5α-androstane-3,6,17-trione - Kneller's Trione: Newly Patented Aromatase Inhibitor that Raises Testosterone Without Lowering Estrogen Levels!?

I happened onto an interesting patent (Kneller. 2011), published on 02/10/2011 the author of which, Bruce Kneller, who was arrested in the course of a steroid bust back in 2006, claims to have invented an aromatase inhibitor, 5α-androstane-3,6,17-trione (Kneller's Trione) which produces "substantial and significant increases in plasma testosterone levels in men while inducing no changes outside the accepted normal limits for plasma estradiol levels". This is very different from your usual AI (ATD, Arimidex, Letrozole, etc.) which tend to eradicate estrogen and thus produce nasty side effects. As far as its concrete applications are concerned the author writes:

The oral, daily dose of Kneller's Trione can be from about 25 mg to about 750 mg per day, such as, for example, from about 25 mg to about 500 mg per day, from about 25 mg to about 250 mg per day, or from about 25 to about 100 mg per day. [...] In some embodiments of the invention the composition comprising Kneller's Trione is formulated as a tablet, capsule, caplet, powder, suspension, gel preparation, aqueous solution, solid food form (e.g., chewable bar or wafer), or liquid dosage form such as elixirs, syrups, dispersed powders, granules or emulsions.

Bruce W. Kneller then cites a pilot study in which Kneller's Trione was administered orally to three individuals at dosages of 25mg, 50mg and 100mg.

Figure 1: Tables from patent of Kneller's Trione

As can be seen from the tables in figure 1 the effect of 5α-androstane-3,6,17-trione depends on a) previous hormone levels and b) dosage. Most interestingly administration of 50mg Kneller's Trione to subject 2 who had low estradiol levels to begin with did not reduce these levels any further. With reference to the optimal dosing scheme and potential side effects Kneller reports:

Although dosing of Kneller's Trione went as high as 750 mg per day in this pilot study, no added benefits were seen with dosages this high. Dosages of 250 mg and 500 mg per day also raised total testosterone and bioavailable testosterone levels substantially and safely but did not seem to offer any added benefit over a dose of 100 mg per day. At the 750 mg per day oral dosing level, occurrence of a priaprism caused the subject to withdraw from participation in this pilot study. No other adverse events were noted by any study subject during this pilot study. Observations of every subject's liver function, kidney function, blood lipid levels, blood pressure, heart rate, respirations, and body temperature were made at frequent intervals during this pilot study and were found to be within medically established normal ranges and values.

While my cursory web-search for available OTC supplements with this product did not produce any results, I assume it won't take long until we see a range of these products on the market - even in view of the fact that a constant boner (priapism) may not be the worst, but certainly an annoying and in the long run painful side effect ;-)

As always, I will inform you as soon as there are more recent study results and or product releases. In view of the fact, that Kneller is also the patent-holder of the "OUTLAST" formula in Gaspari Nutrition's cell-volumizer SizeON it's most likely that we will see a "new Novedex XT" hit the market soon.

Edit: Kevin just posted a comment mentioning, he believes that it is already in "some Gaspari products" and in fact. He is right! Its part of Gaspari's Halodrol MT, which I believe is not produced anymore, though. Well, I assume that's what happens to things which work, these days...