Friday, June 29, 2018

Evolocumab Are You Joking Me ? by Jeffrey Dach MD


PCSK9-inhibitor-evolocumab-Are-You-Joking 
Evolocumab, Are You Joking Me? by Jeffrey Dach MD

Ralph is a 48 year old divorce lawyer who arrives in my office with a history of familial hypercholesterolemia.  Every lab panel since he was a kid showed a cholesterol of 340.  Other family members had the same genetic abnormality, and some even died of heart attack at early age.  About six months ago Ralph switched to a new doctor whor was alarmed by his high cholesterol.  The new doctor started him on a statin drug which reduced his LDL cholesterol down to 95. However, thinking this was insufficient, the new doctor added Evolocumab, to drive the LDL cholesterol even lower. Header image courtesy of LongevityFacts.com 

FDA Approved in Dec 2017

Amgen’s Evolocumab (Repatha), was recently FDA approved, and requires an injection every two weeks.  At $14,000 a year, Evolocumab is the most expensive cholesterol drug on the market.   A similar PCSK9 inhibitor drug, bococizumab,  under development by Pfizer was discontinued after a failed study.(7)

Lowest LDL in History

After the Evolocumab drug was added to the statin drug, Ralph’s labs showed an LDL cholesterol of 30, the lowest in the history of Western Civilization in a human. I looked at Ralph and asked him if he was all right.  Not exactly, he said.  Ralph has trouble sleeping ever since starting the cholesterol lowering drugs.  He has been experiencing troublesome tingling and burning sensations on his arms at night while trying to sleep.   In a nutshell, Ralph is miserable, and wants to know if he can safely stop the cholesterol medication.

“A Lifesaving Miracle Drug”

Many newspapers and Cardiologists proclaim Evolocumab is a “lifesaving” miracle drug.(1)(27)  Let us see the data showing the number of lives saved.  Here is the data table (below) from Dr Marc Sabatine’s FOURIER study .(2) In this study, 27,500 patients on statin drugs for atherosclerotic heart disease were randomized to either drug (Evolocumab) or placebo.  The drug reduced the LDL-cholesterol by 60%, from 90 to 30 mg/dl.

Below Image Table 2  FOURIER Study  courtesy of Sabatine, Marc S., et al. “Evolocumab and clinical outcomes in patients with cardiovascular disease.” New England Journal of Medicine 376.18 (2017): 1713-1722.(2) Red arrow and circle=drug group.  Green arrow and circle=placebo group.



Cardiovascular Death- No Lives Saved

At the end of the 2.2 year study period there were eleven more deaths in the drug treated group.  There were 251 cardiovascular deaths in the drug group (red arrow and circle), and only 240 in the placebo group (green arrow and circle).  No lives saved.

Death from Any Cause – No Lives Saved

There were 444  deaths in the drug group (red arrow and circle), and only 426 in the placebo group (green arrow and circle).  No lives saved.  Eighteen more deaths in the drug treated group.

Hospitalization for Unstable Angina- No Difference

There were about the same number of hospitalizations for unstable angina in each group.

A Lifesaving Drug that Actually Kills More People Than Placebo ?
Perhaps someone can explain to me how this can be called a “lifesaving” miracle drug, when in fact, more people died in the drug group, and no lives were actually saved by the drug?

The Miraculous Benefit of Intensive Lowering of LDL Cholesterol

If one is coldly objective about the data coming in, one might say the PCSK9 drug trials have actually falsified the cholesterol theory of heart disease.  Here we have the lowest LDL cholesterol ever achieved in the history of medicine, yet no lives are saved. Bryan Hubbard says in May 2017:
The PCSK9 drug trials are inadvertently challenging the cholesterol-heart disease theory. The drugs are bringing down ‘bad’ LDL cholesterol to unprecedented levels, and yet similar numbers of people are dying from heart attack and stroke whether taking the drug or a placebo.(20)

Wait Just A Minute, Fourier Showed Reduction in MI’s
The Fourier study data (above) showed 171 fewer Myocardial Infarctions (MI) in the PCSK9 Evolocumab drug group. Isn’t this a real benefit of the drug?   Here is what Dr Harumi Okuyama had to say about that.(55)  The data is biased and faked:
“The composite end point included measures that were less objective; hence, the accuracy of these measures as used across 49 different countries could have been biased, with the exception of mortality. For example, troponin level is known to be elevated after coronary angioplasty, leading to more frequent diagnosis of MI in the placebo group….However, we speculate that the reported data do not substantiate the conclusions made by the original authors, and we recommend against accepting their conclusions as an endorsement of PCSK9 inhibitors.

Heart Attacks Kill People, Don’t They? 

I think we are all in agreement with the statement: “Heart attacks kill people”.  You might ask, how many people?  According to Dr Viola Vaccarino in the New England Journal from 1999, early mortality after myocardial infarction is 16.7 per cent in men and 11.5 per cent in women.(57)  If we have two randomized groups, and one group has more heart attacks, then this should translate into increased mortality for that group. This is just common sense.  The Fourier Evolocumab drug study showed the opposite.  The placebo group had 171 more heart attacks, yet did not show increased mortality compared to the drug group.   Exactly how an FDA committees can overlook this blatantly obvious contradiction is mind boggling.

Effect of Intensive Cholesterol Lowering on Calcium Score

We have made the case for annual calcium score progression as our most important tool in the management of coronary artery disease.  Where is the calcium score data for the FOURIER Evolocumab study?  There is none.  The study neglected to obtain annual calcium scores.
Remember, statin cholesterol lowering drugs were studied with annual calcium score by Dr Paolo Raggi in 2004.  His study showed that 41 of 500 patients on statins had heart attacks over 6 years in spite of cholesterol lowering.  The feature which defined the heart attack group was greater than 15 % annual calcium score progression, not the cholesterol level which was identical for both drug and placebo groups.  Dr Paolo Raggi showed progression of calcium score and myocardial infarction in 41 patients in spite of statin treatment. Will Amgen’s Evolocumab yield similar results?  We await these studies.

Non-Statin Cholesterol Lowering Drugs Abandoned 

Non-statin cholestrol lowering drugs have not fared well in the past.  Statin drugs have the advantage over these newer drugs because statins not only lower cholesterol, they also have pleomorphic effects (anti-inflammatory effects) which some would say provide the real benefit.
High hopes were raised for the non-statin  CETP inhibitor drugs including Eli Lilly’s Anacetrapib and Merc’s Evacetrapib.  Both were highly effective for reducing LDL cholesterol,  yet both failed to reduce the rate of cardiovascular events in patients with high risk cardiovascular disease.  Because of failed clinical trials, both drugs were abandoned and never brought to market.  In retrospect, perhaps the newer non-statin  PCSK9 inhibitor drugs should all share this same fate.(7)  In my opinion,  lack of mortality benefit should have prevented FDA approval of Evolocumab, which was approved anyway, raising the question of behind the scenes political influence.   It is indeed a difficult thing to walk away from a 500 million dollar investment.

Concern for Adverse Neurocognitive Effects 

The FOURIER Evolocumab study reported no adverse effects from intensive lipid lowering. I find this difficult to believe in view of the FDA warning letter asking for a prospective study of neurocognitive adverse effects in the PCSK9 Inhibitor treated group.(29,30)  Neurocognitive effect is a polite way to say loss of ability to focus, think and remember. In other words, drug induced dementia.

Dr Kristopher Swiger wrote an article in 2015 Drug Safety entitled: “PCSK9 Inhibitors and Neurocognitive Adverse Events: ” (31).  He says:
On both theoretical and empirical grounds, concern for adverse neurocognitive effects currently extends to PCSK9 inhibitors.(31) These events  included delirium, cognitive and attention disorders and disturbances, dementia, disturbances in thinking and perception, and mental impairment disorders.(32)

Adverse Psychiatric Reactions with Intensive Cholesterol Lowering

Lower cholesterol level is associated with a number of adverse psychiatric reactions, such as increased risk of suicidal and violent behavior, depression, aggression, and impulsivity  . (35-37)  Dr Eriksen wrote in  Psychiatry Research 2017:
“low cholesterol is a risk marker for inpatient and post-discharge violence in acute psychiatry.”(39) 

People with low cholesterol are more likely to commit violent crimes.(41)  Dr Beatrice Golomb found that low cholesterol was associated with:
“severe irritability homicidal impulses, threats to others, road rage, generation of fear in family members, and damage to property.”(42)

Dr Michael Tatley writes about “Psychiatric adverse reactions with statins, fibrates and ezetimibe.” in Drug Safety 2007(43).  He says:
“The reactions mentioned … include depression, memory loss, confusion and aggressive reactions….The observation that other lipid-lowering agents have similar adverse effects supports the hypothesis that decreased brain cell membrane cholesterol may be important in the aetiology of these psychiatric reactions.”

Dr Repo-Tiihonen investigated “associations between Total Cholesterol levels, violent and suicidal behavior, age of onset of the conduct disorder (CD) and the age of death among 250 Finnish male criminal offenders with ASPD (Antisocial Personality Disorder)”, finding lower cholesterol a  prognostic marker for early unnatural death, and violent crimes. (44)

We Cannot Ignore the Massive Data of Negative Impact

In 2016 Drug Safety, Drs Cham, Koslik, and Golomb reoorted on “Mood, Personality, and Behavior Changes During Treatment with Statins: A Case Series.   Adverse events related to cholesterol lowering drugs included violent ideation, irritability, depression, and suicide.  These problems resolved when the drug was stopped and recurred when the drug restarted. (45)

Dr Alfonso Troisi says in Neuroscience & Biobehavioral Reviews  2009 :
“we cannot ignore the mass of data showing a negative impact of low cholesterol in some clinical populations or healthy subjects.”(38)

U Shaped Curve Associates Low Cholesterol With Increased Mortality
The finding of increased mortality at low cholesterol levels is not surprising, and  has been known for decades. Back in the 1990’s, accumulated data from multiple studies showed that low cholesterol is associated with increased mortality.(46-53)  The cholesterol data chart reveals U shaped curve in all the cohort studies such as the J-Lit, HUNT-2, and MRFIT.(46-53)  Both left and right arms of the curve show increased mortality.  Dr Petursson from Norway says in 2012:(48)

“Regarding the association between total cholesterol and mortality, our results generally indicated U-shaped or inverse linear curves for total and CVD mortality….Our results contradict the guidelines’ well-established demarcation line (200 mg/dl ) between ‘good’ and ‘too high’ levels of cholesterol. They also contradict the popularized idea of a positive, linear relationship between cholesterol and fatal disease. Guideline-based advice regarding CVD prevention may thus be outdated and misleading, particularly regarding many women who have cholesterol levels in the range of (200-270 mg/dl) and are currently encouraged to take better care of their health….recommendations regarding the ‘dangers’ of cholesterol should be revised. This is especially true for women, for whom moderately elevated cholesterol (by current standards) may prove to be not only harmless but even beneficial.”(48)

In Circulation 1992, Dr Judith Walsh says :
There is an association between low blood cholesterol and noncardiovascular deaths in men and women.  There is no association between high blood cholesterol and cardiovascular deaths in women.”(50)

In 1993, Dr Jacobs speculated on the reason why low cholesterol is associated with risk of non-atherosclerotic death. He says: (49)

“Cholesterol affects the fluidity of cell membranes, membrane permeability, transmembrane exchange,  signal transmission, and other cell properties. Cholesterol is a precursor for five major classes of steroid hormones. It affects gluconeogenesis and immune function; its transport forms, the lipoproteins, also serve as vehicles for fat-soluble vitamins, antioxidants, drugs, and toxins. Thus, cholesterol plays general, fundamental, and highly specific roles in the economy of the body.  …Several authors have recently suggested caution in the pursuit of low Total Cholesterol,  recommending against Total Cholesterol  lowering in persons with Total Cholesterol less than 225 mg/dl.”(49)

Review and Meta-Analysis of PCSK9 Drug Trials

In 2018, Dr Alessandro Battaggia reviewed all the PCSK9 studies and says there was no benefit.  Even in trials recruiting familial hypercholesterolemia patients, there is “tendency to harm” (56) :

No beneficial relationship was found between LDL-C lowering and cardiovascular events explored by meta-regression; instead, there was a trend toward harm. For any of the other outcomes there was no significant association between LDL-C lowering and risk…..A separate meta-analysis of trials recruiting familial hypercholesterolemia patients have showed a tendency to harm for almost all outcomes….Therefore, at the moment, the data available from randomized trials does not clearly support the use of these antibodies.”(56)

Conclusion:  The lack of mortality benefit reported in the FOURIER study, in spite of the lowest LDL levels in medical history is not surprising, since increased mortality associated with low cholesterol has been known for decades.  In addition, it is clear from both failed CETP inhibitor drug trials, and the PCSK9 drug trials, that lowering cholesterol with a non-statin drug is a futile exercise which provides no health benefit.   I would agree with Dr Alessandro Battaggia’s report, that intensive cholesterol lowering with expensive non-statin drugs has a “tendency to harm”.(56)  This is a medical practice that should be halted immediately.

Articles with Related Interest:

Coronary Calcium Score benefits of aged Garlic
Calcium Score Paradigm Shift in Cardiology
Statin Denialism on the Internet
Autopsy Studies and Cholesterol No Correlation
Familial Hypercholesterolemia and Statin Drugs

Jeffrey Dach MD
7450 Griffin Road
Suite 180/190
Davie, Florida 33314
954-792-4663

Links and References

see original article at: https://jeffreydachmd.com/2018/06/evolocumab-are-you-joking/

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