By now, most of you have heard about the most potent, legal prosteroid ever conceived or sold on planet earth— Methyldienolone® (17a-methyl-17b-hydroxyestra-4,9(10)-3-one)— discovered by yours truly. It literally can’t be beat as far as oral, legal stuff goes. It is highly anabolic, not very androgenic and works in doses as low as 1/4 milligram per day (in women) and one milligram per day (in men), amazingly. I keep hearing folks comparing it to a hybrid of Winstrol (stanozolol) and Parabolan (trenbolone). In fact, a lot of people are now calling Methyldienolone® “trenbolone’s little brother,” which I find ironic since it’s at least 50 times more powerful than trenbolone milligram for milligram. I actually could swear I heard that Bill Phillips said it “feels like Deca” and I got an e-mail saying TC Luoma went around smashing in steel walls and doors after taking a few doses of Methyldienolone®— it made him that strong!

OK, OK, I’m kidding. I’m making a good on Phillips’ fatal words about HMB feeling like Deca and Luoma’s quote about BioTest’s MAG-10 product (which actually is a pretty good product). But, hey, I have an e-mail “inbox” of success stories of men and women using this new stuff. Listen, Rich Gaspari was so impressed with Methyldienolone®, the former multi-Olympia, Arnold and Night of Champions competitor has licensed the name from me and is now selling the stuff and selling at ton of it under his Gaspari Nutrition label.  That says a lot. Rich is a smart bodybuilder, one of the smartest ever.  Remember, back in his heyday, Rich came in second only to Lee Haney at the Olympia and Rich did this with substantially less than good genetics for bodybuilding. He had to be very smart and clever about what he used and did in order to place second for the Sandow behind Lee Haney. 

The fact that this guy has chosen my idea as one of his “prohormones of choice” to sell should speak spades about it. One of the largest wholesalers of sports supplements told me they can’t even get enough of this stuff to cover their retailers’ demands. So, apparently, you guys like the stuff. And why wouldn’t you? It is amazing; it is the best oral prosteroid that will ever exist in our industry, end of discussion. It blows 17a-methyl-1-testosterone, its closest contemporary, way the fuck away.

But sadly, this and other prosteroids, in fact, all prosteroids and prohormones, are more than likely going to be illegal in the next 12-18 months. First it was norephedrine/phenylpropanoloamine and now we just lost ephedra. The dark ages will be upon us soon guys, bans will be coming and my guess is any hormonal supplement that’s outright anabolic or converts to something anabolic is going to be banned and made schedule C-III. I mean, keeping a few thousand bodybuilder types smaller or turning them into criminals is so much more important that rebuilding Iraq or finding Osama bin Laden or dealing with any of the other thousands of ills that plague the world and America. But I’ll get off my soap box and deal with reality.

    Dealing with Reality
Actually, I have been dealing with reality for a while now. My company, Therachem, is no longer interested in developing prosteroids. We’re focusing on what is ultimately going to be the next best thing. See, if you can’t (at least legally) increase the amount of an anabolic substance in your blood by ingesting it outright, the next best thing would be to coax your body into making more anabolic stuff on its own, right? Today, there are some pretty good supplement anti-estrogens and anything that’s a true anti-estrogen is going to cause the body to produce more testosterone (our “anabolic substance”!).  From an herbal standpoint, Tribulus and Vitex are your best bets for increasing endogenous androgen levels. I happen to like BioTest’s “M” product and even more than that, I like Nutrex Research’s “Vitrex” product. Both are exceptional herbal anti-estrogens that can cause an endogenous increase in the amount of testosterone. There are two other products that are currently being sold that are single-agent hormonals that are amazing anti-estrogens.

King among these is 4-hydroxyandrostenedione (4-OHA, also known as Formestane and sold under a whole host of supplement brand names by over a dozen companies). This stuff works amazingly. It’s a fantastic anti-estrogen, actually; it is an anti-aromatase by mechanism of action, which makes it even better than just merely “blocking” the actions of estrogen. Even better, Formestane is a 5-alpha reductase inhibitor (J Steroid Biochem Mol Biol, 1992 Jun;42(5):509-14), so it will prevent testosterone from converting to DHT. In addition to raising endogenous testosterone levels, 4-OHA will help you keep the hair on your head if you have a tendency toward male pattern baldness.  4-OHA is an amazing substance. No doubt about it.

But pucker up and kiss it goodbye soon. It’s only a matter of time before 4-OHA is removed from the supplement market. First of all, it really isn’t a supplement at all, it is a drug, a real drug, that has been used, and still is used, to treat post-menopausal women who have breast cancer. So for that reason alone, you can expect the FDA to yank 4-OHA in a matter of months. Drug companies making bazillions of dollars and charging mega money per dose don’t exactly like it when some supplement companies come along and sell the exact same compound for one-tenth the price (only we just can’t and don’t claim it’s effective in treating breast cancer, or anything, for that matter). But the other problem, aside from the fact that 4-OHA is a real drug is that it has a metabolite, 4-hydroxtestosterone, that is a pretty cool anabolic in its own right.  That alone will eventually be enough to get 4-OHA dethroned and banished to the ash bin of supplement history.
So where does that leave us next? With the upcoming abdication of the king of anti-estrogens (4-OHA), we are left with the “queen of anti-estrogens” I guess?

Playing Poker and Sports Supplements
6-OXOtm (3,6,17-androstenetrione) is the brainchild of Patrick Arnold, a guy who is certainly a pioneer in the supplement industry for sure. Sold through his company ErgoPharm, 6-OXOtm is a popular product that’s a very effective anti-aromatase, anti-estrogen (which again, means it will cause the body to produce more testosterone, which is, of course, what we want and what this discussion is about). Pat did his homework with this supplement; it’s not just one of the best supplements he sells, it is one of the best supplements sold, bar none. And the best part about it is that even though it’s a hormone, it has no inherent anabolic/androgenic properties by itself, nor do any of its first-degree metabolites. This means it’s probably as “FDA proof” as any supplement is going to get (if such a category is even possible). When the proverbial brown stuff hits the giant FDA supplement-slicing-away-off-the-market fan in the next year or two, 6-OXOtm will probably be allowed to remain on the market and thus, it will be instantly propelled to the forefront of the “supplement dome” as the most effective supplement for raising endogenous anabolic substance (testosterone) levels. Or will it? Or does someone else have an ace up his sleeve to trump Arnold’s queen?

Do any of you play poker? I do. I’ve been playing for years. I play Texas Hold ‘Em and Omaha Hold ‘Em. I learned to play after I saw a movie called “Rounders” with Matt Damon and Ed Norton. Great movie, by the way. I suggest you rent the DVD if you need something cool to watch some night. Poker has become ever more popular since ESPN televised the World Series of Poker and a long-shot amateur named Chris Moneymaker walked away as the champion. Now, everyone and their mother plays poker and they think they’re the next Doyle Brunson, Scotty Nguyen, Johnny Chan or Phil Helmuth. I like sitting down next to fish like these because it means I come away a winner most of the time. I’ve actually competed in eight poker tournaments and believe it or not, I won the last one I entered and walked away with $25,000 (well, less than that after taxes) after 17 hours of almost continuous poker play. I play a tight and conservative game, usually rarely bluffing or semi-bluffing. If you’re in a casino, check out some of the 20/40 or 40/80 tables and you might find me sitting in, hopefully taking down stacks if chips sky high, thank you very much.

I mention poker because the supplement industry from behind the scenes in the R&D area is a lot like playing poker. Each company is interested in what the next company is working on (the other guy’s hand) and is trying to protect other companies from finding out what they’re working on (their hand).  Basically, it’s just like poker: I want to see your hand or guess your hand without you guessing mine, so I can decide what to do next; know when to hold ‘em and know when to fold ‘em.

Just like in real poker, in online conversations and in media interviews, a lot of the brains behind what’s soon to be coming out in the supplement world either bluff (that is to say they lie or misrepresent which way their product development is going, to throw off competitors), stay silent until they’re ready to drop one whale of a bomb, or they have such an unbeatable hand, maybe like having a straight or flush in poker, that they just lay their “supplement cards down” for the world to see and collect their huge “pot” of consumer money, which you guys spend on worthy stuff.

So allow me to “set up” a mythical “Supplement Hold ‘Em” poker game for you as I see it now. At this table we have “Poker” Pat Arnold from ErgoPharm, who after the two hole cards and the flop is definitely in it with 6-OXOtm for sure. The other supplement luminaries and gurus, “our serious and professional poker players” say Bill Roberts from BioTest, Bill Llewellyn from Molecular Nutrition, Caleb Stone from Avant Labs, Derek Cornelius from Syntrax and yours truly.  Well, it looks pretty much like we’re fucked hard and put away dirty. With the impending ban in the majority of hormonally based supplements and his cool and effective 6-OXOtm product, it’s looking like Patrick “has the nuts” after the flop, his tell is so obvious. 

I’m watching my contemporaries at this mythical “Supplement Hold ‘Em” poker game just throw their cards in the muck and fold out. Maybe they move onto a different approach in a different game. Hey, there are all sorts of new Creatine products in the pipeline and insulin mimickers and whatnot. And maybe that’s what my contemporaries are going to work on after folding on the anti-aromatase hand. I really don’t know. And I really don’t care because I am still in it. Yes, Pat’s holding a monster hand after the flop and 6-OXOtm looks to be unbeatable, I admit it. The key word is “looks.” Because while the 6-OXOtm hand is a fantastic hand, almost like getting a belly buster nut straight with the two hole cards and the three card flop right from the get-go. Maybe it is not unbeatable after all. Maybe at the run and the river, 6-OXOtm will not be enough?

Guess What?
Kneller has been dealt a pair of pocket rockets in the hole (that’s a set of aces for you non-poker types) and although the flop did nothing to improve my supplement poker hand, the final two cards, the turn and the river cards, well maybe they’re going to both be aces or maybe create a set of trips (that’s three of a kind) for show on the board, giving me a full house which croaks the 6-OXOtm nut straight Pat Arnold is holding. I don’t know. So I am going to tell you guys about my new anti-aromatase that like 6-OXOtm  does not have any inherent anabolic activity and does not convert to anything that has any anabolic activity. Yet like 6-OXO,tm it is a suicide inhibitor of aromatase that will lower estrogen levels and thereby raise testosterone levels. Actually, my compound (patent pending, by the way, in case any vultures think they’re getting free R&D out of me) is a metabolite of 6-OXOtm actually.  6-OXOtm happens to be a prohormone to my anti-aromatase!

So what is it? The compound is called 3b-hydroxyandrost-4-ene-6,17-dione (3-OHAT) which is the 3 beta-reduced metabolite of 3,6,17-androstenetrione. The only difference between the two is that at carbon 3b, my molecule has a hydroxyl functional group and Pat’s has an oxo/keto functional group. 3-OHAT has been absolutely shown to be a competitive (Ki = 6.5 microM) and irreversible inhibitor (suicide inhibitor) of aromatase (J Steroid Biochem,1987 Sep;28(3):337-44). Actually, 3,6,17-androstenetrione (6-OXOtm ) is rapidly metabolized into 3-OHAT and more than likely, most of 3,6,17-androstenetrione is really due to that of the metabolite, 3-OHAT. Both do the exact same thing (6-OXOtm and 3-OHAT) in the exact same manner because ultimately 6-OXOtm becomes 3-OHAT. The question now is: Which one is better?

Honestly, I do not know. And for that matter, it’s too early to tell which one will be better. Obviously, both will be highly effective anti-aromatic, anti-estrogen supplements that will survive the forthcoming “supplement hormonal excoriation” by Congress and the FDA.  3-OHAT has one advantage over 3,6,17-androstenetrione that I can think of. Because it has a hydroxyl at carbon 3, this could be replaced with something like an ethyl carbonate ester or THP ether (covered in my patent application, by the way), which would make the entire thing much more lipophilic.

This could mean that the bioavailability of a 3b-ester or 3b-ether analog of 3-OHAT might be vastly more bioavailable per the oral route than either plain 3-OHAT or 3,6,17-androstenetrione. This might mean that you, as the consumer, might be able to get away with once-per-day dosing and smaller dosing, clearly two advantages. It’s too early to tell yet, but what I can tell you is that a 3-OHAT ether product is in the works by yours truly and it will be launched via Kilosports and more than likely, Rich Gaspari and his Gaspari Nutrition company (and a few others). It may be better than 3,6,17-androstenetrione or it may not, but it will work very well at its intended purpose and it will remain (or at least should remain) legal.
Well guys, let’s go turn those final two cards in the supplement poker game and see what happens next, OK? Like they say in the World Series of Poker…”I’m all in.”

3-OHAT (3b-hydroxyandrost-4-ene-6,17-dione aka “Kneller’s anti-aromatase”)

6-OXOtm  (3,6,17-androstenetrione)