New drug for cholesterol
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New Drug for Cholesterol: Emerging Therapeutics and Innovations
Oligonucleotide Therapeutics: siRNA-Based Drugs
A promising new class of cholesterol-lowering drugs involves small interfering RNA (siRNA) therapeutics. These drugs work by destroying RNA before it can synthesize proteins, effectively reducing cholesterol levels. One such siRNA drug is chemically modified and conjugated to trivalent N-acetylgalactosamine, which targets and degrades specific RNA sequences involved in cholesterol production .
Berberine: A Novel Mechanism
Berberine (BBR), a compound derived from a Chinese herb, has shown significant cholesterol-lowering effects. Clinical trials with hypercholesterolemic patients demonstrated that oral administration of BBR reduced serum cholesterol by 29%, triglycerides by 35%, and LDL-cholesterol by 25% over three months. The mechanism involves upregulating LDL receptor (LDLR) expression through ERK activation, independent of sterol regulatory element-binding proteins, and stabilizing LDLR mRNA.
PCSK9 Inhibitors: Monoclonal Antibodies
PCSK9 inhibitors represent a breakthrough in cholesterol management. These monoclonal antibodies inhibit the PCSK9 enzyme, which plays a crucial role in cholesterol metabolism. Clinical trials have shown that these inhibitors can reduce LDL cholesterol levels by up to 75% in patients already on statins, offering a potent alternative for those who cannot tolerate statins or need additional cholesterol reduction .
Inclisiran: siRNA Therapy
Inclisiran is another innovative siRNA-based drug that targets cholesterol. Administered via injection twice a year, inclisiran has shown promise in reducing LDL cholesterol levels in patients who are already on statins but still have elevated cholesterol. It is currently undergoing clinical trials and is expected to be available soon.
Emerging Lipid-Lowering Agents
Several other new drugs are being developed to target different aspects of lipid metabolism. These include:
- Lomitapide and Mipomersen: Targeting LDL cholesterol through different mechanisms than traditional statins.
- Bempedoic Acid: An ATP citrate lyase inhibitor that reduces cholesterol synthesis.
- Gemcabene: A drug that lowers both LDL cholesterol and triglycerides.
- Evinacumab and IONIS-ANGPTL3-LRx: Targeting both LDL cholesterol and triglycerides .
Conclusion
The landscape of cholesterol-lowering drugs is rapidly evolving with the introduction of novel therapeutics such as siRNA-based drugs, PCSK9 inhibitors, and compounds like berberine. These new drugs offer hope for patients who are resistant or intolerant to traditional statin therapy, providing more options to achieve optimal cholesterol levels and reduce cardiovascular risk.
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