would like to know more about formestane

[Ritch]

I`ve been curious about this compound as it`s touted as a natural AI. Have searched the site here and nothing came up. Was curious if anyone used it, during or after a cycle as pct and the protocols used. Formestane only costs $15 for 5 grams. The only info I found was on BB.com and I don`t trust what those 150 lbs nuggets have to say about anything related to getting big!

Ritch

[AlbertaBeef]

Looks good for post cycle and bridging. I found some quick info on it but I haven't tryed it.Formastat™ -- Clinically Proven Anti-estrogen
Reprinted by permission from William Llewellyn, author of Anabolics 2002

Molecular Nutrition, the company that introduced the first steroidal aromatase inhibitor to the sports supplement market just a year ago, has teamed up with Syntrax Innovations to bring the war on estrogen to a close, once and for all. Formastat™ contains the suicide aromatase inhibitor formestane (4-hydroxyandrostenedione), a clinically proven anti-estrogen exceedingly more potent than any supplement to come before it. 6-oxo-androstenedione, chrysin, indole-3-carbinol, calcium d-glucarate, trihydroxystilbene, not even our old Viratase (5-alpha-androstanedione) can't come close. All of them combined in one capsule still wouldn't even have a shot. Formastat™ is such a revolutionary advance in the area of estrogen suppression because it contains the only agent backed by not one but numerous placebo-controlled human medical studies, and so effective it is actually a prescription breast cancer drug in other countries.




Formestane (4-hydroxyandrostenedione)


Suicide Aromatase Inhibitor
Formastat is in many regards similar to a competitive steroidal aromatase inhibitor like Viratase. Both are steroidal compounds that work by attaching to the active binding site of the aromatase enzyme, preventing it from interacting with other steroids (such as testosterone) that are capable of being converted to estrogen. With the enzyme binding site occupied, it is for all intents and purposes inactive. If the inhibitor is present in a high enough level it will dramatically suppress estrogen concentrations in the blood. The difference between a competitive inhibitor like Viratase, and Formastat, is that the former will detach after some time, rendering the enzyme active again. Formastat on the other hand binds permanently with the aromatase enzyme, making it useless until the body actually replaces it through the normal metabolic attrition of enzymes. This type of compound is called a suicide or irreversible aromatase inhibitor, and has the benefit of being both highly selective in its action on estrogen and long-lasting in effect.

Because of its potent estrogen-suppressing action, 4-hydroxyandrostenedione has been successfully used on breast cancer patients in many other countries including England, Germany, Switzerland, Spain, Australia, New Zealand, Italy and Malaysia.12345678 It has been shown to be an effective option often compared to tamoxifen (a prescription drug). Those of us in the bodybuilding world looking to mitigate the physiological effects of estrogen for other purposes have likewise been confronted for the first time with a legal supplement that has all the actions and potency of a pharmaceutical agent, which would normally be obtained only with a doctor's prescription.

Dose and Pharmacokinetics
After oral administration peak levels of 4-hydroxyandrostenedione are reached in the blood at approximately 1.5 hours, and the drug is cleared from the body with a half-life of approximately 3 hours. Due to its nature as an irreversible inhibitor, its estrogen-suppressing activity outlives it actual active lifespan in the bloodstream. Studies have demonstrated that maximum estrogen suppression is achieved with an oral dose of only 250mg per day12. Doubling this dose to 500mg, or even quadrupling it to 1000mg, was shown to have no effect on aromatase inhibition or estrogen levels appreciably different from the 250mg dose.

The Need for Estrogen Maintenance
Estrogen has both positive and negative effects that you should be aware of. On the positive it supports "good" high density cholesterol, increases muscle glucose utilization for tissue growth and repair, and even increases androgen receptor concentrations in various tissues. It is now understood that estrogen serves many useful purposes in men, particularly if we are looking for rapid muscle mass gain. If bulk is the goal it is therefore usually advised to hold off on estrogen maintenance compounds until there is a clear need for them. This brings us to the negative side of estrogen, namely that it can work to hide muscle definition by increasing water retention and fat buildup. It can also promote gynecomastia (the development of female breast tissue) in men if levels get too high. Since androgens and estrogens playing opposing roles on the disposition of body fat and the growth of mammary tissues, maximizing the ratio between these two hormones is often an important objective, particularly at times when dieting and cutting are key goals or gynecomastia is a worry because strongly aromatized hormones such as testosterone are being supplemented.

Testosterone Stimulation
Despite the fact that 4-hydroxyandrostenedione is also a weak prohormone to the anabolic steroid 4-hydroxytestosterone as an aromatase inhibitor, it also possesses notable testosterone stimulating properties. Whatever weak androgenic activity it may have is more than compensated for by its strong ability to lower estrogen levels. This action, of course, reduces the suppressive signal estrogen sends to your brain (estrogen is a main feedback signal to control the release of testosterone), increasing the testicular output of testosterone. In-vivo human studies show clearly that 4-hydroxyandrostenedione will suppress estrogen concentrations at levels that were not high enough to suppress gonadotropins13. Studies using 250mg to 500mg of 4-hydroxyandrostenedione injected every 2 weeks, or oral doses as high as 1000mg daily have failed to show any notable suppressive effect towards testosterone concentrations14. When the drug was given to men, including oral doses as high as 500mg (double the maximum recommended dose), we have seen measurable increases in serum testosterone concentrations 15 16 17. Due to the theoretical potential for androgenic feedback inhibition at high doses we do recommend, however, keeping within the recommended dosage range, and perhaps even limiting the dose to 2-3 caps per day, at times when increasing testosterone levels is a primary focus of use.



Figure 1. Mean testosterone increase in 6 normal men given 500mg of oral 4-hydroxyandrostenedione. Source: Comparison of the pharmacokinetics and pharmacodynamics of unformulated and formulated 4-hydroxyandrostenedione taken orally by healthy men. Cancer Chemother Pharmacol 1990;27(1):67-71


Post-Cycle Use
When used during the recovery window after a cycle of prohormones, or even steroids for that matter, Formastat can offer a very unique additional benefit. The main focus at this time is of course minimizing the post-cycle hypoandrogenic (low androgen) state, mainly by trying to restore the natural production of testosterone, which in many cases has been suppressed by the cycle of hormones. In most cases some type of anti-estrogen is incorporated into an athlete's recovery program, due to the effect they can have on testosterone release (discussed above). Because Formastat is also a prohormone to 4-hydroxytestosterone, however, it allows for some small level of continued supplementation of exogenous androgen during this window. Normally this would be considered a very bad idea, as androgens are usually suppressive towards testosterone release. But, with this product, its weak androgenic activity is compensated for by its estrogen suppressing action. So, it can essentially serve as a small bridge to full testosterone recovery.

DHT Inhibition
This compound has also demonstrated some ability to inhibit the 5-alpha reductase enzyme in certain in-vitro studies. This would seem to suggest it could offer some benefit by reducing androgenic activity in sensitive target tissues with high concentrations of 5-alpha reductase. At least one study in Scotland, however, suggests that this trait of 4-hydroxyandrostenedione is not strong enough to offer much of a physiological effect. Another makes note of both testosterone and DHT increases in some male patients taking the compound, not testosterone alone, which clearly does not support a strong DHT inhibiting role. Therefore, we do not have enough evidence to conclude that 4-hydroxyandrostenedione is a potent 5-alpha-reductase inhibiting compound. However, we will continue to investigate this possible activity.

A Naturally Occurring Hormone
4-hydroxylated androgens such as 4-hydroxyandrostenedione have been shown to be naturally occurring 22 and can be legally sold as nutritional supplements.






S FILES

Q: I have noticed that you seem to favor the use of Lentaron as an anti-aromatase. Why is this? The other gurus all recommend clomid or arimidex. Aren't these drugs as effective?

A: Although it would be more convenient if all the writers pulled in the same direction, it wouldn't be realistic. I'm not saying that anybody else is wrong, I'm simply telling you what I have found. It's a case of there being more than one route from A to B and we're telling you about our journeys with our own individual vehicles.

I personally like Lentaron (formestane or 4-hydroxyandrostene-3, 17-dione), but I accept that it is not as selective as Arimidex. However, this is quite irrelevant at the dosage I advocate (250 mg every two weeks), as impact on adrenal steroidogenesis is negligible.

Some bodybuilders claim to harden up as soon as they start on Lentaron, which is possibly the result of its powerful anti-aromatase and mild anabolic activity (it has been marketed in Italy as a weak anabolic). Or, it could be from its ability to cause a slight reduction in aldosterone.

Although the desk references refer to it as a painful injection, believe me, it's no different than some of the other products that you will have poked in your hide from time to time (suspension, stanazolol, etc.). I'll admit that some people have said they suffered flu-like symptoms the day after a shot, but I also get people complain about nausea or upset stomachs from using Arimidex.

At the end of the day, it's not rocket science. I also advocate Arimidex to people when it is hard to obtain Lentaron. The price is pretty much extortionate for both drugs, but it tips in favour of Arimidex. Whichever drug you choose, it's not a good idea to stay on either of them for too long because of the stress that they can place on the system.

The issue of Clomid vs. Nolvadex is a similar story, as there are positives and negatives on both sides. As an anti-estrogen, there's not really a lot of factors supporting the use of one over another, but Nolvadex seems to have less negative impact on the body (liver function) when used long-term. For this reason, when I choose an anti-estrogen for use during a course, I tend to favour Nolvadex. If I am looking to use one during short cycles or periods after or between cycles, I go with Clomid, as it appears to be slightly better at restoring normal gonadal function.

With older athletes, it is advisable to avoid long periods of anti-estrogen use, as there can be an adverse effect on serum lipids.

Recently, I've experimented with a topical preparation of formestane on people suffering from the early stages of gyno. The results look very promising. Basically, all I've done is dissolve around 10 grams of formestane in Nandrosol. Warming the solution will help it dissolve more easily. A better addition to Nandrosol, though, may be the prohormone of DHT (5-alpha-androstanediol), which is known to inhibit estrogen formation and is available from several chemical houses. This combination may well yield similar results to Andactrim, a transdermal DHT treatment for gyno.

[small_guy]

You need to make a transdermal as oral absorption sucks, and from what I understand it is no longer availabe OTC.

[Ritch]

Very interesting post. So it looks like 250mg 3 x`s a day would do the trick. Was thinking of using for a pct. I checked to see if they sell it on BB.com and it is sold as formadex and the capsules are 25mg and says to take 50-100mg daily. But you can take a bottle of vit.c that are 250mg and it will say take 1/day then see another bottle of 1000mg and could say to take 2/day. So conflicting advice concerning dosages is nothing out of the ordinary. It`s just that with estrogen you don`t want to take chances...

The last paragraph says he took 10 grams and dissolved in nandrosol. This may sound stupid but how does this work as a topical solution? He just put it in a bottle of nandrosol and sprayed it on himself like he would normaly? Would this work in a different spray bottle? Who the hell knows? Perhaps I will try to find where Brian Batchelor is these days and see what he thinks. Thanks again for that post.

[small_guy]

You can buy premade transdermal lotions from supp stores.

[Ritch]

Well that`s what I need to find because I was looking into the whole making it yourself method. I`m sure I would screw it up!

[Ritch]

I`ve spent the better part of this evening reading on formestane and the spray version seems to be the best route. It is well priced and everyone using it says it`s the most underated supp out there. It`s out of stock everywhere I checked as well. Something to surely use in the future.

[champcar99]

http://www.zsupps.com/bulkpowders.htm

[Ritch]

Their formestane sells for $35, that`s $20 more than at bulknutrition and the other places I saw, just incase anyone was to purchase some! I will look into the other bulk powders they have available. Thanks for the link.

[Ritch]

I saw zsupps have something called M1, 4ADdiol and couldn`t find it at bulk nutrition and just think these compounds (the pro steroids) as I`ve heard many times before are just not worth it. These compounds are just too new to actually know what the hell they will do to us in the long run. When they first come out the reviews are all good then we start to hear funny things about them. Delayed gyno... Or maybe I`m just tired of always having to keep up with these new compounds it just seems like you have to be a ****ing chemist to actually understand them.

At least with test (which has decades of bodybuilder experimentation) you know what will happen to acutally control side effects and so on. Sure I started a thread about formestane which is rather new and natural but not much newer than stuff like letro, arimidex and latest arival aromasin... Having no experience in neither, I think I would go with Formestane in spray or make the solution myself and it seems a blindfolded retartded chimpanze could do it (Mike Mentzer used to say this... RIP)

Just a thanks for the links given to me here. Being new to this website I wasen`t sure if I would even get any info on Fomestane, it being smaller than the other I posted (MD). So far I didn`t get any info there and in one day of going from link to link here, I pretty much found what I need to know. (Not claiming to be an expert or anything.) When it does become available somewhere, I will give it a run.