Mdv3100 (enzalutamide) - Superstrong Antiandrogen Topical

[SpaceInvader]

With just DMSO, it itches like hell, but I think it should be penetrating since it takes everything with it. Mixing just 2 mL PEG-400 with 4 mL DMSO reduces the itch significantly, but I went with pure DMSO to make sure it certainly goes in, incase PEG-400 is too thick.

Still, let's see out if distilled water is really needed.

 

[BlueLion]

I can't think of any reason this would be true. Minoxidil is done with just propylene glycol and alcohol and it penetrates just fine.

Inactive ingredients of Minoxidil are
(96 Vol.-%)Alcohol 30% , propylene glycol 50% and purified water 20%

 

[joshcrd]

Could anyone with some chemistry knowledge pitch in and say whether distilled water is actually needed? I haven't seen any info saying it helps other than Xandrus mentioning he used it.

-Size/weight of the drug molecule
-Solubility in water/alcohol
-Stability in the solution/suspension over time
-Potency of the drug
-Half-life

These are just some of the factors the compounding chemist would need consider when developing a vehicle for the delivery system.

I haven't looked into the properties of Enzalutamide (as a topical solution) but it may be because the drug most soluble in alcohol, followed by PG, then maybe slightly soluble in water. The chemist has decided on the ratio of ethanol/PG/water so as to maximise solubility but minimise irritation to the scalp. Too much alcohol and PG would do that.

It may also be to maximise dermal circulation and minimise systemic absorption.

 

[joshcrd]

The systemic issue is exactly why darolutamide is a much better option once it becomes cheaper. Shorter half life. If you haven't seen that thread, check it out:

spot on, topicals should have a short half life

 

[el_duterino]

Interesting thread guys

I looked into that MDV3100 few years ago hen it was still under testing but the very long half life will make this impossible long term, you wont be able to have much of a sex life and feel tired/brain fogged. I had these sides on Flutamide.

Quick update on my own case -started finasteride i 1998, then after 6 years on finasteride, plus 4 on dutasteride I switched to flutamide then RU ith dutasteride and finally RU alone since 2010

Also tried CB 2 years ago for 2 months but found the effect no different than RU, but at a much higher cost and bit harder to dissolve in Neogenic (Stemox) since this is my vehicle

I must say that the best combo I ever used is RU (or CB) + Stemox + minoxidil

None of these drugs will ever regrow lost hair.. if this is what people expect - it just wont work even at mega doses. In fact , as mentioned in this thread Even castration, which is more effective than any of these super anti androgen has been proven to not regrow lost hair and we know this since the 1940's

The key with RU is to store the powder properpy and mix a fresh dose it right before aplication - which tkes 20 seconds really. I suspect that the folks ho mentionned lck of success on it arent using it the right way.
You also would need to massage the topical quite hard and apply bit by bit as it dries fast -

RU is very cheap over time, I use 10mg a day or 15mg EOD, at night in Stemox and minoxidil foam in the morning. So my RU is only a few cents a day, Neo is the most expensive of the 3.

We don't need the 5% or higher dosages like in the studies because over time the continuous use of Ethanolic topical will make the scalp very porous

In fact I believe that a lower dosage works better over time because the body isn't going to over compensate by producing more AR with a lack of a systemic effect is not

Most of my loss is at the temples this is here topical anti androgen work better than finasteride/dutasteride.

Any topical with a serum half life longer than 1 hour is going to be impossible to stick to for long term maintenance.

 

[el_duterino]

We know that RU is not stable in a solution.

I don't think we ever saw an independent test proving the contrary - sure Kane may say otherwise as he has a vested interest in selling the product and people don't like to mix it themselve, but how can you test a solution anyway ?

I did the same thing you are doing when I started RU around 2008, a mix of a 10 days or so batch and found that it was not as effective as a fresh powder mix, especially towards the end.

15 mg is not a small amount at all..we use 1 mg of finasteride which is a lot less and diluted in the whole body not directly applied to the scalp.

It all depends on how porous the scalp is. Those older RU studies were done on people not using other alcohol based topicals

 

[el_duterino]

the 750 mg is for prostate cancer - a very high dosage because it is diluted in the blood and will end up in the whole body where only a very small amount will be available for the AR at the prostate .

I started with 400mg of RU, then went down to 200, then 100, 50 over the years. Eventually I noticed I got side effects at 40 mg even when I had none at 200mg at first - before I was using minoxidil and stemox - this is all due to the scalp being more porous which really varies on each person and is linked to using alcohol on the scalp over time.

15 mg is a lot provided most of it can cross the top skin layer and get to those AR - this may not be the case if the vehicle is not very good, if hair is too long, if it dries too fast before entering the scalp etc..

 

[el_duterino]

I looked into the issue of RU58841 stability further. Kane claims 6 month stability of his RU based on a "new more stable synthesis method".

Looked into that claim further and found this paper from 2014 that describes a "new" method of making RU58841 which is probably what he's referring to:

https://researchbank.rmit.edu.au/view/rmit:24419

So it's possible older synthesis methods of RU58841 were super unstable. But likely the more modern method described here is more than stable enough for even a month at a time.

this statement makes no sense at all
the molecule of RU is the same once its diluted - its RU molecules in ethanol


Sure the raw powder consistency may be different and could be more stable at room temperature - in my experience I kept RU in hot places/car trunks in summer etc.. for weeks on travel with no decrease in effectiveness

 

[whatevr]

My RU starts falling out of solution (even if refrigerated) into tiny crystals after a week or so. Standard 70/30 Ethanol 96% & Propylene Glycol mix. Bought from Group-Buys.

 

[ElTioLaBota]

Interesting thread guys

I looked into that MDV3100 few years ago hen it was still under testing but the very long half life will make this impossible long term, you wont be able to have much of a sex life and feel tired/brain fogged. I had these sides on Flutamide.

Quick update on my own case -started finasteride i 1998, then after 6 years on finasteride, plus 4 on dutasteride I switched to flutamide then RU ith dutasteride and finally RU alone since 2010

Also tried CB 2 years ago for 2 months but found the effect no different than RU, but at a much higher cost and bit harder to dissolve in Neogenic (Stemox) since this is my vehicle

I must say that the best combo I ever used is RU (or CB) + Stemox + minoxidil

None of these drugs will ever regrow lost hair.. if this is what people expect - it just wont work even at mega doses. In fact , as mentioned in this thread Even castration, which is more effective than any of these super anti androgen has been proven to not regrow lost hair and we know this since the 1940's

The key with RU is to store the powder properpy and mix a fresh dose it right before aplication - which tkes 20 seconds really. I suspect that the folks ho mentionned lck of success on it arent using it the right way.
You also would need to massage the topical quite hard and apply bit by bit as it dries fast -

RU is very cheap over time, I use 10mg a day or 15mg EOD, at night in Stemox and minoxidil foam in the morning. So my RU is only a few cents a day, Neo is the most expensive of the 3.

We don't need the 5% or higher dosages like in the studies because over time the continuous use of Ethanolic topical will make the scalp very porous

In fact I believe that a lower dosage works better over time because the body isn't going to over compensate by producing more AR with a lack of a systemic effect is not

Most of my loss is at the temples this is here topical anti androgen work better than finasteride/dutasteride.

Any topical with a serum half life longer than 1 hour is going to be impossible to stick to for long term maintenance.

Have you achieved to mantain your hair on ru during 7 years!?

 

[whatevr]

Castration is actually not more effective than enzalutamide orally. These drugs are made for treating castration-RESISTANT prostate cancer.

Side effects experienced by people so far do not seem to line up with what is expected theoretically so the drug may still prove to be useful (i.e. there is a surprising lack of side effects).

 

[el_duterino]

Castration is actually not more effective than enzalutamide orally. These drugs are made for treating castration-RESISTANT prostate cancer.

Side effects experienced by people so far do not seem to line up with what is expected theoretically so the drug may still prove to be useful (i.e. there is a surprising lack of side effects).

Maybe - but in practice actual castration is not used in prostate cancer due to its irreversible effect.
You are referring to a castration-like androgen deprivation treatment

Anyway - these new drugs may not have side effects for the first few weeks - but it will eventually build up in blood and you wont have much of a sex life - which again is not a priority when dying from prostate cancer

The best option over time is to tackle male pattern baldness from different angles at the same time by using Stemox, minoxidil and a low side effect topical anti androgen so that the body cannot compensate easily as its not aware that anything is out of the normal.

In 1 or 2 years Winlevi (CB for acne) will be available from drugstores as well

 

[whatevr]

If we could maintain on RU (much less CB which is supposed to be even weaker) then we wouldn't really have a need to explore these substances.

I failed on Propecia, RU just slows my hair loss down at best, so I don't really have a choice and my hair already looks like crap.

 

[Grasshüpfer]

I mix my ru weekly. Also group buys. Will keep an eye open and report back.

 

[sunchyme1]

@Grasshüpfer @whatevr

you boys buy your ru from groupbuys?

how much it cost you?

if you dont mind saying....

 

[ElTioLaBota]

If we could maintain on RU (much less CB which is supposed to be even weaker) then we wouldn't really have a need to explore these substances.

I failed on Propecia, RU just slows my hair loss down at best, so I don't really have a choice and my hair already looks like crap.

I mix my ru weekly. Also group buys. Will keep an eye open and report back.

Im a nw2, i might get gyno from finas so i'll quit, would i be able to maintain my hair by using 7,5% RU once daily until something better cames out?

 

[whatevr]

Im a nw2, i might get gyno from finas so i'll quit, would i be able to maintain my hair by using 7,5% RU once daily until something better cames out?

Depends on the mg, not the %. I can't maintain on 75 mg anymore.

 

[CinnamonRoll]

My RU starts falling out of solution (even if refrigerated) into tiny crystals after a week or so. Standard 70/30 Ethanol 96% & Propylene Glycol mix. Bought from Group-Buys.

Does this only happen to your high concentration 7.5% mix or even lower?
I was using 1/2 pg and 1/2 water and it was staying mixed for me, but only at 2.5%

I'm thinking about bumping it up to 5% next time, but it sounds like I may end up ruining it if I do.

 

[whatevr]

Does this only happen to your high concentration 7.5% mix or even lower?
I was using 1/2 pg and 1/2 water and it was staying mixed for me, but only at 2.5%

I'm thinking about bumping it up to 5% next time, but it sounds like I may end up ruining it if I do.

My mix is actually 2.5% and it happens regardless.

 

[whatevr]

@whatevr Started enzalutamide today. Wish me luck

Mix:
15% DMSO
70% PEG-400
15% Ethanol-96