Can Bicalutamide upregulate Androgen Receptors?

[Cooper]

I am writing this as a Post Accutane Syndrome victim. Studies showed that Accutane downregulates ARs on skin tissues and we suppose on other tissues as well due to most patients not responing to androgenic treatments. We know external androgen intake downregulates ARs further more.

So i was thinking doing the opposite, taking anti- androgens to fix my sexual health.

Anyone knows that can Bicalutamide upregulate the ARs without damaging my healthy ARs on my other tissues? (I guess my issue is located on my prostate.)

It is a non-steroidal AR antagonist, so i am rooting for this drug as a recovery option, if it works, then we can eliminate thousands of Accutane sufferers around the globe!

I need some help with this.

@haidut Anyone knows the science of this?

 

[Riesensackteil]

We know external androgen intake downregulates ARs further more.

And why? Strong Androgens might increase the expression of certain genes who produce more proteins in the Androgens likings

 

[Cooper]

And why? Strong Androgens might increase the expression of certain genes who produce more proteins in the Androgens likings

Well i know from many Post Finasteride cases that they recover with strong androgens. In PAS, it does not work. I don't think androgens can upregulate AR in the longterm, you take external stuff, so your receptors downregulate to create a balance.

Any more input would be helpful though, im eager to learn if Bicalutemide can upregulate ARs in theory, i will be the lab mice, i already though about suicide (I am hopeful and happy most of the time now.) many times before, so who cares anymore.

 

[Aries]

I can’t really help but I’m interested. Quick search on pubmed has hits for AR overexpression by prolonged bicalutamide therapy so in theory it could work.

According to wikipedia, bicalutamide crosses BBB and causes gyno, so it would be reasonable to assume that it upregulates the AR outside the prostate as well. Accutane also crosses BBB so it might be just fine.

What do you think about ulipristal acetate and mifepristone? Is bicalutamide more attractive for the selectivity of receptor?

About the theory, not that you are wrong but I’m quite baffled about the up- and downregulation of ARs by androgens as it doesn’t seem to happen outside PFS cases. People on TRT/roids don’t lose AR expression by prolonged exposure, even supraphysiological.

 

[Cooper]

I can’t really help but I’m interested. Quick search on pubmed has hits for AR overexpression by prolonged bicalutamide therapy so in theory it could work.

According to wikipedia, bicalutamide crosses BBB and causes gyno, so it would be reasonable to assume that it upregulates the AR outside the prostate as well. Accutane also crosses BBB so it might be just fine.

What do you think about ulipristal acetate and mifepristone? Is bicalutamide more attractive for the selectivity of receptor?

About the theory, not that you are wrong but I’m quite baffled about the up- and downregulation of ARs by androgens as it doesn’t seem to happen outside PFS cases. People on TRT/roids don’t lose AR expression by prolonged exposure, even supraphysiological.

Thank you for your interest and help Aries. I needed this. Having a hard time.

Well i actually ordered Mifepristone and waiting for it, i may try Bic. if Mifep. fails. It failed for 2 other PAS cases in our group right now.

Can you please share the study about Bicalutamide and AR overexpression? Was it this one?

Prolonged treatment with bicalutamide induces androgen receptor overexpression and androgen hypersensitivity - PubMed

Bicalutamide-resistant LNCaP-BC2 exhibited AR overexpression and hypersensitivity to low levels of androgen. Our data suggests that AR overexpression is a significant mechanism of bicalutamide resistance similar to resistance from chronic androgen depletion. In addition, pAR(210) overexpression...

pubmed.ncbi.nlm.nih.gov

This is done on prostate cancer cells. So im not sure about the credibility.

And yeah i am thinking to use Bic. with Tamoxifen to avoid Gynecomastia.

Early Data: Tamoxifen May Reduce Symptoms of Bicalutamide... : Oncology Times

An abstract is unavailable.

journals.lww.com

The dosage seems too low for me though i have used 20mg every other day in the past before. I can do that again to avoid any breast issues.

So do you think Bicalutamide can really be my best shot? I haven't researched it that much for now.


About the other route, well im not sure if Supra. doses of androgens really safe to use... I have read and heard stories. "Deca d*ck" cases for example.

 

[Cooper]

@Aries Any comments mate?

 

[Aries]

I am a bit busy for the time being but I’ll definitely share if I find anything interesting about AR regulation.

That’s the study and you're right that results from cancer research aren't necessarily directly applicable to normal cells. We do know about epigenetic changes on AR in non-cancerous cells in other circumstances though. Androgen receptor expression has been shown to change on cells without cancer (Accutane) and there is also research about the CAG repeat length affecting androgen receptor effectivity etc. I don't think it's unreasonable to expect the AR expression changes of bicalutamide to be applicable on non-cancerous cells as well but from this data it's of course not explicitly certain.

I think deca **** is usually caused by excess estrogen from combining nandrolone with test or other aromatasable steroids. Nandrolone alone seems to avoid the issue, combining with test causes the excess estrogenicity perhaps by nandrolone competing with test on AR, leaving less androgenic signaling on the cells by weaker androgen (nandrolone) while plenty of unbound test is available for aromatasation. Or the progestinic activity of deca primes estrogen receptors. 19-nors can be tricky sometimes.

There is still a lot of people on steroid forums who have blasted supraphysiological levels of various steroids for years yet their AR (nervous system, sexuality etc.) is responsive to the levels of the hormones like before. I don't think supraphysiological androgens alone can cause AR downregulation.

 

[Cooper]

I am a bit busy for the time being but I’ll definitely share if I find anything interesting about AR regulation.

That’s the study and you're right that results from cancer research aren't necessarily directly applicable to normal cells. We do know about epigenetic changes on AR in non-cancerous cells in other circumstances though. Androgen receptor expression has been shown to change on cells without cancer (Accutane) and there is also research about the CAG repeat length affecting androgen receptor effectivity etc. I don't think it's unreasonable to expect the AR expression changes of bicalutamide to be applicable on non-cancerous cells as well but from this data it's of course not explicitly certain.

I think deca **** is usually caused by excess estrogen from combining nandrolone with test or other aromatasable steroids. Nandrolone alone seems to avoid the issue, combining with test causes the excess estrogenicity perhaps by nandrolone competing with test on AR, leaving less androgenic signaling on the cells by weaker androgen (nandrolone) while plenty of unbound test is available for aromatasation. Or the progestinic activity of deca primes estrogen receptors. 19-nors can be tricky sometimes.

There is still a lot of people on steroid forums who have blasted supraphysiological levels of various steroids for years yet their AR (nervous system, sexuality etc.) is responsive to the levels of the hormones like before. I don't think supraphysiological androgens alone can cause AR downregulation.

Thanks. Well i just ordered Test P.

Im going try and see if Testosterone can upregulate my ARs or not. Science really lacks evidence so i wanted to test a safer protocol before jumping into Bicalutamide.

Im gonna inject 150mg of SubQ Test P a week, divided into 3x- 50mg doses. With 250iu 3xW HCG.

I want to increase my TT up to 1200. And monitor any changes on my prostate and sexual function.

If this fails, i will try Mifepristone and then Bicalutamide.

https://pubmed.ncbi.nlm.nih.gov/25130462/

Any takes on this study? They didn't mention what tissues were collected for AR changes... Such a weird study but it says that it increased AR expression?

 

[Cooper]

Can anyone else help me out please? Any medical students or Dr's here? I need to be sure that Bicalutamide can upregulate my ARs before i take it. Thanks.

 

[Cooper]

Can someone who studies medicine or something chime in and help me out?

Thanks.

 

[Cooper]

Bump. Anyone can help me out if this can fix my issues? I just want to upregulate the AR on my prostate with Bicalutamide if it does that. And i am scared of my other ARs getting affected too. Let's hope they fix themselves after i quit Bicalutamide with the root cause of my issue..

 

[aliml]

Bicalutamide increases activity AR and decreases reaction AR.

SelfDecode | Genome Analysis

Use SelfDecode to get personalized health recommendations based on your genes. Get started today with an existing DNA file or order a SelfDecode DNA kit!

selfdecode.com

Mifepristone decreases activity AR and affects binding AR.

SelfDecode | Genome Analysis

Use SelfDecode to get personalized health recommendations based on your genes. Get started today with an existing DNA file or order a SelfDecode DNA kit!

selfdecode.com

 

[Cooper]

Bicalutamide increases activity AR and decreases reaction AR.

SelfDecode | Genome Analysis

Use SelfDecode to get personalized health recommendations based on your genes. Get started today with an existing DNA file or order a SelfDecode DNA kit!

selfdecode.com

Mifepristone decreases activity AR and affects binding AR.

SelfDecode | Genome Analysis

Use SelfDecode to get personalized health recommendations based on your genes. Get started today with an existing DNA file or order a SelfDecode DNA kit!

selfdecode.com

God damn! Why i didn't know about this site before.

So, let me get it straight, what is ''reaction'' of AR. All i need is to increase the expression of that gene. So ''activity'' is what i need to increase i guess?

Dank, bad that it decreases IGF-1 expression. Would that expression correct itself after i quit the drug or is it a permanent change?

Thanks!

Btw, i completed a cycle of Testosterone Cyp. for 7 weeks. 200mg a week and on PCT, i must say my sexual symptoms worsened and i believe Test caused more downregulation on my AR. So this kinda prooves it for me that Post Accutane Syndrome can be cured by AR upregulation. Other cases experience similar outcomes as me too.

 

[aliml]

God damn! Why i didn't know about this site before.

So, let me get it straight, what is ''reaction'' of AR. All i need is to increase the expression of that gene. So ''activity'' is what i need to increase i guess?

Dank, bad that it decreases IGF-1 expression. Would that expression correct itself after i quit the drug or is it a permanent change?

Thanks!

Substances That Increase AR:​

Selfdecode

Use SelfDecode to get personalized health recommendations based on your genes. Get started today with an existing DNA file or order a SelfDecode DNA kit!

selfdecode.com

 

[Cooper]

Substances That Increase AR:​

Selfdecode

Use SelfDecode to get personalized health recommendations based on your genes. Get started today with an existing DNA file or order a SelfDecode DNA kit!

selfdecode.com

Good to know. I just need to increase the expression of it, so i assume the ''activity'' of it.

Strange though, aren't we all know that taking external androgens like Testosterone would cause DOWNregulation of AR instead of upregulation? That's how body responds to high levels of androgens in blood, it lowers the ARs to not disturb the body on a more serious manner... So it ''balances'' it out.

In that link it shows T as a AR expression ''increaser''.

Hmm...

 

[methylenewhite]

Just use l-carnitine, injectable is even better. Proven to upregulate AR.

 

[Cooper]

Just use l-carnitine, injectable is even better. Proven to upregulate AR.

I did, it is not working i tried high doses and injecting L- Carnitine... Nah, it has to be veins. I can't do daily intravenious injections to myself at home.

 

[methylenewhite]

What dosages did you use?

 

[Cooper]

What dosages did you use?

5grs usually. My issue is pharma grade hardcore sh*t i suppose. A normal supplement won't fix me you know.

 

[methylenewhite]

Bicalutamide just doesn't sound right at all IMO