Bolasterone has a reputation as one of the most potent and toxic AAS ever produced. The name “bolasterone” was used to not only describe the above steroid, but also by an underground lab that for a counterfeit drug that consisted of anadrol tabs ground up and dissolved in testosterone cypionate. Underground labs and even supplement companies will occasionally use the names or previously and currently marketed AAS in some form to give their products instant cache. The true bolasterone, whose structure is shown above, was rumored to be the most effective steroid on the market. It was also rumored to be very liver toxic, in fact, probably the most liver toxic of all commonly available steroids.
While the addition of the methyl group at the C-7 position did increase the binding to AR slightly, it also increased the binding to PR 3-4 fold resulting in a substantially progestational molecule. This significant progestational activity combined with the strong androgenic activity is probably what led people to believe that this was such an effective molecule. This activity would cause rapid and large increases in skeletal muscle, body fat accumulation as well as water retention, which would all result in large body weight increases. This is evidenced in the anabolic/androgenic ratios of bolasterone that show it to be ten times more anabolic than testosterone and twice as androgenic.
The 7-alpha methyl group seems to interfere with 5-alpha reduction but it is likely that this molecule was still vulnerable to aromatization1. This steroid was removed from the market soon after its introduction because of problems with liver toxicity. This created a new problem. The reputation of bolasterone’s effectiveness inspired the production of several counterfeit concoctions after it was removed from the market. None of these counterfeits contained actual bolasterone but were instead a mixture of other steroids (usually a testosterone, anadrol and deca) that was supposed to mimic bolasterone’s effects. They slapped the bolasterone name on the counterfeits and made a bundle off of the reputation of the real bolasterone.
Why did I bother to tell you about this when neither the real bolasterone nor the counterfeits are currently available? There are several reasons. The first is that steroids have a way of popping up on the black market. There are always several illicit manufacturers in operation around the world that are capable of making just about any steroid. So, you never know if real bolasterone or a “new” fake will pop up again in the future. Second, the structural motif of bolasterone is important in understanding how different substitutions change a molecule’s activity. Third, to make you aware of the fact that, when it comes to counterfeits, you can never be quite too sure of what is really in the bottle.
1. Schanzer W: Metabolism of anabolic androgenic steroids. Clin Chem. Jul;42(7):1001-20, 1996
Adapted with permission from Seth Robert’s Anabolic Pharmacology, all rights reserved.