What are Peptides?

WARNING: Before I begin, I should tell you that this week’s newsletter is rather long. I don’t expect anyone to read or watch the embedded podcasts in a single sitting…God bless you if you do.(If you don’t have time, you should at least try to watch the 22 minute Podcast on Semax) As I was composing this offering, it kept growing longer and longer because my ultimate goal is to thoroughly educate my readers about the state of our healthcare system…and that’s not a simple task. To do that, I need to give you the “BIG PICTURE” so you can see how it all works, and why. One of the peptides I will discuss today was discovered in Russia where it is now considered a “Vital and Essential Drug” to show you how our health system differs from that of other countries. If you stick with it until the end, I promise that you will come away with a much better understanding of the importance of peptides and the way our healthcare system functions than you have ever had. (If your email service truncates or cuts off part of this email simply click on “view entire message” and it should be restored)

 Do you know what a peptide is? I’m sure that some of you do, but most of you don’t. So let me explain…

A peptide is a short chain of amino acids linked by chemical bonds, called peptide bonds. Peptides are made up of 2 to 50 amino acids, while a longer chain of amino acids (51 or more) is called a polypeptide. Proteins are made up from one or more polypeptides. Peptides are naturally occurring, but some are also artificially created in laboratories for industrial use. They play an important role in many of the body's processes, including: Digestion, Energy from food, Hunger, Hormone function, Muscle building, and Fat formation.

Before continuing, I want to emphasize something, so you will clearly remember it. ALL peptides are naturally occurring and were created by, and are active in, the human body during life. So, they are not “drugs” in the strictest sense of the word. This distinguishes them from the products made by big Pharma where scientists develop, and test substances designed to affect processes of the human body in normal or pathological states. Their ultimate goal is to patent these drugs in the hope of being approved by the FDA for use in the U.S.A… Unless they are updated, these patents last for 17 years. Thereafter, these same drugs can be marketed as “generic equivalents” which usually cost substantially less.

You may be surprised to learn the name of the first peptide to be discovered. It is insulin… by far the best-known peptide in the world, and as you will learn, one of the most important substances in the human body. This hormone is both vital for life and at the same time, excessive amounts are responsible for virtually all chronic diseases related to aging, which I will expand upon later.

But I digress, because I want to share its history with you first. In 1921Frederick Banting, an orthopedic surgeon, had the idea of isolating pancreatic islet extracts by ligating (tying off) the pancreatic duct of dogs, keeping them alive until the acini (small saclike cavities in the pancreas) degenerate, leaving the islets of Langerhans in isolation. He approached John Macleod, professor of physiology and department head at the University of Toronto, for laboratory space. Macleod granted him laboratory space, ten dogs for his experiments, a student research assistant (Charles Best), and provided supervision and guidance.

The first use of insulin to treat diabetes was on January 11, 1922, when 14-year-old Leonard Thompson received an injection of the hormone developed by Eli Lilly. Thompson was a patient at Toronto General Hospital who was in and out of consciousness and dying from type 1 diabetes.

Over the next several years, Lilly experienced several problems, first with insulin harvested from dogs and later harvested from pigs. They had great difficulty maintaining consistent concentrations which made treatment very difficult. Recognizing that there had to be a better solution, scientists began work attempting to synthesize human insulin. This work continued unsuccessfully for several decades.

The first synthetic insulin, also known as "human insulin," was produced using recombinant DNA technology in 1978 by scientists at Genentech, with David Goeddel being a key researcher, using E. coli bacteria to produce the insulin chains; this marked the first genetically engineered human insulin

Since the discovery of insulin, remarkable achievements have been made resulting in the approval of more than 80 peptide drugs worldwide. Recently, peptides have become one of the important trends in pharmaceutical research. Now, the most well-known peptides are those being used in adults with type 2 diabetes such as Ozempic and Mounjaro. Ozempic, known generically as semaglutide, was modified from liraglutide by Novo Nordisk, and was approved by the FDA in 2017 by the U.S. However, since then, these GLP-1peptides have moved to the forefront of the latest trend in pharmaceuticals: “Weight-Loss Drugs”. In large part, these medications have gone “viral” because they have shown impressive results for high-profile stars such as Oprah Winfrey and Kelly Clarkson that have struggled with their weight for years.

In the link following this paragraph, in a two minute and 40 second video from CNN, Oprah comments on her use of these medications and the fact that there is no difference between weight-loss drugs and medications approved for diabetes EXCEPT that insurance pays for one, and not the other. (Forgive the mandatory ad at the beginning. Also, you may have click to close the tab after it finishes)

Oprah on Weight-Loss Medications (click to view)

GLP-1(Glucagon-Like Peptide-1) agonists are currently the most effective anti-obesity medications and are considered safe for long-term use. Currently, only liraglutide (Saxenda), semaglutide (Wegovy), and tirzepatide (Zepbound) are approved for weight loss, though some other GLP-1 drugs may be prescribed off-label. Because of their growing wide-spread use you should expect more reports of side-effects. However, if you consider the effects of alternative drugs, many of which have proven far more dangerous, or the effect of long-term obesity, there are many more positives than negatives.

Okay, now that you are familiar with some of the best-known peptides, let’s dive into Semax. This peptide is a HEPA peptide that is an analog of the N-terminal fragment of adrenocorticotropic hormone (ACTH) that is produced by the pituitary gland. As hinted by its name, ACTH triggers the adrenal glands to produce cortisol, also known as the “stress hormone”.  Although Semax has no hormonal activity, it is believed to have neuroprotective and nootropic effects. Semax is used as a prescription drug in Russia and Eastern Europe but is not approved for use in most other countries. It is widely sold online and used as a purported cognitive enhancer. It was developed at the Russian Academy of Sciences in 1991 and is administered in nasal drops or sprays and are formulated to be safe for children. The following podcast on Semax from the Revitalyze MD channel featuring Dr. Debra Durst discusses uses and study results for Semax (about 22 min).

SEMAX: Increase MEMORY, learning CAPABILITY, and mental SHARPNESS (click)

Semax has been used to treat the following conditions:

• Memory and cognitive disorders. One study found that Semax improved attention and short-term memory in healthy subjects, especially after an 8-hour work shift. 

•  Stroke and transient ischemic attacks

• Anxiety and depression

• Assisting in nerve regeneration

• ADHD and dyslexia

• Opioid withdrawal

• Chronic neurological diseases such as ALS, Parkinson's Disease, and Alzheimer's

• In combination with rehabilitation therapy to treat PTSD

• In combination with rehabilitation therapy to treat substance withdrawal from heroin and amphetamines

• Ocular nerve atrophy, glaucoma and macular degeneration

• Neurological deficits in newborns

Despite the information stated in the Revitalyze MD podcast, Semax and some of its advanced forms are indeed legal and available without a prescription online in the United States. Going a step further, I am including an image of an advanced Semax product currently available on Amazon at a very reasonable price. Thoughtfully, this product comes in the form of a freeze-dried peptide powder, that must be reconstituted with the included water for maximum life expectancy. As with all peptides, the product should be stored in a refrigerator once reconstituted to maintain potency and prolong shelf-life.

As you can see, Semax has a myriad of established uses and has been shown to be safe for children. I should also point out that in the United States we have no approved alternative treatments for the conditions listed above.  Not only that, but many of the approved drugs used to treat ADHD and dyslexia are schedule II drugs, some of which are listed below.  Each has strong potential for abuse and can be addictive with several side-effects. Examples of other Schedule II drugs include: hydromorphone (Dilaudid®), methadone (Dolophine®), meperidine (Demerol®), oxycodone (OxyContin®, Percocet®), and fentanyl (Sublimaze®, Duragesic®) …all of which are illegal in Russia.

Prescription drugs used to treat ADHD and dyslexia in the U.S. include: 

• Atomoxetine (Strattera): A non-stimulant medication that is commonly used to treat ADHD. A 2017 study found that atomoxetine can improve reading scores in children with dyslexia or ADHD and dyslexia, compared to those who received a placebo. 

• Methylphenidate (Ritalin): A stimulant medication that can improve reading performance in children with ADHD and dyslexia. 

• Adderall: A stimulant medication that contains amphetamine and dextroamphetamine. 

• Focalin: A stimulant medication that contains dexmethylphenidate. 

• Guanfacine (Intuniv): A non-stimulant medication that can improve attention and reduce blood pressure. 

As most of you are probably aware ADD, ADHD, and dyslexia have been increasingly diagnosed in the past 40 years, even when the symptoms do not “check all the boxes”.  Not knowing exactly how to label the observed behavior can lead to misdiagnosis, only to discover years later that the cause for this behavior was related to a different pathology that requires a different treatment. In addition to this kind of error, children often react atypically to drugs like Adderall. In fact, my son was diagnosed with ADHD and prescribed Adderall, a class II drug. Instead of improving his behavior, it caused him to react emotionally and would often lead to crying spells. Needless to say, his use of Adderall was discontinued. As a doctor, I have to wonder if the use of a more natural substance like Semax, as compared to amphetamine, would have created a similar problem or other serious side-effects?

The reason I pose this question is to point out that although we have an excellent healthcare system for the most part, it does have at least one significant flaw…the requirement for big Pharma to be able to patent any drug they develop. This problem is more complex than it seems at first glance. Ultimately, everything gets back to money. It takes an enormous amount of it to get a new drug approved by the FDA, because of its design as you will see below. Much of that money is used to pay for human studies. That’s why there are so few human studies for peptides…and that is because unless they are modified in some way, peptides cannot be patented because they are naturally occurring.

As a result, virtually all studies for peptides and supplements are first done on yeast, worms, flies, and mice, in that order. If these studies show promise, research moves to the next phase, where venture capitalists seek to raise money to fund studies on higher mammals including dogs, cats, monkeys, and humans. Then we wonder why medications cost so much. So, before we point a finger at big Pharma, realize that if the money to pay for the drug approval process didn’t come from patents...it would have to come out of your pocket as taxes. “Pay me Now, or Pay me Later”

Being honest, I believe there are several peptides that can provide valuable benefits for aging-related problems that are not available from any other existing medications…and there is a reason. Peptides developed by the human body have evolved over millions of years that contribute to ALL our bodily functions and are largely responsible for the success of our species. As we age, our bodies begin to fail due to the loss of these vital substances that are present throughout our lives.  Eventually, later in life, the cells that produce these peptides age and become faulty, which leads to further aging and eventual death. However, studies have shown that when we reintroduce these peptides from exogenous sources, they can restore lost function… Given these facts, is it so unreasonable to think that proper use of peptides together with improved diet and regular exercise could extend our life and health span?

While I’m at it, I’m going to share additional information that most of our population is unaware of. If you have read and understood the things that I have told you about peptides, it might occur to you that many of these potentially valuable substances may never be approved by the FDA because there is not enough monetary incentive to pay for the drug approval process. This is truly regrettable, since there is so much potential benefit from their use. Interestingly, the FDA has provided a “loophole” that many are not aware exists…If you were to search the internet you would find dozens of sites selling some of the most popular peptides. Most of these peptides are third-party certified for purity. BUT there is an apparent “catch”. The FDA requires a mandatory statement be prominently displayed saying “All products are sold for research, laboratory, or analytical purposes only, and are not for human consumption” (wink-wink) But anyone can still purchase them without a prescription…

Looking at this policy from a distance, I see this as very clever on the part of the FDA. What they have accomplished using this tactic, without any new legislation, or opposition from big Pharma, is impressive in an “under-the-radar” sort of way. This allows health practitioners, clinics, and compounding pharmacies to work with peptides that have not been approved by the FDA for a specific use on a case-by-case basis. What this means is that it allows individuals to legally seek treatment with peptides with expert medical oversight that provides proper testing and management by the medical community. At the same time, it prevents unrestricted use by unlicensed entities attempting to profit from the resale of these substances to the public. Additionally, this approach allows documented data associated with their use to be recorded for future analysis and possible approval by governing bodies… “Sometimes Less is More”

Until next time, take care and stay positive… Dr. G