SARMS – Functional Fitness

Back in 2007, a nondescript bottle with a medicine dropper was delivered to me at my Texas address. Inside the unmarked bottle was MK-2866 (Ostarine), a Selective Androgen Receptor Modulator (SARM) – it was one of the first bottles produced specifically for the black market, and I was likely the first person to experiment heavily with the drug. Fast forward to 2015 and it’s become the first legit performance enhancing drug to cause a positive result in CrossFit’s doping program.

I’m not going to get into my thoughts on the actual positive result, or whether I believe the athlete’s excuse of cross-contamination holds water – but I will say that I believe SARMs are a great choice in terms of PED use in the functional-fitness world, especially if you’re not worried about being tested.

With SARMs, the mechanism of action is Androgen Receptor (AR) stimulation – which is a large part of how anabolic steroids exert their positive effects. Generally speaking, Selective Androgen Receptor Modulators bind to the receptor and cause both muscle and bone to hypertrophy, which is where we get the name Ostarine (osteoporosis, etc…). There are different SARMs with slightly different effects on either bone or muscle or whatever, but they’re all basically anabolic with few side effects. However, because SARMs aren’t actually a hormone per se, there is no conversion to metabolites like estrogen or dihydrotestosterone. For most people, this translates to less side effects. Early on, it was believed that SARMs didn’t effect hormone levels at all, but now it’s been proven that they actually do reduce natural testosterone levels.

Back in 2007, when I started using Ostarine, a positive test would have been impossible, because at the time it was still undetectable. In fact, when I spoke to the top doping lab in the country, in December of that year, they knew nothing about it, and didn’t want to know anything about it. Until records start falling and rumors start circulating, the anti-doping crowd is comfortable maintaining the status quo. And as these drugs were still in the experimental phase for the companies developing them, nobody had even thought to develop a test. Within a few years, that would all change…They were specifically banned by the World Anti-Doping Agency (WADA) in January 2008, a month after I’d received my first bottle – marking one of the first times a drug was banned before it was actually on the market or in clinical use.

Selective Androgen Receptor Modulators were born from the pharmaceutical industry’s desire to create something that could provide the benefits of traditional anabolic/androgenic steroids(i.e. increased muscle mass & strength, fat loss, and bone density), but without being an actual steroid. Steroids, you see, are bad (mmmkay). The public doesn’t like steroids because cheaters use them to hit homeruns. And steroids are old – like really old. There have been literally hundreds of anabolic steroids synthesized and documented in the scientific literature, even if only a few dozen ever made it to the legitimate market…of which very few still remain (alas poor Trenbolone). This is a shame because while steroids have been taken off the market due to an unfavorable political climate, wasting diseases such as HIV/AIDS and Cancer (or just plain old aging), haven’t likewise disappeared.

Another factor in the interest and ultimate marketability of SARMs is the fact that they are oral – and most people hate injections. Testosterone replacement therapy is at an all-time high, and that’s due in part to the various delivery methods that have garnered FDA approval – i.e. creams, patches, and gels. Previously, those who wanted to avoid injections had very few options:

1. Andriol (very expensive and only moderately effective)
2. Methyltestosterone (toxic and not effective on a mg/mg basis)

Therefore, SARMs were developed as an alternative to oral testosterone, while being more effective and less toxic. They combine high oral bioavailability with reasonable effectiveness. In terms of a standalone oral anabolic, I’d be hard pressed to think of an alternative that was more effective without being far more toxic. A good equivocation would be that the anabolic effects of SARMs are similar to a low-ish dose of injectable testosterone.

I have a suspicion that there isn’t a great dose/response curve here, and that taking a ton of Ostarine (or whatever) won’t cause muscle and strength accrual similar to a whopping dose of steroids…but then again, I don’t know anyone who’s tried. For bodybuilders and powerlifters, who are pushing the envelope of polypharmacy with little to no oversight from doping authorities, anabolic steroids will always provide greater value than SARMs. If you’re an athlete of the CrossFit/Functional-Fitness variety, SARMs would provide a significant edge, at a fairly low dose and cost. However, as we’ve seen in CrossFit, SARMs are detectable – (ergo, if you’re reading about something in 2015 that I wrote was undetectable back in 2009, use some common sense).

Still, detectable or not, they’re widely available, effective, and being widey used, and I doubt that’s going to change any time soon.