angiopoietin-like protein 3 (such as evinacumab and IONIS-ANGPTL3Rx) and additional antisense oligonucleotides are being studied, but their safety and efficacy profiles are less well established, especially in patients with multiple health conditions .
Safety and Tolerability of Injectable Cholesterol Drugs
PCSK9 inhibitors (evolocumab, alirocumab, and ongericimab) and inclisiran have demonstrated good safety and tolerability in clinical trials, with most side effects being mild and related to the injection site 12459. Mipomersen and similar drugs require more long-term safety data, particularly regarding liver effects 12.
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 beneficial for improving adherence in real-world practice 710. Efficacy in lowering LDL cholesterol remains the most important factor for prescribing decisions, but cost and convenience also play significant roles .
Conclusion
Injectable cholesterol-lowering drugs, including PCSK9 inhibitors, siRNA therapies like inclisiran, and antisense oligonucleotides, offer effective and generally well-tolerated options for patients who need additional LDL cholesterol reduction beyond what statins can provide. These therapies are especially valuable for high-risk patients and those with adherence challenges. Ongoing research will further clarify their long-term safety, cost-effectiveness, and best use in clinical practice 12456789+1 MORE.
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