The Only Truly “Orally Active” Prohormone

Natural androgenic steroids are normally not very active orally. Large amounts have to be taken orally to see biological effects. This is because the first pass through the liver causes a massive deactivation of the compounds, primarily through the oxidation of the 17beta-hydroxyl to a 17-keto group. Chemists long ago found that by adding an alkyl (methyl or ethyl) chemical group to the alpha position of the 17 carbon, this oxidation can be prevented. However, this alkyl derivatization also greatly increases the liver toxicity. Therefore the usage of such synthetically altered compounds (methyltestosterone, oxymetholone, stanozolol) are not without substantial risk.

Luckily, there are other ways to render a steroid orally active, and do so without making the compound toxic to the liver. Certain structural modifications can alter the metabolism of steroids making them resistant to liver breakdown. One of these modifications is unsaturation (presence of a double bond) in the 1-position. One steroid that has this structural modification and is orally active is the anabolic steroid Methenolone, also known as Primobolan.

A Natural Hormone Made in the Body

One of the beautiful things about 1-AD is that in addition to its impressive pharmacological activity, it is also a natural androgen made in the human body(4) . This means that it is not foreign to your body, and that it can legally and openly be sold as a nutritional supplement. Furthermore, 1-AD’s high rate of active conversion after oral administration is not just a “theory”– it has been demonstrated and published in a highly reputable peer reviewed journal.

Summary

Let’s put it all together and see what 1-AD has to offer:

There can be no argument that this is the ultimate prohormone. Believe us, there simply are no natural compounds out there that can come close to what 1-AD does, so don’t even bother looking.

References

1.Counsel et al., “Anabolic Agents. Derivatives of 5alpha-Androst-1-ene”, J. Org. Chem., 27 (1962), 248-251
2. Galletti and Gardi, “Metabolism of 1-Dehydroandrostanes in Man”, J Steroid Biochem, 3 (1972), 933-936
3. Langecker, “Beziehungen Zwischen Substitution im Ring A und Abbau im Stoffwechsel bei Verwandten des Testosterons”, Acta Endocrin, 41 (1962), 494-506
4. Lieberman et al., J. Biol. Chem, 182 (1950), 299
5. Galletti and Gardi, “Metabolism of 1-Dehydroandrostanes in Man”, J Steroid Biochem, 3 (1972), 933-936

1-AD FREQUENTLY ASKED QUESTIONS (FAQ)

What do you mean specifically when you say that 1-AD converts to a hormone that is over 7 times as anabolic as testosterone?
1-AD converts to an isomer of testosterone known as 1-testosterone. The anabolic potency of 1-testosterone and testosterone were determined (Counsel et al., Anabolic Agents. Derivatives of 5alpha-Androst-1-ene, J. Org. Chem., 27 (1962), 248-251) by the rat levator ani assay, which is the way that steroids have traditionally been tested for muscular anabolic activity.

In this study, testosterone was assigned a myotrophic potency of 26, while 1-tesosterone was given a myotrophic potency of 200. These potencies were determined by measuring the minimal doses from which significant increases in muscle weight were observed. It took over 7 times LESS 1-testosterone than testosterone to produce the same increases in muscle weight.

To sum it up, this means that it should take much less 1-AD to stimulate your muscles to grow than with a testosterone precursor like 4-androdiol (4-AD) — and this is without taking into consideration 1-AD’s oral bioavailabilty advantage over traditional prohormones.

1-AD sounds good in that it doesn’t convert to estrogen, but what about DHT? Is this going to have the same effects as Andro on my prostate?
While 1-testosterone can convert to DHT through an unusual pathway, the extent of that conversion is unknown. The extent of 1-tesotsterone’s impact on the human prostate is unknown as well. According to assays on rats, prostate growth is similar to that with an equal dose of testosterone. But this is in castrate rats that have underdeveloped prostate glands to begin with. This kind of prostate growth (developmental growth) is in no way the same thing as benign prostate hypertrophy (BPH), the kind that can be damaging in humans.

Since BPH is estrogen dependent, there is a possibility that 1-AD is in fact very prostate friendly. In case you do not know, DHT given by itself can actually reduce BPH because it reduces serum estrogen (US patent# 5,648,350, Dihydrotestosterone for use in androgenotherapy). The same may be true for 1-AD — at this point we don't really know.

I know you say that a lot of this makes it past the liver, can you give a rough percent?

All I can say is that more gets through than for other prohormones. This is based on data examining the recovery of active 17-beta hydroxy steroids from the urine of subjects given various steroids including 1-AD (Galletti and Gardi, Metabolism of 1-Dehydroandrostanes in Man, J Steroid Biochem, 3 (1972), 933-936).

What do you mean specifically that 1-AD is not outstanding for mass gains?

1-AD can put bodyweight on you, but if you compare the strength and pure muscle gains to the overall bodyweight increase it is less than what you would see associated with an aromatizing steroid like testosterone (for the same given amount of strength and pure muscle gains). This is because the mass gains seen with 1-AD are not associated with water retention.

This is considered by many to be a very desirable property in an anabolic agent. It is for this reason that strong anabolic steroids such as Trenbolone, Halotestin, and Winstrol are so treasured for pre-contest usage. These steroids are not noted for promoting great body weight increases, but they increase pure muscle mass considerably and without definition-obscuring water.

Would 1-AD be a good product to use for losing fat or cutting up?? I assume it would be anabolic enough to counteract some of the catabolic effects of an aggressive dieting program.

1-AD can be extremely useful for cutting up, and this is probably its most valuable use. While 1-AD will not impart any direct fat burning effects like you would get from a thermogenic product, it can assist in losing fat indirectly. 1-AD can minimize the loss of lean body mass (LBM) while dieting, aiding in the maintenance of a high basal metabolic rate.

While all prohormones can help maintain LBM, most of them also convert to estrogens. Estrogens promote fat gain and therefore their elevation is counterproductive while dieting. 1-AD does not increase estrogen levels making it a superb prohormone choice for cutting-up.

Furthermore, since 1-AD has little associated water retention, your muscle definition will not be adversely affected. You will maintain a lean, hard look to your physique.

What about stacking 1-AD with other types of prohormones? Is this advisable? Would this help mass gains??

Stacking 1-AD with 4-AD (Androdiol®) or nor-4-AD (Norandrodiol®) prohormone products can be of value. You can get the mass gain benefits of the diol prohormones combined with the strength benefits of 1-AD.

In particular, stacking 1-AD with one of the topical spray prohormone products should be very effective. Such a stack would include a sustained release component with an oral, fast acting component. This would be pharmacokinetically similar to a traditional “injectable/oral stack”.

Could you give some dosing and cycling info for 1-AD?

The recommended dosage is one to three capsules (100-300mg) per day with meals. If three capsules are taken, then these should be spread out over the day (i.e. breakfast, lunch, and dinner). Subjects have taken more 1-AD (600-900mg per day) and gotten excellent results with no adverse side effects, but the (conservatively labeled) bottle tells you to limit your intake to 300mg per day.

Can women take 1-AD?

1-AD is significantly androgenic, which means that it will put women at risk for virilizing effects much more so than a low virilizing product such as Norandrodiol®. For that reason, it would probably be advisable for most women to avoid 1-AD. Some women may be able to tolerate one capsule a day perhaps, but certainly for the majority of women it is just a better idea to take a Norandrodiol product.

How do I cycle 1-AD?

A cycle of 1-AD can vary between 2 weeks and 10 weeks. However most cycles are from 4-6 weeks long. Maximum results are usually seen within 4-6 weeks. Be advised that the longer you stay on 1-AD the more substantial the suppression of endogenous testosterone production will be. Restoration of endogenous production of testosterone can be accelerated by the use of 6-oxo, however the effectiveness of 6-oxo will become less and less the longer the 1-AD cycle is prolonged.

The off cycle time should be 1-2 times the length of the on cycle.

How should I stack 1-AD with other prohormones?

The most common cycle of 1-AD is to combine it with the testosterone precursor 4-AD, usually a topical such as Androspray. This stack will allow for a little extra size due to the water retaining properties of testosterone, and also might help minimize any loss of libido from the use of 1-AD alone.

What is the recommended dosage of 1-AD?

The recommended dosage is 1 to 3 capsules a day. However, some people have found that greater results can be obtained with as much as 3 to 9 capsules a day.

What are the possible side effects of 1-AD?

Side effects from 1-AD are not serious, however several have been reported and you should be aware of these.