Making Testosterone Obsolete – a look at SARMs

By Anthony Roberts

Sitting on my desk next to a pile of books, magazines and half eaten Chinese food is the future of athletics in a bottle. And it didn’t even involve harvesting Michael Phelps’ DNA.

The bottle itself is unassuming enough; less than four inches high, royal blue, medicine-dropper-top shrink wrapped around, and half filled with fluid. There are small crystals stretching far above the line where the liquid has stopped, a sign that the amateur chemist who suspended the active powder in poly(ethylene) glycol didn’t get it to totally dissolve. Swirling it around makes the crystals float awkwardly and retreat back into the viscous oil; my own clandestine performance enhancing snow globe.

It’s not from BALCO, and it’s not some new undetectable steroid. It’s not even a steroid. It’s better.

Anabolic steroids work by stimulating a receptor within the body called (you guessed it) the androgen receptor. Most of the effects athletes experience on steroids has to do with this steroid/receptor interaction. This innocuous looking bottle on my desktop is filled with something that has the ability to stimulate the androgen receptor and yet isn’t a steroid. It’s called a SARM, or Selective Androgen Receptor Modulator.

And it’s the future of sports doping.

The idea behind SARMs is to find an effective replacement for anabolic steroids, that are more user friendly. Most people who take testosterone either inject it or use a cream. Neither method is particularly convenient. Injections either require weekly trips to the doctor’s office, or learning how to do it yourself – and for most people self injecting conjures up images of a strung out Kurt Cobain. Creams require…well, rubbing cream on daily.

SAMS are not new idea, but rather a new approach to an old problem.

SARMs are not a new idea, just a new solution to an old problem.

The first anabolic steroid to be synthesized was testosterone. It is both highly anabolic (muscle building) and androgenic (causing male sexual traits). Testosterone remains the gold standard of steroids, i.e. all steroids are measured on an anabolic:androgenic rating against testosterone (which itself is scored at a perfect 100:100). But it’s far from ideal. It converts to estrogen and Dihydrotestosterone. Estrogen causes water retention and the development of breast tissue (yes, in males). Dihydrotestosterone causes acne, prostate enlargement, and hair loss.

So although testosterone is the gold standard, there are problems with it. Science has been working for decades to sort them out.

Dianabol was the first real contender to solving the evils inherent with testosterone. It’s an oral steroid that converts to estrogen at half the rate of regular testosterone. However, to make a steroid orally effective, the basic four ring carbon structure of it needs to be modified – and this causes the new compound to stress the liver. You can’t stay on Dianabol (or any oral steroid) for very long, and ultimately this is why people tend to prefer injections (or cream) to oral steroids.

Throughout the ‘50s and ‘60s, thousands of different anabolic steroids were synthesized, all in an effort to find the Holy Grail – a steroid that is both highly anabolic and doesn’t cause side effects. No such steroid currently exists, although several come agonizingly close. There were steroids that didn’t convert to estrogen and steroids that didn’t convert to Dihydrotestosterone, yet the side effects remained.

Trenbolone converts to neither estrogen nor DHT, and has nightmarish side effects on some people: uncontrollable sweats, insomnia, and a cough that tastes like tin. Deca-Durabolin, considered one of the mildest steroids available can cause impotence. Out of those thousands of synthesized steroids, less than a few dozen are still sold on the legitimate market (Trenbolone is not one of them). Most of the research was filed away and forgotten about. Today, the few steroids still available are prescribed for hormone replacement therapy (in men) and for diseases with wasting conditions.

The Holy Grail was never found – until now.

SARMs, the theory goes, would give you the good without the bad: the cream without the milk, the Damon without the Affleck (or the Garner without the Affleck, if you prefer).

They’ve been on the underground radar for years, along with ubiquitous rumors about their presence in the United States. Don Caitlin, the world’s premier anti-doping scientist told me that the problem in keeping up with doping is that he’s seeing drugs in a lab rat one day, and athletes the next. There’s no lag time any more, he said, exasperated.

And there’s still no reliable test for Growth Hormone or Insulin-like Growth Factor, and more performance enhancing drugs are hitting tracks and gyms daily.

SARMs aren’t on the National Import Alert List, so United States Customs isn’t looking for them yet. They’re not even illegal. Some doctors-in-the-know have heard about them, and the black market is scrambling to secure a reliable pipeline. China, now that the Olympics are over, is the most likely choice. The bottle on my desk started its life somewhere in China, made its way through Texas (by way of Houston), and then ended up in New Jersey. I know this because my bottle included something called, in chemistry jargon, a C.O.A. – a certificate of analysis. The document assured me that it was indeed a SARM.

Oliver Caitlin (yes, Don’s son) couldn’t test it for me. There’s no existing standard in the USA – and they’d need one to test it against. They have no plans to develop such a test, but where did you get it, Oliver wanted to know. I know a guy who knows a guy…

Just in case you’re guessing: The guy I know isn’t former BALCO chemist Patrick Arnold, who is also well aware of SARMs. He has been in touch with my supplier numerous times, in a thus far fruitless attempt to procure some for himself. Mr. Arnold tells us that by bypassing the classic four-ring steroidal structure, SARMs may well be undetectable for a very long time.

“This is the type of thing they use in the development of SARMS…Why confine you[rself] to the four ring structure of steroids when that is too easy for the drug testers to figure out? And (in the case of legit medicine) too politically incorrrect.”

Of course, Patrick is correct. Using testosterone for androgen replacement therapy (which is a recognized medical condition) makes you a steroid user. Like me. But…this little blue bottle I have…well, that’s not a steroid at all. So I made the decision to use it.

I hoped that the amateur chemist who mixed it up didn’t use Chinese poly(ethylene) glycol. You see, ethylene glycol and diethylene glycol are both toxic and deadly. The former is used in anti-freeze, and the latter is found in Chinese manufactured toothpaste that the FDA will not allow into America. Too toxic, they say.

Not minty enough, I say.

Theoretically SARM use should improve strength and muscle mass on par with straight testosterone. The side effects are supposed to minimal if not nonexistant, mere fractions of what you see from steroids – SARMs don’t convert to estrogen or DHT, and they don’t inhibit your own testosterone production as much as steroids do. I’m familiar with how testosterone feels, at least subjectively; for the past three years, I’ve been on supervised testosterone therapy.

And I’m not alone. Baby-Boomer aged clients have been flocking to doctors in record numbers for testosterone and other goodies, euphemistically labeled anti-aging medication. Aging, it should be noted, is not recognized as a medical condition – and the American Medical Association doesn’t recognize anti-aging as a legitimate specialty. Still, it’s a multi-million dollar niche. But there’s a problem…there’s always a problem…

Testosterone is naturally occurring…and therefore not patentable, or profitable for big pharmaceutical companies. Any company can produce and sell testosterone (and most steroids at this point, because the patents have expired). There’s just no money to be made in testosterone, and with the baby boom generation getting older and feeling worse every morning, this presents a huge problem.

SARMs are a win/win situation for the pharmaceutical companies developing them: they’re patentable, they tap into an already existing market, and they can charge an arm and a leg for them.

They are simply a ‘politically correct’ alternative to anabolic steroids” said Patrick Arnold. “They don’t have the steroid structure therefore they are not steroids, yet they are pharmacologically pretty much exactly the same as steroids.”

So I stopped taking my own prescription testosterone. I cleaned out for a couple of months, so that there was no lingering exogenous (outside) testosterone in my body and took my first SARM dose. I only received a month’s supply, and when its acrid chemical taste hit my mouth, I wished the month was over. On the underground market, many oral products are sold as liquids, even when their legitimate counterpart is a pill. Buying a large pill press now requires having your name put into a federal database – not a wise move for someone operating on the black market.

SARMs are almost 100% absorbed orally, but aren’t liver toxic like most oral steroids are. I took one milliliter each day, or 100 milligrams (this is slightly over 1mg/kg of bodyweight in my case). This is the dose most comparable to a replacement dose of testosterone, and enough to see results.

It worked exactly as advertised – testosterone without the usual testosterone-side effects. I didn’t gain much weight, but I found myself getting stronger beginning at week two and counting. I could have used ten times as much and still tested clean – easily. A professional athlete using this stuff would have a huge advantage over his clean competitors…if there remains such a thing.

The cost for my personal supply of this new drug was almost double what you could expect to pay for a similar amount of “regular” (and now passé) testosterone. This is not something that pharmaceutical companies have failed to notice, and if we see this drug hitting the legitimate American market (as it’s already on the black market, clearly), expect to see a price tag that reflects the convenience and research that went into research and development – and then some.

Undetectable, convenient, and potent – SARMs are what will replace anabolic steroids in the Olympics of tomorrow. And by tomorrow I mean yesterday, because they’re already here and available.

Besides, testosterone is so…2008.