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SARMs: Steroid Replacement or Crazy Concoction?

Victoria Felkar, (PhD Candidate)

SARMs: Steroid Replacement or Crazy Concoction?

In recent years, selective androgen receptor modifiers (SARMs) have gained a cult-like following among competitive bodybuilders and other athletes. A booming black-market business for SARMs has developed from outlandish claims, exploitation of pharmaceutical patents, and abuse of legal loopholes, all of which has the potential to destroy SARMs before they can even turn a profit or before they can be used to treat disease in the populations who might benefit from their use. But what are SARMs and why are athletes using them? MUSCLE INSIDER takes an uncensored look at the “research chemicals” being experimented with by many, but understood by few.

What Are SARMs?
Believe it or not, that’s not actually the simplest question to answer. For the purposes of this article, we’ll be looking at a new class of non-steroidal “selective androgen receptor modulators” that fall under the popular umbrella name of SARMs.
Before we go any further, let me clarify something: SARMs are drugs, and as such, they have medical, ethical, and legal implications associated with them, and yet most recreational bodybuilders don’t have a clue what they are or how they work. With so much bro-science and misinformation out there, it’s become a trend of the blind leading the blind.

New Kids on the Anabolic Block
Compared to steroids, GH and other PEDs, SARMs are a relatively new ergogenic aid. In fact, SARMs haven’t been used in sport for even 20 years yet, which makes them very new. It took researchers a few decades, lots of funding, and many failed experiments, but by the late 1990s, pharmaceutical companies believed they finally had the perfect oral anabolic drug for use in clinical populations. Developing a non-steroidal substance that could do the job of a steroid by acting on an androgen receptor while producing little “sides,” being easily dosed, and having high anabolic benefits was by no means an easy feat. And if you’ve been following the bodybuilding industry closely, up until a few years ago you couldn’t easily purchase SARMs from various pseudo-supplement retailers, but all of that has changed now. But don’t let that fool you about their effectiveness, safety, or purity. As it stands, there’s a lot still to be uncovered about the newest kid on the anabolic block.

To understand SARMs, we must understand androgens. Even though androgen is dubbed a “male” hormone, men and women both produce varying degrees of androgens naturally. As an essential sex hormone, androgen is produced at different locations within the body, including the ovaries and/or testes, adrenal glands, and fat cells. While there are different types of androgens, all are steroidal compounds—little chemical messengers that share a special kind of four-ringed molecular structure.
These messages are delivered inside specific cells known as androgen receptors. As a member of the steroid receptor family, the androgen receptor is an incredibly important target for numerous pharmaceutical interventions, including, for example, cases of androgen deficiency, osteoporosis, and muscle wasting.
A host of different drugs have been created to interact with the androgen receptor in order to elicit various androgenic or anti-androgenic effects. These are known as “androgen receptor ligands” and typically are thought of as causing either androgenic results or anti-androgenic results.

How SARMs Work
Unlike steroids, SARMs can’t metabolized into dihydrotestosterone (DHT) or aromatize to estrogen, which means they shouldn’t have the same side effects such as male pattern hair loss or gynecomastia. So how do they work? The easiest way to understand this is to think of the good ol’ lock and key analogy—only certain keys can unlock certain doors. You’ve got a house that has a front door, back door, side door, and a door that provides entrance to a basement suite. You have a master key that can open all four doors. This “key” represents substances such as testosterone and other steroids. These drugs “unlock” androgenic receptors, resulting in various androgenic effects. But what happens if you only want to provide limited entrance to your house through just the basement door?
Well, you can now do that with the help of SARMs. In fact, the ability to “unlock” only selective androgen receptors was the main reason behind scientists manufacturing SARMs to begin with! In doing so, researchers believed that they would be able to minimize the undesirable side effects associated with anabolic-androgenic steroids, while being able to exploit the desirable ones—i.e., the gains—and make it happen by only needing to swallow a pill only once a day. Sounds almost too good to be true, right?

SARMs and Steroids Share Similar Risks
The chemical structure of SARMs may not “look” like steroids, yet they share many of the same risks associated with their use. They have androgenic properties and have nearly the same side-effect profile as oral anabolic steroids, causing things such as the rapid breakdown of levels of high-density lipoprotein (HDL) cholesterol and rise in liver enzymes due to inflammation. While it’s theoretically possible that using an injectable form of SARMs could mitigate these sides, the reality is that this probably won’t be manufactured anytime soon. Remember, these drugs were almost exclusively designed for oral use.
Also, keep in mind that many of SARMs’ side effects are exaggerated by taking “higher than suggested dosages”—which we all know bodybuilders and other athletes love to do.

Is There Any Research?
Clinical studies on SARMs have only been done in vitro (i.e., in test tubes), in isolated cells, or in animal studies (i.e., on rats), or on sick and old human subjects. They haven’t been tested on healthy, young active males and females. The doses within the research on SARMs are significantly lower than those required for performance-enhancing effects—and even those lower dosages have resulted in side effects! Because of how little human research has been done, scientists still don’t know the full extent of their side effects, or the long-term health damage using SARMs may cause.

Second-Generation SARMs
Currently pharmaceutical companies are testing “second-generation” non-steroidal SARMs—leaving an entire flock of first-generation SARMs behind. Why is that? Simple—the first generation (those currently being used in sport) didn’t work well enough and had far too many side effects to ever get the “stamp of approval” required for human use. No stamp of approval means no profit for drug companies. And so, first-gen SARMs got scrapped by the pharmaceutical world.

Steroids Are Far More Effective Than SARMs
First-generation SARMs being decried as useless or dangerous by the research community hasn’t stopped fitness “gurus” from manufacturing, propagating, and making millions off their sale. The hype and lies surrounding SARMs are plentiful. Most of it is nothing more than a myth, holding only a small fragment of reality. For example, SARMs do build muscle. In some of the early studies on first-gen SARMs, there were “modest gains” in lean mass—2.2 to 3.3 pounds over the course of four to six weeks. But here’s the kicker—studies on injectable testosterone resulted in 11 to 15.4 pounds over the same period! Plus, the modest SARMs gains came with nasty side effects!

SARM Code Names: What Do They Mean?
If you’re familiar with SARMs, you’ve probably noticed that many of them have code names, usually made of a combination of letters followed by numbers. The reason for this is rather simple: SARMs are patented products that haven’t been approved for human use, and are either still in—or never made it out of—clinical trial phases. They are experimental drugs that haven’t been offered for commercial sale by legitimate pharmaceutical companies.

SARMs Are Banned Substances
Despite SARMs still being experimental drugs, that hasn’t stopped athletes from using them to gain an edge. The World Anti-Doping Agency (WADA) recognized this, and in 2008, added SARMs to WADA’s prohibited list, making them one of the many substances banned for use in athletic competition. However, in terms of mainstream use, they continued to fly under the radar for quite some time. By May 2016, the FDA began exploring complaints that specific SARMs were being marketed and sold by supplement companies.

Barely Legal
For several years now, many US companies have started selling SARMs as “dietary supplements,” which has caused a few different legal issues to be exposed. Under US federal law, dietary supplements can’t include a substance that’s being investigated as a new drug, which SARMs most definitely are! So to get around this, some unscrupulous companies have added SARMs to dietary supplements without declaring them on their labels! This could have been from cross contamination in the manufacturing process or outright SARM spiking, so it’s been a classic buyer-beware situation. Furthermore, as mentioned earlier, many SARMs are patented, which means any company manufacturing them without the consent of the founding pharmaceutical company is doing so illegally. While it’s known that at least one pharmaceutical company has begun sending cease-and-desist letters to stop the illegal manufacture of a specific SARM, numerous other SARMs remain still readily available for purchase.

Legal Loophole
So how do companies get away with selling SARMs? Through the lovely legal loophole known as “research chemicals.” At this time, SARMs aren’t available for resale under any circumstances in both the United States and Canada. Yes, Canada too! Contrary to popular belief, SARMs aren’t licensed or permitted for medical or therapeutic use here either. If you doubt this, just take a look at the numerous cases against athletes who have been caught using SARMs through the Sport Dispute Resolution Centre of Canada. There are also major questions being raised about the purity of SARMs currently being sold on the grey market. Underground SARMs have been tested by academic researchers and found to contain at least 15 percent impurities. It’s another case of buyer beware that hasn’t stopped bodybuilders and other athletes from testing out various SARMs as human guinea pigs. This also hasn’t stopped researchers from continuing to develop new SARMs at an astronomical pace. Next-generation SARMs may one day fulfill the anabolic dream of providing anabolic gains without side effects. But until that day, the use of SARMs comes with very real health risks that athletes must take seriously.