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December 7, 2020 CardiovascularCholesterol

For some patients, managing cholesterol creates a challenge. Statins are a safe and standard treatment but many people have very high levels of cholesterol that require more than statin drugs alone.  Others cannot easily tolerate statins.  Nonetheless, treating cholesterol saves lives and avoids heart attacks and strokes.

Thankfully, the future is here with new breakthroughs that can change the way we maintain healthy cholesterol levels due to continued research and clinical trial participants. We outline some of these exciting technologies below.

Antisense oligonucleotides (ASOs) are short, synthetic single stranded fragments of RNA that can reduce, restore or modify protein expression. ASOs have been designed specifically to target high levels of LDL (bad cholesterol) in the bloodstream in a different way than current medications. Firstly, ASOs targets the source of the disease resulting in a higher chance of success compared to therapies targeting downstream pathways. Secondly, ASOs are not metabolized by cytochrome P450 as most other drugs are. This significantly reduces the chance of one drug interacting with another drug in the body which could potentially cause more harm than good.

Small interfering RNA (SiRNAs) are another type of RNA therapy that is being used in clinical trials to reduce the risks of cardiovascular disease. Unlike ASOs which are single-stranded oligodeoxynucleotides, siRNAs are double-stranded RNA molecules. SiRNAs are used in the silencing of disease-causing genes, in this case the genes involved in creating cardiovascular diseases, and it has made great progress. 

Adnectins are a class of drugs used to target proteins. Adnectins can be rapidly developed to bind proteins or other necessary targets. Currently, adnectins are being used in clinical trials to bind with a human protein called PCSK9. This binding blocks the interactions between PCSK9 and LDL (bad cholesterol) receptors. As a result, the levels of LDL cholesterol in the body are lowered.

These technologies hold the potential to not only better manage cholesterol levels and thereby reducing heart attack and stroke risk, but many other conditions as well.

Source:

US National Library of Medicine
National Institutes of Health


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If you have high cholesterol you may dread going to your doctor, especially if they are going to complete a cholesterol blood test. You know they prescribed a statin, but the muscle cramping you experience after taking it just isn’t worth it. How do you tell your doctor that the medication they prescribed just isn’t working for you? You are not alone, and there are options available for you.

 

We all know that having excess cholesterol in our blood is a bad thing, but why is it so bad? High cholesterol has often been called ‘The Silent Killer’. In fact, according to the CDC heart disease is responsible for 1 in 4 American deaths every year.[1] High cholesterol is known to cause plaque formation in arteries, constricting blood flow to vital organs in your body. Even worse, cholesterol plaques can become dislodged from the walls of the arteries potentially causing blood clots. Both heart attacks and strokes can be caused by plaques reaching the heart or brain respectively. If lifestyle changes such as a good diet and exercise can’t bring down your cholesterol numbers, you may need a medication. The most common cholesterol lowering medications to date are statins such as Crestor, Lipitor, or Zocor.  These medicines have been life saving for many people that can tolerate them. However, some people are intolerant to statins and will experience side effects such as painful muscle cramps, inflammation and more.

 

If you are allergic to or can’t handle statins what can you do? It is crucial to keep your cholesterol levels down, lowering your risk for a heart attack and stroke. You may try one of the medications already on the market for people with statin intolerance such as Zetia, Juxtapid and Repatha. However, each of these drugs have their own risks. Zetia can cause symptoms similar to those caused by statins. Juxtapid, a newer medication, has been found to significantly reduce LDL bad cholesterol by 40-50%.  Sadly, it also caused diarrhea, nausea, vomiting or abdominal pain in 28% of patients.[2] In 2015 the FDA approved Repatha, a new class of drug called a PCSK9 inhibitor that is very successful in lowering LDL.  Unfortunately, due to the cost of development and production the annual cost is around $14,000 dollars making it unaffordable for most people.

 

If you’ve had trouble taking statins in the past you may be asking “what do I do now”? Many of our participants are looking for alternative treatments or want to be part of cutting edge research. I encourage you to check out the cholesterol research studies we are conducting at many of our research centers. You may qualify for a new oral medication or to receive PCSK9 in an upcoming study! The medicines being researched for people who cannot take statins may significantly alter the future of cardiovascular disease.  We need your help to bring these new medications to market!

 

References:

[1] “Heart Disease Fact Sheet.” Centers for Disease Control and Prevention. Centers for Disease Control and Prevention, 16 June 2016. Web. 27 Apr. 2017.

[2] Orrange, Sharon, MD. “Finally, a Non-Statin Cholesterol Medication That Works: Introducing Juxtapid.” The GoodRx Prescription Savings Blog. N.p., 06 June 2014. Web. 27 Apr. 2017.

 


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