Home Forums General Medicine PCSK9 inhibitors instead of Statins

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      Anonymous
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      There is a new drug available for treating some patients with high cholesterol where routine treatment is difficult. Many of them who suffer from familial hypercholesterolaemia, people who are unable to lower their LDL cholesterol inspite of being on maximum dose of statins or some who have a heart disease and still are unable to lower LDL-cholesterol may all benefit from this drug. The drug is called “PCSK9 inhibitor”.

      Normally the surface of healthy liver cells have LDL receptors which bind LDL cholesterol and are then endocytosed. Within the cell, these receptors are either recycled or degraded. The PCSK9 protein which is produced by the liver cells is responsible for degradation. If PCSK9 is inhibited, more LDL receptors are recycled to the cell surface, which can result in them taking up more LDL cholesterol. The fewer receptors there are, the less able the liver is to keep our blood cholesterol low.

      So PCSK9 inhibitors target the PCSK9 protein making it less effective at breaking down LDL receptors. The result is more working receptors on the surface of liver cells, and more cholesterol can be removed from the blood.

      The first PCSK9 inhibitors that are being developed are a kind of drug called a monoclonal antibody or MAB. All MABs are made in a laboratory. They can recognise and attach to specific proteins produced by cells in our bodies. Each monoclonal antibody recognises just one particular protein. They work in different ways depending on which protein they target.

      Method of Treatment:
      Monoclonal antibodies (MABs) can only be injected directly under the skin. They cannot be taken orally. The good news is that PCSK9 inhibitors only need to be taken once every 2 to 4 weeks dependent upon which drug is used and its strength. Most people can inject themselves.

      Side effects:
      PCSK9 inhibitors appear to be well tolerated. The main side effect noted was mild soreness or itchiness at the site of injection.

      How effective are they?
      PCSK9 Inhibitors seem to be very effective. Clinical studies have shown that they can cut LDL cholesterol levels by more than half in a wide variety of patient types. They are also effective alongside other cholesterol lowering treatments such as statins. Early data also suggests that there are fewer heart attacks and strokes amongst people that have taken these drugs compared to people on a placebo drug.

      Available Drugs:
      There are two PCSK9 inhibitors which are already licenced for use in the UK. These are Evolocumab and Alirocumab.

      On May 5th 2016, Following HEART UK’s #Yes2PCSK9 campaign, the National Institute for Health and Care Excellence (NICE) published a final draft guidance recommending Evolocumab and Alirocumab for some people who have conditions that put them at extremely high risk of heart attacks or strokes. The draft guidance recommends Alirocumab (Praluent, Sanofi) and Evolocumab (Repatha, Amgen) for adults with primary hypercholesterolaemia/mixed dyslipidaemia and those with heterozygous familial hypercholesterolaemia (HeFH) to help reduce their risk of cardiovascular disease.
      Furthermore the drugs are recommended for people whose cholesterol levels are not controlled adequately using other drugs such as statins, or who can’t tolerate statins because of their side effects or have another condition which means they can’t take them.

      The drugs are very expensive at the moment, costing between $1000 to $1500 per patient per year. We will probably continue using statins for a long time before the new drugs become affordable for the general population

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