TheGreatSatan

Written by: Manfred Bachmann.

The idea of consuming a product with limited or no biological activity in itself, which can then be enzymatically altered by the body to produce a secondary metabolite with high biological activity is by no means a new concept. This "idea" has been utilized by all aspects of the pharmaceutical industry for decades. However, this idea is relatively novel with regards to the sports supplement market. As we emerge out of the infancy of the legal pro-drug in the sports supplement industry it is both valuable and entertaining to look back and see just how far we have progressed in under a decade.

Pro-Drugs... Not Prohormones

This article has two parts: part one, which you are reading now, will discuss the various types of legal pro-drugs that are, or have been available over the last 5-6 years. Part two, which you will read in the forthcoming weeks, will deal exclusively with the myriad of delivery methods and systems utilized to get these legal pro-drugs to their target tissues.

You'll notice I am not using the words "prohormones" or "prosteroids". I don't feel that these descriptors accurately reflect the nature of the chemicals I will be discussing. Prohormone insinuates that these chemicals are not hormones until they are altered by the body. Prosteroid also insinuates that these chemicals are not steroids until they are altered by the body. This is not true; all of these chemicals are steroidal in structure and hormonal in structure. So I prefer to use a term similar to that coined by Brock Strasser of Biotest - I call these compounds "legal pro-drugs" while Strasser calls these compounds "legal steroids". These descriptors far more accurately reflect what these chemicals truly are.

The Evolution Of Pro-Drugs

Patrick Arnold, President of LPJ Research/Ergopharm is the undisputed "godfather" of legal pro-drugs as Patrick was the 1st individual to make and actively sell a legal pro-drug in the context of the sports supplement market. The very first legal pro-drug sold was androstenedione. This was an amazingly crude compound that had horribly oral bioavailability, as well as a very low rate of conversion to an active androgen (testosterone). However, androstenedione did seem to convert quite well to estrogenic chemicals. The biggest problems with the original androstenedione were that you needed to use greater than one gram (more than 1000 mg/day!) of this chemical per day to see any real improvements in strength and at that dose, the estrogenic side effects were intolerable to all but the most resistant people. Patrick quickly realized that androstenedione was not the "end all, be all" of legal pro-drugs and shortly there after launched one of the most useful legal pro-drugs we have ever seen in the sports supplement market, 4-androstenediol.

4-androstenediol (4-AD) is an amazing substance, especially when compared and contrasted to the original androstenedione. 4-AD is intrinsically anabolic before it undergoes metabolisms, being 80% as anabolic as testosterone is. Androstenedione is not active in an anabolic sense before metabolism. 4-AD converts to testosterone at a rate about 3X that of plain androstenedione. Additionally, 4-AD does not seem to impart the estrogenic side effects that plain androstenedione does. What is especially nice about 4-AD is that it imparts about 60%-80% of the effects of testosterone does on a mg-per-mg basis without the gyno (bitch tits) and water retention that testosterone can cause. Despite all the legal pro-drugs coming after it, 4-androstenediol may be the greatest legal pro-drug of all time.

If Patrick Arnold is the godfather of legal pro-drugs in the sports supplement market then Brock Strasser, Derek Cornelius of Syntrax, Bill Roberts, and Bill Llewellyn of Molecular Nutrition are the "great uncles". While Patrick Arnold was busy with androstenedione and 4-androstenediol, Derek Cornelius brought us 19-norandrostenedione - a legal pro-drug of the anabolic steroid nandrolone. 19-norandrostenedione is to nandrolone what androstenedione is to testosterone. 19-norandrostenedione "worked" but not very well. Again, it required gram per day dosing, was not intrinsically anabolic and had a poor side effects profile. It did not take very long for Derek (then working with Mass Quantities) to realize this. Teaming up with Brock Strasser, Derek pushed the envelope quite a bit and brought two new legal pro-drugs to the sports supplement market, 19-nor-4-androstenediol and 5-andostenediol. 19-nor-4-androstenediol was not only a precursor to nandrolone, it was intrinsically active in it's own right, with about 80% of the effect of nandrolone. Additionally, this compound was once patented and sold as a legit anabolic steroid by the pharmaceutical giant, G. D. Searle & Company who sold this under the trade name "Bolandiol". 19-nor-4-androstenediol was and is an amazing substance and is one of the "top three" best legal steroids currently being sold.

5-androstenediol (5-AD) on the other hand was a complete bust. Though originally touted as an amazing compound by Brock Strasser in an article of Muscle Mag, 5-AD actually turned out to be one of the most estrogenic pro-drugs we have ever seen. The 17-alpha methylated version of 5-AD called "methandriol" was a popular drug in Australia and was made even more popular by the late, great, Dan Duchaine who erroneously claimed that methandriol "cleaned out your androgen receptors". The truth is that methandriol while chemically being an "androgen" had a high estrogenic profile and was usually found as the dipropionate ester, mixed into injectable oil with "truly anabolic and androgenic substances". It was also exclusively found in the realm of veterinary medicine, where it was used to beef up cattle much like the various implant pellets people can buy today do. Adding an estrogenic substance to an androgen will cause more "growth" in cattle and since we don't care if cattle "get gyno", these type of side effects don't matter. However, they do matter in humans. I can't think of another legal pro-drug in the short history of such in our industry that has caused more detriment than the "demethylated" version of methandriol. At one point in time, Derek Cornelius actually sold a sterile suspension of 5-AD and 19-nor-5-andostenediol that many people used as an injectable, much to their detriment. Why Derek did not make a 4-AD and 19-nor-4-androstenediol suspension is not known, as these clearly would have been far better choices.

Pat Arnold brought the testosterone precursors. Brock Strasser and Derek Cornelius brought us the nandrolone precursors. And it was Bill Llewellyn who brought to us the boldenone precursors having been the 1st person to sell 1,4 androstadienedione (1,4-AD), which is an immediate precursor to the anabolic steroid boldenone. Of all the base legal pro-drugs mentioned, 1,4-AD is the one that has the highest conversion rate to its "active steroid metabolite". This doesn't mean 1,4-AD is "better than the other pro-drugs" for unlike 4-AD it is probably not intrinsically anabolic. But what it does do is it makes this pro-drug very predictable - it's effects are pretty close to that of boldenone because more of it becomes boldenone than say 4-AD becomes testosterone or 19-nor-4-androstenediol becomes nandrolone. There is another chemical being sold right now called 1,4, androstadiene-3-diol that the seller (not Bill Llewellyn) claims converts to boldenone. Basically this "3-diol" version is the same chemical as boldenone except that instead of having a "diol" in the beta position of the 17th carbon this chemical has it at the 3rd carbon. I do not know if this chemical is intrinsically active or if it even converts to boldenone to any great degree so I am not going to comment on it much here. Suffice it to say, if you are looking for a true boldenone precursor, 1,4-AD is the better bet.

After these eight pro-drugs debuted, the race was on to develop bigger and better legal pro-drugs and delivery systems. I will discuss the delivery systems in the next article but there are a few more legal pro-drugs to discuss here.

The Latest Advancements

5-alpha-androstanediol (5-AA) is a pro-drug to dihydrotestosterone (DHT). This compound was 1st introduced by Derek Cornelius through his company, Syntrax. While not a particularly good mass builder, 5-AA/DHT is quite good at "hardening" you up and many also claim it has an amazingly positive neurogenic/psychogenic effect. The downside is that both 5-AA and DHT are about the worst offenders of any legal pro-drug sold in the industry with regards to causing alopecia ie. hair loss. If you are genetically non-sensitive to androgenic alopecia then you may really like 5-AA. If you are quite concerned about your hairline then you might want to investigate other alternatives.

About two years ago, Patrick Arnold contributed yet another amazing discovery to the legal pro-drug market with 1-androstenedione; a compound that is converted into something called 1-testosterone. 1-testosterone is a chemical that is 700% more anabolic than "normal testosterone" is in rat levator ani muscle. This doesn't mean it is 700% more anabolic in humans as a host of steroids that are "significantly more anabolic" than testosterone is in rats and other rodents but are complete flops when people have tried them. 1-androstenedione did have some unpleasant side effects, causing stomach pains and urethral burning in many users. Enter Mr. Arnold's improved version, 1-androstenediol (1-AD), which is probably intrinsically active and seems to impart about 40%-60% of the anabolic effect of testosterone.

1-testosterone is an interesting compound that has a double bond in the same position that methenolone (Primobolan) does. In fact, 1-testosterone looks an awful lot like a demethylated version of methenolone, a fact not lost upon Bill Roberts. Bill decided that since 1-testosterone is not on the DEA's controlled substance list and is naturally occurring, why waste time with a pro-drug of it (1-AD)? Why not just sell 1-testosterone itself? Indeed, that is exactly what Bill Roberts did. Most users report that 1-testosterone causes an effect somewhat between that of trenbolone and methenolone, which makes a lot of sense if you look at the chemistry and stoichiometry of 1-testosterone. 1-testosterone is clearly the most inherently potent of the legal pro-drugs we have seen to date.

Some time ago, Pat Arnold again launched an amazing pro-drug. This chemical is called 3,6,17-androstenetrione known as 6-OXO. What sets the "trione" apart from all the other pro-drugs is that this chemical is not meant to be a "mass building anabolic" but rather, it is an exceptional suicide inhibitor of the aromatase enzyme, making it similar to the prescription drugs letrozole and anastrazole. The trione quite literally knocks all the estrogen out of your body and certainly prevents any aromatizable steroid from becoming an estrogen. At about the same time as Pat launched this trione, Bill Llewellyn decided to launch 4-hydroxyandrostenedione (4-HA) which is a prescription, injectable, anti-aromatase sold in Europe. Although 4-HA is probably active orally as an anti-aromatase, it is my opinion that this is being sold illegally. There is an active patent on the compound (look up Formestane) and it is unlikely the patent holder or the FDA will allow Bill to sell this compound for much longer.

What's Next?

So what's next? What is new on the horizon in the legal pro-drug market? I guess we will have to wait and see. I don't think we're going to see too many new legal pro-drugs but I am confident that we will see a host of new delivery systems for the existing pro-drugs, delivery systems that make these more effective, causing less side effects and requiring smaller and smaller dosages. In fact, the company I am working with, Nutrex Research, is investigating an interesting compound that has about 60% of the effect of methandrostenolone (Dianabol) without the aromatization issues that using D-bol causes.

Written By Manfred Bachmann