List Of Strongest To Weakest Antiandrogens

[itchymadscalp]

WHy did you not include the part where it says that the drug builds up to concentrations thousands above both testosterone and dht?

For that you need high dose ... something like 50mg and sometimes more. And some trans took 300mg with no success.
https://www.reddit.com/r/TransDIY/c..._way_to_actually_measure_progress_on/e4zoz6y/
https://www.reddit.com/r/MtFHRT/comments/9i0yh2/bicalutamide_casodex_as_an_antiandrogen_for/

"A rough estimate for the blocking ability of 50 mg/day bicalutamide would be: 50 mg x 4 ng/dl T = 200 ng/dl of (post bicalutamide) T. Where each 1 mg bicalutamide is calculated to block 4 ng/dl of T."

And again you cannot know if its safe in a long term use for people who just want to keep their hair, especially if 50 or 100 or more are needed to be effective (liver issues for example).

Bicalutamide + Estradiol ... why not, but still not safe for healthy people. Bicalutamide alone ... no really a good alternative to finasteride. And even if it works we are not sure it's safe to mess up with androgen receptors. So we should be cautious when we are promoting some drugs. That's all.

"Gooren (2009) and Randolph (2018) recommend a dosage of bicalutamide of 50 mg/day in combination with testosterone suppression (via, e.g., estrogen therapy) in adult transgender women, while Fishman et al. (2019) recommend a dosage of 25 to 50 mg/day for this purpose. Neyman et al. (2017) used a dosage of bicalutamide of 50 mg/day as a monotherapy puberty blocker in adolescent transgender girls. However, although this was clinically effective in producing the desired effects (including promotion of feminization and breast development and apparently preventing or reducing masculinization), the dosage of bicalutamide in the Neyman study was very likely much too low to be fully effective for such purposes"

"Taken together, I would guess that doses of bicalutamide of 6.25 to 50 mg/day may be appropriate for use in the context of substantial suppression of testosterone levels (<200 ng/dL), whereas higher doses of 150 to 300 mg/day may be appropriate for use as a monotherapy (i.e., without an estrogen or other antigonadotropin, for instance to block puberty). Note that, due to increased estradiol levels, considerable to full feminization will likely occur with bicalutamide monotherapy (at sufficiently high doses such that testosterone is adequately blocked). Hence, there isn't really a good reason to actually use bicalutamide monotherapy. It's best to just combine it with at least some amount of estrogen, which will suppress testosterone levels and greatly reduce the required bicalutamide dosage (and cost)."

Haha thanks!

BTW, thanks to itchymadsclap, when I was reading AR page of wiki, I came across this. https://en.m.wikipedia.org/wiki/Dimethylcurcumin. It is interesting that it's been investigated for male pattern baldness.
That’s a SARD : selective androgen receptor degrader, very heavy on the sides.

Yeah I wanted to try this some years ago and impossible to buy it. But it still not something I would recommend even if it had worked for me. Because it might not* be safe to use.

 

[DHTcel]

For that you need high dose ... something like 50mg and sometimes more. And some trans took 300mg with no success.
https://www.reddit.com/r/TransDIY/c..._way_to_actually_measure_progress_on/e4zoz6y/
https://www.reddit.com/r/MtFHRT/comments/9i0yh2/bicalutamide_casodex_as_an_antiandrogen_for/

"A rough estimate for the blocking ability of 50 mg/day bicalutamide would be: 50 mg x 4 ng/dl T = 200 ng/dl of (post bicalutamide) T. Where each 1 mg bicalutamide is calculated to block 4 ng/dl of T."

And again you cannot know if its safe in a long term use for people who just want to keep their hair, especially if 50 or 100 or more are needed to be effective (liver issues for example).

Bicalutamide + Estradiol ... why not, but still not safe for healthy people. Bicalutamide alone ... no really a good alternative to finasteride. And even if it works we are not sure it's safe to mess up with androgen receptors. So we should be cautious when we are promoting some drugs. That's all.

"Gooren (2009) and Randolph (2018) recommend a dosage of bicalutamide of 50 mg/day in combination with testosterone suppression (via, e.g., estrogen therapy) in adult transgender women, while Fishman et al. (2019) recommend a dosage of 25 to 50 mg/day for this purpose. Neyman et al. (2017) used a dosage of bicalutamide of 50 mg/day as a monotherapy puberty blocker in adolescent transgender girls. However, although this was clinically effective in producing the desired effects (including promotion of feminization and breast development and apparently preventing or reducing masculinization), the dosage of bicalutamide in the Neyman study was very likely much too low to be fully effective for such purposes"

"Taken together, I would guess that doses of bicalutamide of 6.25 to 50 mg/day may be appropriate for use in the context of substantial suppression of testosterone levels (<200 ng/dL), whereas higher doses of 150 to 300 mg/day may be appropriate for use as a monotherapy (i.e., without an estrogen or other antigonadotropin, for instance to block puberty). Note that, due to increased estradiol levels, considerable to full feminization will likely occur with bicalutamide monotherapy (at sufficiently high doses such that testosterone is adequately blocked). Hence, there isn't really a good reason to actually use bicalutamide monotherapy. It's best to just combine it with at least some amount of estrogen, which will suppress testosterone levels and greatly reduce the required bicalutamide dosage (and cost)."





Yeah I wanted to try this some years ago and impossible to buy it. But it still not something I would recommend even if it had worked for me. Because it might not* be safe to use.

OK that is not true, the 1mgx4ng= testosterone is completely wrong and has no scientific backing.

1mg of bicalutamide ACTUALLY blocks 10ng/dl of testosterone and dht from binding to the androgen receptor see here: "Although the affinity of bicalutamide for the AR is approximately 30 to 100 times lower than that of DHT (IC50 ≈ 3.8 nM),[37][13][1][38] the main endogenous ligand of the receptor in the prostate gland, sufficiently high relative concentrations of bicalutamide (1,000- to 10,000-fold excess) are able to completely prevent activation of the AR by androgens like DHT and testosterone and subsequent upregulation of the transcription of androgen-responsive genes and associated effects.[39][20][40][41] At steady-state, relative to the normal adult male range for testosterone levels (300–1,000 ng/dL),[42] circulating concentrations of bicalutamide at 50 mg/day are roughly 600 to 2,500 times higher and at 150 mg/day around 1,500 to 8,000 times higher than circulating testosterone levels"

there only needs to be a reach of 1000 fold excess of bicalutamide metabolites to prevent activation of the AR, with 150mg bicalutamide, this is achieved for 1500ng/dl of testosterone or less, 100mg bicalutamide works for 1000ng/dl of testosterone or less and 50mg bicalutamide works for 500ng/dl of testosterone or less

good luck trying to get bicalutamide prescribed, I already said 4 to 5 times that I have called multiple trans doctors and they told me the drug is NOT able to be prescribed for hrt because it doesn't reduce androgen levels, it isn't an antigonaditropen, it isn't a SAA, its actually an NSAA, it has antiprogestinic effects, it doesn't reduce muscle mass, it doesn't reduce bone mass, or redistribute body fat, and you continue to keep posting random quotes backing your claims with no studies to support.

 

[itchymadscalp]

OK that is not true, the 1mgx4ng= testosterone is completely wrong and has no scientific backing.

1mg of bicalutamide ACTUALLY blocks 10ng/dl of testosterone and dht from binding to the androgen receptor see here: "Although the affinity of bicalutamide for the AR is approximately 30 to 100 times lower than that of DHT (IC50 ≈ 3.8 nM),[37][13][1][38] the main endogenous ligand of the receptor in the prostate gland, sufficiently high relative concentrations of bicalutamide (1,000- to 10,000-fold excess) are able to completely prevent activation of the AR by androgens like DHT and testosterone and subsequent upregulation of the transcription of androgen-responsive genes and associated effects.[39][20][40][41] At steady-state, relative to the normal adult male range for testosterone levels (300–1,000 ng/dL),[42] circulating concentrations of bicalutamide at 50 mg/day are roughly 600 to 2,500 times higher and at 150 mg/day around 1,500 to 8,000 times higher than circulating testosterone levels"

there only needs to be a reach of 1000 fold excess of bicalutamide metabolites to prevent activation of the AR, with 150mg bicalutamide, this is achieved for 1500ng/dl of testosterone or less, 100mg bicalutamide works for 1000ng/dl of testosterone or less and 50mg bicalutamide works for 500ng/dl of testosterone or less

please don't pass around false information

I still think you're wrong.
But you see maybe with all your posts promoting Bicalutamide some guys will be willing to try and maybe we will see a lot of good reviews thanks to Bicalutamide. And maybe those guys who will take Bicalutamide for years and it will work wonders with no bad side effects and everyone will be happy with that.
Or ... It will do the opposite and be dangerous. But who cares ? ...
I think you shouldn't pretend Bicalutamide is safe and effective, because you just don't know and you're not a doctor. I'm not a doctor either, that's why I say we should remain cautious, and if we want to try it's at our own risks ... and that what I did ... I tried and it was a big fail. Even Lupron + high dose Estradiol is a fail. I'm not promoting it, even if I think it's safer (Lupron) than Bica.

 

[itchymadscalp]

You can dislike my posts like a kid, I will give you twice as much dislikes. Keep going.

 

[DHTcel]

You can dislike my posts like a kid, I will give you twice as much dislikes. Keep going.

I stopped, are you going to continue?

 

[DHTcel]

You can dislike my posts like a kid, I will give you twice as much dislikes. Keep going.

stop disliking my posts

 

[itchymadscalp]

I stopped, are you going to continue?

When you give me 1 I give you 2 dislikes, sometimes 3.

 

[Ikarus]

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2981508/

https://en.wikipedia.org/wiki/Bicalutamide#cite_note-pmid19359544-155

"Bicalutamide has relatively low affinity for AR (at least 30-fold reduced relative to the natural ligand dihydrotestosterone (DHT))"

So Bicalutamide is pretty weak when used alone and if testosterone is not lowered enough. I really don't think it's a good alternative to Finasteride, because it increase testosterone and thus DHT and it cannot compete well with DHT. It's just a fact.
But if you use it alongside with an another AA like Cyproterone or Estradiol (you need high levels) so of course it will help, by a lot. The main issue is that it will make you at best dependant to it in a long term use, and sometimes (but pretty rare) can make your androgen receptors really sensitive. That's why some trans experience remasculinisation when they stop Bicalutamide (and in some extent CPA) after an orchiectomy.


It's not something we can recommend blindly to everyone as an alternative to Finateride/Dutasteride/Spironolactone/Cyproterone ... except if you're willing to use Estradiol with it, that way it will obliterate your testosterone and make the few of it inactive.

I agree. If I can recall correctly, Ein had to use finasteride in combination with bicalutamide to see the results he wanted. It's not a great medication when used alone for hair loss, neither is spironolactone and cyproterone acetate. In all honesty, none of these hair medications are great when used alone. 5AR inhibitors lose effectiveness, cyproterone acetate can't lead to regrowth and poses such significant risks with long-term use, spironolactone is a diuretic with its anti-androgenic effects being indirect and greatly weak, bicalutamide has issues with DHT. Bicalutamide, to have great success, can't be used alone. Individually, I originally used spironolactone and estradiol for months prior so my starting point in hormone levels were efficacious. Likewise, Ein originally used spironolactone and finasteride for months prior. Although Maave used bicalutamide alone, if I remember correctly, and experienced great results.

In my opinion, it can be used as an alternative to spironolactone and cyproterone acetate since they are both harsh on our bodies. Spironolactone should not be used in general, and cyproterone acetate can lead to meningiomas, prolactinoma and great hepatic issues. Although bicalutamide raises T, that can be managed when it's in combination with E. And becoming dependant on it is the same as 5AR inhibitors and minoxidil; all hair loss medications require dependance to maintain results. Although, finasteride also causes a raise in testosterone...

 

[itchymadscalp]

I agree. If I can recall correctly, Ein had to use finasteride in combination with bicalutamide to see the results he wanted. It's not a great medication when used alone for hair loss, neither is spironolactone and cyproterone acetate. In all honesty, none of these hair medications are great when used alone. 5AR inhibitors lose effectiveness, cyproterone acetate can't lead to regrowth and poses such significant risks with long-term use, spironolactone is a diuretic with its anti-androgenic effects being indirect and greatly weak, bicalutamide has issues with DHT. Bicalutamide, to have great success, can't be used alone. Individually, I originally used spironolactone and estradiol for months prior so my starting point in hormone levels were efficacious. Likewise, Ein originally used spironolactone and finasteride for months prior. Although Maave used bicalutamide alone, if I remember correctly, and experienced great results.

In my opinion, it can be used as an alternative to spironolactone and cyproterone acetate since they are both harsh on our bodies. Spironolactone should not be used in general, and cyproterone acetate can lead to meningiomas, prolactinoma and great hepatic issues. Although bicalutamide raises T, that can be managed when it's in combination with E. And becoming dependant on it is the same as 5AR inhibitors and minoxidil; all hair loss medications require dependance to maintain results. Although, finasteride also causes a raise in testosterone...

Yeah and Spironolactone and Cyproterone used alone are a lot worse maybe ... because no testosterone and nothing to compensate can be pretty bad for the health (like @Sonolmn98 explained).
Well I agree with you

 

[Ikarus]

For that you need high dose ... something like 50mg and sometimes more. And some trans took 300mg with no success.
https://www.reddit.com/r/TransDIY/c..._way_to_actually_measure_progress_on/e4zoz6y/
https://www.reddit.com/r/MtFHRT/comments/9i0yh2/bicalutamide_casodex_as_an_antiandrogen_for/

"A rough estimate for the blocking ability of 50 mg/day bicalutamide would be: 50 mg x 4 ng/dl T = 200 ng/dl of (post bicalutamide) T. Where each 1 mg bicalutamide is calculated to block 4 ng/dl of T."

And again you cannot know if its safe in a long term use for people who just want to keep their hair, especially if 50 or 100 or more are needed to be effective (liver issues for example).

Bicalutamide + Estradiol ... why not, but still not safe for healthy people. Bicalutamide alone ... no really a good alternative to finasteride. And even if it works we are not sure it's safe to mess up with androgen receptors. So we should be cautious when we are promoting some drugs. That's all.

"Gooren (2009) and Randolph (2018) recommend a dosage of bicalutamide of 50 mg/day in combination with testosterone suppression (via, e.g., estrogen therapy) in adult transgender women, while Fishman et al. (2019) recommend a dosage of 25 to 50 mg/day for this purpose. Neyman et al. (2017) used a dosage of bicalutamide of 50 mg/day as a monotherapy puberty blocker in adolescent transgender girls. However, although this was clinically effective in producing the desired effects (including promotion of feminization and breast development and apparently preventing or reducing masculinization), the dosage of bicalutamide in the Neyman study was very likely much too low to be fully effective for such purposes"

"Taken together, I would guess that doses of bicalutamide of 6.25 to 50 mg/day may be appropriate for use in the context of substantial suppression of testosterone levels (<200 ng/dL), whereas higher doses of 150 to 300 mg/day may be appropriate for use as a monotherapy (i.e., without an estrogen or other antigonadotropin, for instance to block puberty). Note that, due to increased estradiol levels, considerable to full feminization will likely occur with bicalutamide monotherapy (at sufficiently high doses such that testosterone is adequately blocked). Hence, there isn't really a good reason to actually use bicalutamide monotherapy. It's best to just combine it with at least some amount of estrogen, which will suppress testosterone levels and greatly reduce the required bicalutamide dosage (and cost)."





Yeah I wanted to try this some years ago and impossible to buy it. But it still not something I would recommend even if it had worked for me. Because it might not* be safe to use.

I can't exactly agree with 5AR inhibitors either since they have an effect on vital neurosteroids, which is rarely spoken about. My point is that all anti-androgens have negatives, but it depends on whether the potential negatives outweigh the benefits; in my case, the benefits outweigh the negatives. It's a case of carefully picking our choice of poison.

Although, the evidence provided isn't relevant in my opinion; those suffering with androgenic alopecia don't want significant feminisation. Transgender women do want feminisation, in which those doses recommended would be efficacious as mono-therapy especially since bicalutamide has such a significant rate of gynecomastia at those doses. If we look at the two main users of bicalutamide on this site [Ein & Maave] they didn't require such significant doses. Ein experienced great results when using bicalutamide at 50mg/day along with finasteride. Maave had great success when using 100mg/day but didn't accompany it with a 5AR inhibitor.

 

[Ikarus]

good luck trying to get bicalutamide prescribed, I already said 4 to 5 times that I have called multiple trans doctors and they told me the drug is NOT able to be prescribed for hrt because it doesn't reduce androgen levels, it isn't an antigonaditropen, it isn't a SAA, its actually an NSAA, it has antiprogestinic effects, it doesn't reduce muscle mass, it doesn't reduce bone mass, or redistribute body fat, and you continue to keep posting random quotes backing your claims with no studies to support.

Bicalutamide is great for use in non-binary patients, though!

 

[itchymadscalp]

I can't exactly agree with 5AR inhibitors either since they have an effect on vital neurosteroids, which is rarely spoken about. My point is that all anti-androgens have negatives, but it depends on whether the potential negatives outweigh the benefits; in my case, the benefits outweigh the negatives. It's a case of carefully picking our choice of poison.

Although, the evidence provided isn't relevant in my opinion; those suffering with androgenic alopecia don't want significant feminisation. Transgender women do want feminisation, in which those doses recommended would be efficacious as mono-therapy especially since bicalutamide has such a significant rate of gynecomastia at those doses. If we look at the two main users of bicalutamide on this site [Ein & Maave] they didn't require such significant doses. Ein experienced great results when using bicalutamide at 50mg/day along with finasteride. Maave had great success when using 100mg/day but didn't accompany it with a 5AR inhibitor.

Yeah maybe I'm wrong when I say 25-50mg Bicalutamide is not enough and not safe to fight hairloss and stay a male. But it still make sense to me. Time will say maybe. But nobody can pretend we are sure it's safe and effective, especially when used long term. I just want to temper the optimism, not just because I'm an a**h**, but because when I started those drugs I was so happy, I thought I was going to use the perfect drugs to win against baldness. And it made things a lot worse.
We should be a lot cautious. Because we are promoting drugs a lot of guys read us and some of us are desperate (like I was, and still am) and can try everything and it might be detrimental to their health. That's all.

I'm willing to try everything for keep my hair ... no ... to get my hair back. But it's just because I'm insane and I must admit I have some gender issues. But I cannot really recommend what I took and I'm taking, not because it didn't work at all, but because I don't want to be responsible for being someone in a dangerous health situation. Sorry for my english, I hope you can understand what I wanted to say.

 

[Ikarus]

I still think you're wrong.
But you see maybe with all your posts promoting Bicalutamide some guys will be willing to try and maybe we will see a lot of good reviews thanks to Bicalutamide. And maybe those guys who will take Bicalutamide for years and it will work wonders with no bad side effects and everyone will be happy with that.
Or ... It will do the opposite and be dangerous. But who cares ? ...
I think you shouldn't pretend Bicalutamide is safe and effective, because you just don't know and you're not a doctor. I'm not a doctor either, that's why I say we should remain cautious, and if we want to try it's at our own risks ... and that what I did ... I tried and it was a big fail. Even Lupron + high dose Estradiol is a fail. I'm not promoting it, even if I think it's safer (Lupron) than Bica.

Personally I don't believe bicalutamide is entirely safe for use in comparison to 5AR inhibitors, but it's definitely safer than spironolactone/cyproterone acetate/flutamide. I just don't think it should be used alone; I believe it should be used in combination with finasteride/dutasteride/estradiol, just so higher doses aren't required. I would much rather use estradiol and bicalutamide at 25mg/day rather than bicalutamide at 100mg/day alone.

 

[itchymadscalp]

Personally I don't believe bicalutamide is entirely safe for use in comparison to 5AR inhibitors, but it's definitely safer than spironolactone/cyproterone acetate/flutamide. I just don't think it should be used alone; I believe it should be used in combination with finasteride/dutasteride/estradiol, just so higher doses aren't required. I would much rather use estradiol and bicalutamide at 25mg/day rather than bicalutamide at 100mg/day alone.

I agree. I used Cypro ... and my prolactin was really high. It could have been dangerous. And spironolactone was to weak at 200mg a day, it was not wise to increase the dose.
I tried to find pictures of @Ein ... But if I recall correctly his hair condition was not that bad ... and now he has "kid" hairline.

 

[Ikarus]

Yeah maybe I'm wrong when I say 25-50mg Bicalutamide is not enough and not safe to fight hairloss and stay a male. But it still make sense to me. Time will say maybe. But nobody can pretend we are sure it's safe and effective, especially when used long term. I just want to temper the optimism, not just because I'm an a**h**, but because when I started those drugs I was so happy, I thought I was going to use the perfect drugs to win against baldness. And it made things a lot worse.
We should be a lot cautious. Because we are promoting drugs a lot of guys read us and some of us are desperate (like I was, and still am) and can try everything and it might be detrimental to their health. That's all.

I'm willing to try everything for keep my hair ... no ... to get my hair back. But it's just because I'm insane and I must admit I have some gender issues. But I cannot really recommend what I took and I'm taking, not because it didn't work at all, but because I don't want to be responsible for being someone in a dangerous health situation. Sorry for my english, I hope you can understand what I wanted to say.

In your case, you have self-inflicted hyperandrogenicity which plays such a significant factor. Personally, I do not like being overly optimistic about the use of medications because an unexpected u-turn could occur... It would be greatly unfortunate if I had jinxed myself! I just post updates of my hair, and let others dictate the results since I am fearful of jinxing myself.

 

[Ikarus]

I agree. I used Cypro ... and my prolactin was really high. It could have been dangerous. And spironolactone was to weak at 200mg a day, it was not wise to increase the dose.
I tried to find pictures of @Ein ... But if I recall correctly his hair condition was not that bad ... and now he has "kid" hairline.

Ein was suffering from the typical diffuse thinning which south-asian individuals suffer from. It was definitely visible, although minor; his baseline hairline was an norwood zero, though.

 

[itchymadscalp]

In your case, you have self-inflicted hyperandrogenicity which plays such a significant factor. Personally, I do not like being overly optimistic about the use of medications because an unexpected u-turn could occur... It would be greatly unfortunate if I had jinxed myself! I just post updates of my hair, and let others dictate the results since I am fearful of jinxing myself.

Yeah I find it : https://www.hairlosstalk.com/intera...-initial-shedding-from-anti-androgens.111183/
But I dont know if its before or after using Bica ... I really think it's before.

Yeah you're right. My situation is pretty uncommon. But it can happen to everybody. Finateride and Dutateride 'destroyed' me. But I still promoting it anyway. But I won't promote strong AA, because some young men read us, and immaturity + desperation (sorry if this word doesn't exist) can me people do stupid things.

I hope it will work for you. It would be great. But I think it would be better for you if you were using something like Lupron. But I get it, it's not easy to find a doctor ok with that.
BTW ... I'm not sure if I told you about estradiol injection ... a cheaper way to get it

Spoiler: here

lena.kiev.ua/EV

- that's what I use

 

[itchymadscalp]

Ein was suffering from the typical diffuse thinning which south-asian individuals suffer from. It was definitely visible, although minor; his baseline hairline was an norwood zero, though.

Ok my bad then.

 

[Ikarus]

Yeah I find it : https://www.hairlosstalk.com/intera...-initial-shedding-from-anti-androgens.111183/
But I dont know if its before or after using Bica ... I really think it's before.

Yeah you're right. My situation is pretty uncommon. But it can happen to everybody. Finateride and Dutateride 'destroyed' me. But I still promoting it anyway. But I won't promote strong AA, because some young men read us, and immaturity + desperation (sorry if this word doesn't exist) can me people do stupid things.

I hope it will work for you. It would be great. But I think it would be better for you if you were using something like Lupron. But I get it, it's not easy to find a doctor ok with that.
BTW ... I'm not sure if I told you about estradiol injection ... a cheaper way to get it

Spoiler: here

lena.kiev.ua/EV

- that's what I use

I only think those suffering with hair loss similar to mine should consider potent anti-androgens. I most likely have the worst case of hair loss seen on this website for my age, in which dutasteride will not be effective (I will provide an image of the condition of my hair pre-treatment; I was eighteen in this particular image). I actually do want to use Lupron, and I will ask the endocrinologist I visit in two weeks about it...

 

[itchymadscalp]

I only think those suffering with hair loss similar to mine should consider potent anti-androgens. I most likely have the worst case of hair loss seen on this website, in which dutasteride will not be effective (I will provide an image of the condition of my hair pre-treatment; I was eighteen in this particular image). I actually do want to use Lupron, and I will ask the endocrinologist I visit in two weeks about it...

I hope it will work, try to find very good articles about Lupron. It's always nice to have some good data to reassure them. That's what I did.
Lupron + Estradiol will be the safest option for you and maybe the cure !!!
I don't think you're the worst case, but it's very bad for 18.