What is the mechanism of action for Leqvio (inclisiran)?
On the surface of liver cells are receptors for LDL cholesterol that play a critical role in regulating blood cholesterol levels. The more receptors that are present, the quicker cholesterol can be removed from the bloodstream. Receptor numbers are under the control of a protein, called PCSK9 which breaks down LDL receptors, meaning more cholesterol is left in the blood. Leqvio works by blocking this PCSK9 protein which means more LDL receptors are present on liver cells which increases the uptake of LDL cholesterol and lowers LDL cholesterol in the blood, reducing cholesterol levels.
Leqvio blocks the PCSK9 protein by interfering with the translation of PCSK9 messenger RNA (mRNA) which limits the production of PCSK9. It is a double-stranded small interfering ribonucleic acid (siRNA), which is conjugated with triantennary N-Acetylgalactosamine (GalNAc) to allow better uptake by liver cells.
Leqvio is administered by subcutaneous (under the skin) injection every 6 months and is used in combination with a daily oral statin (such as atorvastatin or rosuvastatin) together with a healthy diet. It belongs to the class of medicines known as small interfering ribonucleic acids (siRNAs).
References
- Leqvio (inclisiran) Prescribing Information. FDA Access Data. https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/214012lbl.pdf
- Leqvio (inclisiran) [Package Insert] Updated April 1, 2022. Novartis Pharmaceuticals Corporation https://www.drugclasses.com/pro/leqvio.html
- What is Leqvio. Leqvio.com. https://www.leqvio.com/what-is-leqvio
Read next
What is the difference between Leqvio and Repatha?
Leqvio and Repatha are both injectable medicines that are used for the treatment of high cholesterol, by specifically lowering low density lipoprotein (LDL) levels. Although they both inhibit PCSK9 they work by different mechanisms. Repatha is a monoclonal antibody that binds directly to PCSK9 in the liver preventing it from binding to LDL receptors. Leqvio blocks the PCSK9 protein by interfering with the translation of PCSK9 messenger RNA. Both have the same result – and that is freeing up LDL receptors on the surface of liver cells which allows LDL cholesterol to be removed from the blood. Continue reading
What are PCSK9 Inhibitors and how do they work?
The PCSK9 inhibitors are used for the treatment of high-risk patients with elevated cholesterol, especially when statins aren't adequate. They work by blocking PCSK9, leaving more receptors available to capture your "bad" cholesterol (LDL) for break down and removal from the blood. Continue reading
Can Leqvio be taken without a statin?
Leqvio may be used alone or with other medications, such as statins, to treat high cholesterol, in addition to a heart-healthy diet. But it can be prescribed without a statin if statins are not tolerated or contraindicated. Continue reading
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