Repatha drug classification
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Repatha Drug Classification
Introduction to Repatha (Evolocumab)
Repatha, also known by its generic name evolocumab, is a fully human monoclonal antibody developed by Amgen. It is primarily used for the treatment of hypercholesterolemia, a condition characterized by high levels of cholesterol in the blood. Repatha has been approved for use in various regions, including the European Union, the United States, and Japan, for patients who require additional lowering of low-density lipoprotein cholesterol (LDL-C) .
Mechanism of Action: PCSK9 Inhibition
Targeting PCSK9 Protein
Repatha functions by targeting the proprotein convertase subtilisin/kexin type 9 (PCSK9) protein. PCSK9 is a circulating enzyme that plays a crucial role in the degradation of LDL receptors (LDL-R) on the surface of liver cells. By binding to PCSK9, Repatha prevents it from interacting with LDL-R, thereby reducing the degradation of these receptors. This leads to an increased number of LDL-R on the cell surface, enhancing the liver's ability to remove LDL-C from the bloodstream .
Clinical Efficacy
Clinical trials have demonstrated that Repatha significantly reduces LDL-C levels. When used as an adjunct to diet and statin therapy, it can lower LDL-C by up to 50-60% from baseline levels. It is also effective as a monotherapy in patients who are intolerant to statins . Additionally, Repatha has been shown to reduce other lipid parameters, including total cholesterol, non-HDL cholesterol, apoprotein B, and lipoprotein(a).
Indications and Usage
Approved Indications
Repatha is approved for use in adults with primary hypercholesterolemia (both heterozygous familial and non-familial) or mixed dyslipidemia. It is also indicated for patients with homozygous familial hypercholesterolemia (HoFH) who require additional lowering of LDL-C. The drug is administered subcutaneously at a dosage of 140 mg every two weeks or 420 mg once monthly .
Combination with Other Therapies
Repatha is often used in combination with statins and other lipid-lowering therapies to achieve optimal LDL-C reduction. This combination is particularly beneficial for patients who are unable to reach their LDL-C targets with statins alone .
Safety and Tolerability
Clinical Trial Outcomes
Repatha has been well-tolerated in clinical trials, with a safety profile comparable to placebo. The most common side effects include nasopharyngitis, upper respiratory tract infections, and injection site reactions. Importantly, Repatha does not adversely affect cognitive function, making it a safe option for long-term use .
Conclusion
Repatha (evolocumab) is a groundbreaking drug in the management of hypercholesterolemia. By inhibiting the PCSK9 protein, it offers a powerful option for lowering LDL-C levels, especially in patients who do not achieve their cholesterol goals with statins alone. Its efficacy, combined with a favorable safety profile, makes Repatha a valuable addition to the arsenal of lipid-lowering therapies.
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