Success of New Anti-Cholesterol Drug Eprotirome

HeartHawk Health Guide
  • As both a blogger and a patient "living with heart disease" the recent announcement (see report) of the success of the new anti-cholesterol drug "eprotirome" is the most exciting news I have come across in quite some time. However, the article's headline "Statin Alternative Shows Promise in New Study" tells only half the story!


    Eprotirome is an experimental thyroid hormone mimetic (a drug that "mimics" the action of thyroid hormones) that significantly lowered LDL cholesterol during Phase 2 clinical trials.  Cutting-edge physicians such as expert and cardiologist William R. Davis have demonstrated for some time now that aggressively treating even mild or sub-clinical hypothyroidism (a condition where the body does not produce enough of natural thyroid hormones) can help combat heart disease in several ways.

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    Unfortunately, there is a limit to how much synthetic thyroid hormone you can take before you exhibit the symptoms of hyperthyroidism (too much thyroid hormone) which has it own set of negative cardiac side effects such as heart arrhythmias!  But, what if you could develop a drug that only mimicked thyroid hormones on some organs such as the liver where cholesterol and other lipids are manufactured.  That is essentially what eprotirome does.


    During a 12-week study conducted by Karo Bio AB, 168 participants where given either a placebo or one of three doses of eprotirome along with a statin.  LDL Cholesterol levels were lowered up to an additional 32% over baseline with just a statin alone with none of the adverse effects generally associated with increasing levels of thyroid hormones.


    This result is certainly something to be ecstatic about as there are many people for whom statins do not provide needed reductions in LDL Cholesterol or who simply cannot tolerate the side effects of statins.  However, there was another, under-reported and under-emphasized outcome in the study - and now, as Paul Harvey used to say, here is, "the rest of the story!"


    Near the end of the article Dr. Paul Ladenson, professor of endocrinology and metabolism at the Johns Hopkins University School of Medicine (and lead author of a report on the trial, published in the New England Journal of Medicine) offered this observation which I believe to be the "money" quote, "The second exciting part is its impact on lipids other than LDL cholesterol.  Though statins lower LDL ("bad") cholesterol, they have no effect on other blood fats, such as lipoprotein A, which is believed to be equally damaging . . ."  Eprotirome not only exhibited a dose dependent effect on lowering LDL Cholesterol it showed a similar effect on lowering Lipoprotein(a), recently discovered to be an independent risk factor for heart disease.


    For those not familiar with Lipoprotein(a), often referred to as "Lp(a),"  it is an LDL-like particle that has now been shown to greatly magnify the risk of Coronary Artery Disease (CAD) and is especially identified with very early CAD and hearts attacks - for some as young as their thirties and forties!  Lp(a) is almost entirely genetic in cause, is resistant to changes in diet and exercise, and there are no safe therapeutic agents capable of reliably lowering it.  Niacin is the most well known anti-Lp(a) agent but is often incapable of persistently lowering Lp(a) to acceptable levels.


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    As you may have guessed, Lp(a) is my personal heart disease scourge and that of many in my family (three who have had heart attacks and died) and it includes my son who has also tested positive.  I originally had modest success with niacin but it is no longer effective for me.  There are other agents available but they have some really nasty side effects like deafness and blood clots.  I already take synthetic thyroid hormones to treat hypothyroidism (Hashimoto's Thyroiditis) so there is little room for me to increase the dosage of those drugs.


    Although high Lp(a) is not my only problem, I have successfully modified every other contributing factor to my heart disease with flying colors including pre-diabetes.


    It is terrific that there is a new and promising agent for treating high cholesterol and one that promises fewer side effects than statins.  But there are many ways to treat high cholesterol including powerful, non-drug, diet and nutritional supplement strategies.  Conversely, there are darn few effective therapies for lowering Lp(a), which, if you have it, is potentially more threatening than simple high cholesterol.  Cholesterol lowering continues to get top-billing in trials but back-stories like clinical trial success against Lp(a) is where the real action in my humble opinion.  It is extremely uplifting to know that drugs such as eprotirome are in the pipeline.  Here is hoping it makes it all the way to market.


    I would also be remiss if I did not award kudos to Karo Bio for their diligent research efforts.  Make no mistake; heart disease research is both risky and expensive.  Heart disease sufferers were dealt a huge blow when Pfizer made a business decision to get out of heart disease research after the expensive failure of their HDL raising drug torcetrapib (it did raise HDL dramatically but had side effects that hurt more people than it helped).  In making this move Pfizer shut down and disbanded what was probably the most talented and well-funded heart disease drug research team in the world.  You won't read about the precursors to eprotirome that that did not make it to Phase 2 trial (Karo Bio had another thyroid mimetic code-named KB5359 that did not make it to Phase 2 due to Phase 1 toxicology failure).  Drug development is and time consuming and expensive proposition and so are these trials.  Initial eprotirome testing dates back to before 2007.  Even if everything goes smoothly eprotirome won't get to market for at least two to three years.  Because Karo Bio persisted where others may have given up we may have a whole new and powerful way to treat Lp(a).


    One last caveat and plea to Karo Bio.  It was reported that if eprotirome successfully navigates the remaining clinical trials it may only be offered in conjunction with a statin as an LDL Cholesterol lowering treatment.  Let's hope they see the light and understand we also need effective treatments for Lp(a)!


    Looking out for your heart health,



Published On: April 02, 2010