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These studies suggest that injections such as inclisiran, alirocumab, and other lipid-lowering drugs effectively reduce LDL cholesterol levels and improve cardiovascular outcomes in high-risk patients.
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Inclisiran is a novel small interfering RNA (siRNA) therapy designed to target PCSK9 messenger RNA, leading to reduced levels of low-density lipoprotein (LDL) cholesterol. Clinical trials have demonstrated its efficacy in significantly lowering LDL cholesterol levels in patients at high cardiovascular risk. In a phase 2 trial, patients receiving inclisiran experienced dose-dependent reductions in LDL cholesterol, with the most substantial decrease observed in those receiving two doses of 300 mg, achieving a reduction of up to 52.6% at 180 days. Additionally, inclisiran has shown promise in treating heterozygous familial hypercholesterolemia, with a phase 3 trial reporting a 47.9 percentage point reduction in LDL cholesterol levels compared to placebo. The safety profile of inclisiran is favorable, with injection-site reactions being the most common adverse event .
Alirocumab, a monoclonal antibody that inhibits PCSK9, has been shown to effectively reduce LDL cholesterol levels in patients already on statin therapy. In a randomized trial involving high-risk cardiovascular patients, alirocumab reduced LDL cholesterol levels by 62 percentage points compared to placebo at 24 weeks, with the effect sustained over 78 weeks. The study also indicated a potential reduction in major adverse cardiovascular events, although further research is needed to confirm these findings. Common side effects include injection-site reactions, myalgia, and neurocognitive events.
Sodium Tanshinone IIA Sulfonate (STS) is a traditional Chinese medicine injection that has demonstrated lipid-lowering effects in patients with coronary heart disease (CHD). A systematic review and meta-analysis of randomized clinical trials found that STS significantly reduced total cholesterol (TC), triglycerides (TG), and LDL cholesterol levels while increasing high-density lipoprotein (HDL) cholesterol levels. The safety profile of STS is acceptable, with no significant increase in adverse events reported.
Antisense oligonucleotide inhibitors, such as ISIS 301012, target apolipoprotein B (apoB) to reduce LDL cholesterol levels. A study involving volunteers with mild dyslipidemia showed that administration of ISIS 301012 resulted in a maximum 50% reduction in apoB and a 35% reduction in LDL cholesterol. The effects were sustained for up to three months post-treatment, although injection-site reactions were common.
Danhong Injection (DHI), another traditional Chinese medicine, has been studied for its effects on dyslipidemia and cholesterol metabolism. In high-fat diet-fed rats, DHI treatment significantly decreased levels of TC, TG, and LDL cholesterol while increasing HDL cholesterol. The study also noted improvements in liver function and oxidative stress markers, suggesting potential benefits for hyperlipidemia management.
Genistein and daidzein, isoflavones found in soybeans, have been investigated for their lipid-lowering effects. In middle-aged male rats, subcutaneous administration of these isoflavones significantly lowered TC and LDL cholesterol levels, with the higher doses showing the most pronounced effects. However, these treatments also increased triglyceride levels, indicating a need for further research to fully understand their impact on lipid metabolism.
In summary, various injectable therapies, including inclisiran, alirocumab, STS, antisense oligonucleotide inhibitors, DHI, and isoflavones, have shown significant potential in lowering LDL cholesterol levels and improving lipid profiles. Each therapy has its unique mechanism of action and safety profile, offering multiple options for patients who cannot achieve optimal LDL cholesterol levels with statins alone. Further research is needed to establish long-term safety and efficacy, particularly for newer treatments like inclisiran and antisense oligonucleotide inhibitors.
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