How does repatha work

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How Does Repatha Work?

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 to treat hypercholesterolemia, a condition characterized by high levels of low-density lipoprotein cholesterol (LDL-C) in the blood . Repatha has been approved for use in various regions, including the European Union, and is awaiting approval in other countries such as the USA and Japan .

Mechanism of Action: PCSK9 Inhibition

Targeting PCSK9

Repatha works by targeting a specific protein in the body known as proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a negative regulator of LDL receptors (LDL-R) on the liver cells. Normally, PCSK9 binds to LDL-R, leading to their degradation in the lysosome instead of being recycled back to the cell surface. This process reduces the number of LDL-R available to clear LDL-C from the bloodstream, resulting in higher levels of LDL-C 16.

Blocking PCSK9

Evolocumab, the active component of Repatha, binds to PCSK9 and inhibits its interaction with LDL-R. By preventing PCSK9 from binding to LDL-R, Repatha allows more LDL-R to be recycled to the liver cell surface. This increases the liver's ability to remove LDL-C from the blood, thereby significantly lowering blood LDL-C levels 16.

Clinical Efficacy and Usage

LDL-C Reduction

Clinical trials have demonstrated that Repatha can reduce LDL-C levels by approximately 60% in patients who are already on maximal statin therapy . It has shown efficacy both as a monotherapy and in combination with other lipid-lowering agents such as statins and ezetimibe . This makes it a valuable treatment option for patients who cannot achieve their LDL-C targets with statins alone 24.

Administration and Dosage

Repatha is administered via subcutaneous injection, with recommended dosages of either 140 mg every two weeks or 420 mg once a month 46. This flexible dosing schedule allows for tailored treatment plans based on patient needs and preferences.

Safety and Tolerability

Clinical Trial Results

Repatha has been well-tolerated in clinical trials, with a safety profile comparable to placebo and other active comparators like ezetimibe 46. It has not been associated with serious adverse reactions, and its long-term safety continues to be monitored 23.

Cognitive Function

Importantly, studies have shown that Repatha does not adversely affect cognitive function, addressing a common concern with lipid-lowering therapies . This makes it a safer option for long-term use in managing hypercholesterolemia.

Conclusion

Repatha (evolocumab) is a groundbreaking treatment for hypercholesterolemia, particularly for patients who cannot achieve their LDL-C goals with statins alone. By inhibiting PCSK9, Repatha enhances the liver's ability to clear LDL-C from the blood, significantly lowering LDL-C levels and offering a new avenue for managing cardiovascular risk. Its efficacy, safety, and flexible dosing make it a valuable addition to the arsenal of lipid-lowering therapies.

Sources and full results

Most relevant research papers on this topic

Evolocumab: First Global Approval

Evolocumab has been approved as a treatment for hypercholesterolaemia in the EU, and is awaiting approval in the USA and Japan, for adults with primary hypercholesterolaemia or mixed dyslipidaemia.

2015·

18citations

·A. Markham

Clinical study of Repatha: it does not affect patients’ cognitive function and significantly reduce blood lipid and prevent coronary atherosclerosis

Repatha effectively reduces blood lipids and prevents coronary atherosclerosis in patients with hyperlipidemia, without affecting cognitive function.

2022·

0citations

·Yongzhe Li

Evolocumab (Repatha)--a second PCSK9 inhibitor to lower LDL-Cholesterol.

Evolocumab (Repatha) is a second PCSK9 inhibitor that can lower LDL-cholesterol levels by 60% in high-risk patients already taking maximal statin therapy, but long-term efficacy and safety are unknown and expensive.

2015·

4citations

Evolocumab: A Review in Hyperlipidemia

Evolocumab is a valuable new treatment for primary hypercholesterolemia, mixed dyslipidemia, and homozygous familial hypercholesterolemia, particularly in patients unable to reach LDL-C goals despite statins and those who cannot tolerate or receive statins.

Very Rigorous Journal

2016·

14citations

·G. Keating

Evolocumab (Repatha)--A Second PCSK9 Inhibitor to Lower LDL-Cholesterol.

Evolocumab is an injectable PCSK9 inhibitor that lowers LDL-cholesterol in adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, and is approved as an adjunct to diet and maximally tolerated statin therapy for patients with homozyg

2015·

6citations

[Evolocumab (Repatha®) : a human monoclonal antibody against PCSK9 protein as potent cholesterol-lowering therapy].

Evolocumab effectively reduces LDL-C levels by 50-60% when added to statins, and is a promising treatment for patients with heterozygous and homozygous familial hypercholesterolemia.

2017·

1citation

·C. Wallemacq

Purification and characterization of RepA, a protein involved in the copy number control of plasmid pLS1.

RepA protein plays a role in plasmid pLS1 copy number control by limiting the synthesis of the initiator protein RepB.

1989·

47citations

·G. Solar et al.

Statement for Appropriate Clinical Use of PCSK9 Inhibitors

PCSK9 inhibitors are a powerful option for patients with insufficient LDL-C management, but their use should be limited to those who truly need them and benefit greatly from their use.

Very Rigorous Journal

2018·

5citations

·A. Nohara et al.

Replication control of plasmid R1: RepA synthesis is regulated by CopA RNA through inhibition of leader peptide translation.

CopA RNA indirectly controls RepA synthesis on plasmid R1 by inhibiting leader peptide translation, requiring tap translation for RepA synthesis.

In Vitro StudyHighly Cited

1992·

118citations

·P. Blomberg et al.

The European Medicines Agency's approval of proprotein convertase subtilisin/kexin type 9 inhibitors.

PCSK9 inhibitors, alirocumab and evolocumab, offer a new treatment option for patients with familial hypercholesterolaemia and mixed dyslipidaemia, offering a new treatment option for patients with primary hypercholesterolaemia or mixed dyslipidaemia.

Rigorous Journal

2015·

3citations

·E. Blind et al.

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