Folexen: New Hair Loss Treatment based on S-Equol

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Folexen

Guest
Hi guys,

First off I'd like to say that I work for a company that manufactures a nutraceutical formulation containing S-equol. The company is called Eclipse Nutraceuticals and the product is called Folexen. For those who are interested I will outline details of the product, the science behind S-equol, as well as it’s relevance for the treatment of androgenic alopecia.

The currently accepted wisdom is that the cause of male pattern baldness is a genetic trait in some men that causes scalp follicles to miniaturise when exposed to the hormone DHT (dihydrotestosterone). DHT is produced when an enzyme called 5AR (5-alpha-reductase) acts upon testosterone and adds an electron to it. This chemical change results in DHT having different physiological effects upon the human body when compared to its parent testosterone.

If I could speculate, I’d say that the root cause of male pattern baldness was a genetic expression that causes some of us to have 5AR active INSIDE our follicles, but dependant on location. That’d also explain why male pattern baldness happens in a certain pattern and not in a universal loss of hair. There is some indirect supportive evidence for this theory. [3][5]

Serum DHT is not the issue since it is bound to ABP (Androgen-Binding Protein) and becomes less lipophilic and hence less able to cross the cell membrane into the follicle.

Dutasteride and Finasteride work by inhibiting the action of 5AR so that its ability to convert T to DHT is hampered. These compounds work through a process of irreversible inhibition of the enzyme - they have the ability to modify the active region on the surface of 5AR, so the testosterone cannot use the enzyme. Thus the conversion becomes energetically unfavourable and less likely to occur. To be more precise, there are two types of 5AR. Finasteride targets type 2 while Dutasteride can inhibit type 1 in addition to type 2.

For some men this will be enough to halt hair loss or even regrow hair over time. There are some side effects to inhibiting 5AR because the testosterone that isn’t being converted to DHT can trigger other hormonal responses in the body, as part of the natural hormonal feedback loop that we all have. Some men report lack of libido, erectile dysfunction or other side effects due to the increase in female hormones that are produced to counteract the higher levels of testosterone.

Enzymatic inhibitors have a drawback in that, for some men, the recommended dosage might not be sufficient to deactivate all the 5AR without causing other problems. In other words everyone probably has a dosage level at which the medication will work, but for some people there are too many concomitant side effects for the treatment to be safe. Merck have shown that normal dose Propecia resulted in improvement for 77% of patients [4]. Presumably a different treatment is required for the remaining men.

This is where S-equol can step up to the plate. It has a mode of action that is very different to the 5AR inhibitors. Instead of preventing the production of DHT, it binds strongly to the DHT molecules. When DHT has S-equol attached to it, it is no longer a form of 'free DHT', i.e. it cannot cause male pattern baldness because the molecule is no longer able to bind to receptor sites.

The ability of S-equol to bind to DHT is very strong [1][2], which is good news for us. Theoretically there are sufficient levels of S-equol in serum, all the DHT can be mopped-up before it can cause damage, even the DHT that is inside hair follicles. S-equol is a small molecule, not a protein, so it has no problem crossing cell membranes.

S-equol is formed in some individuals after consuming soy products. Scientists have been able to prove that various bacteria have the ability to transform a soy isoflavone (daidzein) into S-equol. It is theorised that people who are able to produce S-equol have an intestinal environment that supports the species of bacteria that allow this transformation to take place.

If 5AR blockers are working for you then I am not going to recommend cessation of treatment. But anyone who is still looking for a solution might want to consider this product (visit http://folexen.com).

Please let me know if you have any questions and I'll do my best to answer them for you!

Take care,
Andrew


[1]: http://www.biolreprod.org/content/70/4/1188.full
[2]: http://www.ncbi.nlm.nih.gov/pubmed/21232127
[3]: http://www.ncbi.nlm.nih.gov/pubmed/9068725
[4]: http://www.propecia.com/finasteride/propecia/consumer/index.jsp
[5]: http://www.ncbi.nlm.nih.gov/pubmed/8287580
 
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How could it work without side effects, if it doesn't allow DHT to bind to any receptor? If DHT couldn't bind where it's needed, then it's pretty much useless and will cause the same side effects that are caused by the lack of DHT, no?

we dont know if sides are caused by lack of DHT...
 
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Folexen

Guest
seriously guys this is pretty much the cure with no side effects... ALL ATTENTION TO EQUOL!

The only problem with this stuff is its price... why so expensive after so many years?

Hi 2020. I agree that it should be cheaper. However at the moment the commercial reality is that there are a lot of fixed costs involved in it's production. For example, machinery and lab test equipment.

Hopefully there will be a point in the future where we can churn it out at $10 a bottle.. but those economies of scale are a way off yet. I daresay the big pharmas could produce it very cheaply but it would compete against their existing offerings and so they'd view it as counterproductive.

Our evaluations have shown 10mg to be a fairly effective dose. 100mg would probably be even more effective (safety testing in Japan showed doses up to 320mg are OK) but then a one month supply would cost $400 which isn't affordable currently, but might be one day?
 

Finner

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Hi Andrew,

Your solution begs the question that if it binds to DHT such that the DHT can not bind to receptor sites then how do you know that it is side effect free? Have you done any trials? Could your product bind to all DHT because this would suppress even more than Finasteride (and is thus potentially more risky)?

Any response greatly appreciated,

Finner
 
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Folexen

Guest
How could it work without side effects, if it doesn't allow DHT to bind to any receptor? If DHT couldn't bind where it's needed, then it's pretty much useless and will cause the same side effects that are caused by the lack of DHT, no?

Hi TravisB. Good question, it's all down to how complicated and counterintuitive the endocrine system is!

DHT is a more powerful androgen than T, but it acts on different areas to its parent hormone. Receptors mainly reside in places like hair follicles and the prostate. That's why some of the 5AR inihibitors are also good for preventing prostate enlargement.

However.. preventing production of DHT is sometimes bad news because it's one of the pathways that the body uses to rid itself of excess T. When that extra T has nowhere to go, some of it gets turned into estradiol instead. The ultimate irony in this feedback loop is that being 'too much man' can lead to feminisation.

If we allow DHT to be created but then block it's action, the potential for side effects is reduced.
 
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Hi Andrew,

Your solution begs the question that if it binds to DHT such that the DHT can not bind to receptor sites then how do you know that it is side effect free? Have you done any trials? Could your product bind to all DHT because this would suppress even more than Finasteride (and is thus potentially more risky)?

Any response greatly appreciated,

Finner

there's a difference...

5alpha-reductase inhibitors prevents DHT from being synthetisised, thus affecting at least one other hormone (testosterone).....

equol binds to DHT molecules and inactivates them, thus preventing DHT from performing it's physiological roles in the body when it binds to ARs in different tissues.. personally I don't know if this will mean levels of other hormones will increase or decrease or stay the same.....there are a few studies though linked in the first post
 

2020

Experienced Member
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Hi 2020. I agree that it should be cheaper. However at the moment the commercial reality is that there are a lot of fixed costs involved in it's production. For example, machinery and lab test equipment.

Hopefully there will be a point in the future where we can churn it out at $10 a bottle.. but those economies of scale are a way off yet. I daresay the big pharmas could produce it very cheaply but it would compete against their existing offerings and so they'd view it as counterproductive.

Our evaluations have shown 10mg to be a fairly effective dose. 100mg would probably be even more effective (safety testing in Japan showed doses up to 320mg are OK) but then a one month supply would cost $400 which isn't affordable currently, but might be one day?

right... which is why I've complained about it being so expensive. One bottle isn't that expensive but it only contains a one month supply if you were to use 8mg/day which is waaay too litle. It needs to be close to 100mg if not more.

That one study you guys did showed ~2.5% improvement with 4mg/day so it obviously does something but just imagine if these people were using 40mg/day or 100mg/day! Goodbye finasteride and dutasteride. There is so much potential here!!

You don't have to convince us that it works. WE KNOW IT WORKS. Here is just one data graph:



obviously it's pretty effective.

The only problem is cost!

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Hi Andrew,

Your solution begs the question that if it binds to DHT such that the DHT can not bind to receptor sites then how do you know that it is side effect free? Have you done any trials? Could your product bind to all DHT because this would suppress even more than Finasteride (and is thus potentially more risky)?

Any response greatly appreciated,

Finner

because a billion asian people are walking with equol in their system and I don't think any of them are suffering side effects from it.... there are studies done with > 300mg/daily doses and it didn't pose any side effects even though that much equol is probably comparable to dutasteride
 

2020

Experienced Member
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Additionally, from pilot data, serum 5α-DHT levels significantly decreased by 10 to 15% in men (50 to 60 years of age) and 20 to 26% in postmenopausal women (60 to 65 years of age) when an equol oral dose of 3 mg per day was administered (without side effects), suggesting that equol effectively binds and/or alters 5α-DHT levels.

it takes only 3mg to reduce your DHT by 10-15%
 

2020

Experienced Member
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So if I understand correctly this is prevention not a cure. You will have minor regrowth at best since DHT is only part of the problem.

what do you mean part of the problem? DHT interaction with hair follicles IS THE ONLY PROBLEM. Whatever happens after is irrelevant since it wouldn't have happened if DHT wasn't there.

Depending on the dosage, it will have the same results as finasteride/dutasteride with zero side effects and the DHT blocking effect lasts forever unlike finasteride/dutasteride.
If you were to stop using equol after 5 years, you would start losing hair at a normal speed instead of massive sheds and norwood losses with finasteride/dutasteride. Gains are permanent.

As far as I know, minor regrowth is pretty much what the current treatments can do except that equol may do it better and with no side effects
 

2020

Experienced Member
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If you check out http://www.ajcn.org/content/90/4/1029.full.pdf, they administered a bolus of 20mg S-equol and it reached 350 ng/mL in plasma which works out to 1445 nM. So 10mg per day would compare favourably to the in vitro study that you've posted.

some of your math must have went wrong... 1445 nM? That's off the charts. Are those moles?

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Hi zeroes. Some people see only a cessation of shedding, others see regrowth and a few see continued shedding. Maybe regrowth can be encouraged by using other therapies but you are correct in stating that this treatment only aims to counteract DHT.

yeah the results from finasteride/dutasteride studies shouldn't apply to equol since equol wouldn't cause hyperandrogenicity overtime. 100% of people should respond to equol and with luck, maybe get some regrowth, but mostly just maintenance which is good enough since finasteride/dutasteride can't do better than that.
70% reduction of DHT with finasteride is not the same as 70% reduction of DHT with equol...
 
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Folexen

Guest
The molar mass of equol is 242.27 g/mol, so 350 ng/mL is 1.445 nM/mL = 1445 nM/L. A 10mg dose would yield about half that. It might seem off the charts, but we're comparing in vivo to in vitro, so it's not a direct apples/apples comparison (e.g. equol is removed from the blood by the kidneys). The in vitro results are still positive though.
 

Aks20

Established Member
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No DHT binding = side effects!

Dear Folexen, this is a very interesting product, which many of us would love to use if it is truly side effect free, but please provide some more information.

I fail to see how taking DHT out of the equation will lead to less side effects? Granted, Propecia is far more dangerous in that 5Alpha R reduction means that 5 AlphaRs which are used all over the place are also out of the equation..

But DHT itself is critical to male sexual function, and is also linked to stuff like bone density in males. Less DHT = less sexual function and osteoporesis.

Have there been tests conducted on S-equol re: safety and what were the results?

Also, please provide some evidence/more information that DHT blocking by itself is not dangerous.

Thanks,
Aks
 

2020

Experienced Member
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The molar mass of equol is 242.27 g/mol, so 350 ng/mL is 1.445 nM/mL = 1445 nM/L. A 10mg dose would yield about half that. It might seem off the charts, but we're comparing in vivo to in vitro, so it's not a direct apples/apples comparison (e.g. equol is removed from the blood by the kidneys). The in vitro results are still positive though.

ok got it
 
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