Comparison Of Every Possible Treatment Available For Hair Loss

[theotherusero]

I've created a google sheet summary with all the available treatments I was able to gather from the various post I read.
Here's the link:
https://docs.google.com/spreadsheets/d/1T6VtoLMhwm_r-fwq43UQw-elfjBUfMzjwZfX3wm7NPg/edit?usp=sharing

I'm by no means an expert in hair loss, but I'm trying to understand what is the best trade-off in terms of efficacy/safety/price.

For example, a good idea in terms of safety, while maintaining the same efficacy would be using eplerenone instead of spironolactone, as from a post from @pegasus2 "Risk of gyno with eplerenone is only .5% compared with 10% for spironolactone".

Another great quote from @pegasus2 that inspired me to create this document: "RU + estriol + eplerenone may be the right combination for people looking for a simple solution without side effects."

I have seen a lot of good info but it is scattered on various threads. I would think it would be very useful to have a sort of summary to quickly compare the various possible treatments.
What do you guys think?

By the way, as you can see if you open the document, it is a work in progress and I'm sure it has a more than few errors in it. If you would like to contribute to the document just send me a pm with the mail of your google account and I will give you write access.

Regard columns F, G, H respectively efficacy, safety, and monthly price, I was not sure if to include them, as the ranking would be subjective and surely inaccurate, but it seemed a quick way to compare treatments. Of course, take that numbers with a grain of salt.

I hope some you will want to help improve the document.

 

[theotherusero]

5Α-REDUCTASE INHIBITOR COMPARISON

5-ARIs are most known for preventing conversion of testosterone, the major androgen sex hormone, to the more potent androgen dihydrotestosterone (DHT)

Finasteride is a 5α-reductase inhibitor and therefore an antiandrogen. It works by decreasing the production of dihydrotestosterone (DHT) by about 70%, including in the prostate gland and the scalp.

Dutasteride is a 5α-reductase inhibitor. It is also used for scalp hair loss in men.
Dutasteride (brand name Avodart) inhibits all three 5α-reductase isoenzymes and can decrease DHT levels by 95%.

Alfatradiol is a weak estrogen and 5α-reductase inhibitor. In contrast to minoxidil, alfatradiol did not result in an increase of hair density or thickness, but only in slowing down or stabilization of hair loss in this study. In an earlier study, no systemic side effects were noted, and 17α-estradiol was found to reduce androgenic hair loss, though it was not effective at growing new hair.

Saw Palmetto is a weak 5ar inhibitor about half as effective as finasteride for both reducing DHT and halting hair loss.

https://en.wikipedia.org/wiki/5α-Reductase_inhibitor
https://en.wikipedia.org/wiki/Finasteride
https://en.wikipedia.org/wiki/Dutasteride
https://www.hairlosstalk.com/intera...finasteride-studies-and-my-experience.101402/


Finasteride and the more potent Dutasteride are the most common and proven options, unfortunately the possible side effects includes sexual dysfunction, depression, and breast enlargement.
Alfatradiol on the paper is both a 5α-reductase inhibitor (stop DHT) and a weak estrogen (promotes regrowth) and has no side effects. What's the catch? Here's the answer:
https://www.hairlosstalk.com/intera...e-if-its-any-of-the-same.124683/#post-1849627

TLDR: limited evidence, Alfatradiol has never been proven to inhibit 5-ar in vivo, only in an in vitro assay of cut rat liver, Alfatradiol is biologically inactive, it doesn't act agonistically on estrogen receptors in the body, it's supposed to be a weak 5-ARI.
Saw Palmetto, I haven't read a lot a about it, but it is weaker than Finasteride both in terms of efficacy and side effects.

So unsuprisingly the ranking in terms of efficacy and safety for the 4 5α-Reductase inhibitor is specular.
Ranked by efficacy: Dutasteride, Finasteride, Saw Palmetto, Alfatradiol
Ranked by safety: Alfatradiol, Saw Palmetto, Finasteride, Dutasteride
Maybe ranking in terms of the efficacy of Saw Palmetto and Alfatradiol can be reversed?

I would like to write similar posts for other categories of hair loss treatment, such as NSAAs.
If someone more expert would like to contribute or correct me, I would be glad!

 

[theotherusero]

NSAAs COMPARISON

FIRST-GENERATION NSAAS
Relative to the earlier antiandrogens, bicalutamide has substantially reduced toxicity, and in contrast to them, is said to have an excellent and favorable safety profile. For these reasons, as well as superior potency, tolerability, and pharmacokinetics, bicalutamide is preferred and has largely replaced flutamide and nilutamide in clinical practice. In accordance, bicalutamide is the most widely used antiandrogen in the treatment of prostate cancer.
The core side effects of NSAAs such as gynecomastia, sexual dysfunction, and hot flashes occur at similar rates with the different drugs.

SECOND-GENERATION NSAAS
Enzalutamide, along with the in-development apalutamide and darolutamide, are newer, second-generation NSAAs. Similarly to bicalutamide and the other first-generation NSAAs, they possess the same core mechanism of action of selective AR antagonism but are thought to bind to the androgen receptor with higher affinity
In comparison to bicalutamide, enzalutamide has 5- to 8-fold higher affinity for the AR
In terms of tolerability, enzalutamide and bicalutamide appear comparable in most regards, with a similar moderate negative effect on sexual function and activity for instance. However, enzalutamide has a risk of seizures and other central side effects such as anxiety and insomnia related to off-target GABAA receptor inhibition that bicalutamide does not appear to have. On the other hand, unlike with all of the earlier NSAAs (flutamide, nilutamide, and bicalutamide), there has been no evidence of hepatotoxicity or elevated liver enzymes in association with enzalutamide treatment in clinical trials.

STEROIDAL ANTIANDROGENS
Due to the different hormonal activities of NSAAs like bicalutamide and SAAs like CPA, they possess different profiles of adverse effects. CPA is regarded as having an unfavorable side effect profile, and the tolerability of bicalutamide is considered to be superior. One advantage of CPA over NSAAs is that, because it suppresses estrogen levels rather than increases them, it is associated with only a low rate of what is generally only slight gynecomastia (4–20%).
https://en.wikipedia.org/wiki/Comparison_of_bicalutamide_with_other_antiandrogens


So it can be said that:
- Bicalutamide is more potent and safer than the steroidal antiandrogen Cyproterone acetate.
- Bicalutamide is more potent and safer for the treatment of prostate cancer than other first-gen NSAAs flutamide and nilutamide.


What about hydroxyflutamide/oh-flutamide?
Hydroxyflutamide (HF, OHF) (developmental code name SCH-16423), or 2-hydroxyflutamide, is a nonsteroidal antiandrogen (NSAA) and the major active metabolite of flutamide, which is considered to be a prodrug of hydroxyflutamide as the active form.
https://en.wikipedia.org/wiki/Hydroxyflutamide
So I suppose it should have the same effects and sides as flutamide, therefore Bicalutamide is better?
Here is a thread about it https://www.hairlosstalk.com/intera...abolite-of-flutamide-a-better-ru58841.121993/
@TK421 has used it for a while and suggest Topilutamide instead "as it's less expensive and commercially available."


It is more difficult to rate in terms of efficacy/safety the remaining NSAAs:
- Bicalutamide
- Apalutamide
- Enzalutamide
- Darolutamide
- RU58841
- Topilutamide


What about Topilutamide, the only NSAAs marketed for hair loss?
Topilutamide (Eucapil): Also known as fluridil. Marketed as a topical medication for the treatment of pattern hair loss (androgenic alopecia) in the Czech Republic and Slovakia. Limited availability and lack of an oral formulation for systemic use make it a very little-known drug.
https://en.wikipedia.org/wiki/Topilutamide

Quotes from various threads:
@xaragedom finasteride is a 5ar inhibitor while eucapil is working by blocking androgen receptor so you can use both at the same time although I dont know if eucapil give you any effects. Never saw an improvment with it.
@el_duterino on paper its great, in practice its very weak, and i tried like 3 times the amount per day for months not worth your money or time no side effects but no effects on hair
@mannyFJ Probably 4 months and still on fence if its helping
@TK421 The only topical compound I know of that supposedly binds directly to androgen receptors and has no side effects is Fluridil (topilutamide). However, after using for 8 months I can say that it wasn't strong enough for me. I noticed a decrease in shedding for maybe the first month but then shedding went back to normal. I definitely lost ground the past few months. Are the two compounds you posted available?

The reviews aren't very promising...
So, the safest NSAAs is Topilutamide, unfortunately, it is also very weak in terms of efficacy.


How does Bicalutamide compare with second-generation NSAAs such as Apalutamide, Enzalutamide Darolutamide?

What about RU58841 it is better/safer than the rest of NSAAs?

 

[d3nt3dsh0v3l]

NSAAs COMPARISON

FIRST-GENERATION NSAAS
Relative to the earlier antiandrogens, bicalutamide has substantially reduced toxicity, and in contrast to them, is said to have an excellent and favorable safety profile. For these reasons, as well as superior potency, tolerability, and pharmacokinetics, bicalutamide is preferred and has largely replaced flutamide and nilutamide in clinical practice. In accordance, bicalutamide is the most widely used antiandrogen in the treatment of prostate cancer.
The core side effects of NSAAs such as gynecomastia, sexual dysfunction, and hot flashes occur at similar rates with the different drugs.

SECOND-GENERATION NSAAS
Enzalutamide, along with the in-development apalutamide and darolutamide, are newer, second-generation NSAAs. Similarly to bicalutamide and the other first-generation NSAAs, they possess the same core mechanism of action of selective AR antagonism but are thought to bind to the androgen receptor with higher affinity
In comparison to bicalutamide, enzalutamide has 5- to 8-fold higher affinity for the AR
In terms of tolerability, enzalutamide and bicalutamide appear comparable in most regards, with a similar moderate negative effect on sexual function and activity for instance. However, enzalutamide has a risk of seizures and other central side effects such as anxiety and insomnia related to off-target GABAA receptor inhibition that bicalutamide does not appear to have. On the other hand, unlike with all of the earlier NSAAs (flutamide, nilutamide, and bicalutamide), there has been no evidence of hepatotoxicity or elevated liver enzymes in association with enzalutamide treatment in clinical trials.

STEROIDAL ANTIANDROGENS
Due to the different hormonal activities of NSAAs like bicalutamide and SAAs like CPA, they possess different profiles of adverse effects. CPA is regarded as having an unfavorable side effect profile, and the tolerability of bicalutamide is considered to be superior. One advantage of CPA over NSAAs is that, because it suppresses estrogen levels rather than increases them, it is associated with only a low rate of what is generally only slight gynecomastia (4–20%).
https://en.wikipedia.org/wiki/Comparison_of_bicalutamide_with_other_antiandrogens


So it can be said that:
- Bicalutamide is more potent and safer than the steroidal antiandrogen Cyproterone acetate.
- Bicalutamide is more potent and safer for the treatment of prostate cancer than other first-gen NSAAs flutamide and nilutamide.


What about hydroxyflutamide/oh-flutamide?
Hydroxyflutamide (HF, OHF) (developmental code name SCH-16423), or 2-hydroxyflutamide, is a nonsteroidal antiandrogen (NSAA) and the major active metabolite of flutamide, which is considered to be a prodrug of hydroxyflutamide as the active form.
https://en.wikipedia.org/wiki/Hydroxyflutamide
So I suppose it should have the same effects and sides as flutamide, therefore Bicalutamide is better?
Here is a thread about it https://www.hairlosstalk.com/intera...abolite-of-flutamide-a-better-ru58841.121993/
@TK421 has used it for a while and suggest Topilutamide instead "as it's less expensive and commercially available."


It is more difficult to rate in terms of efficacy/safety the remaining NSAAs:
- Bicalutamide
- Apalutamide
- Enzalutamide
- Darolutamide
- RU58841
- Topilutamide


What about Topilutamide, the only NSAAs marketed for hair loss?
Topilutamide (Eucapil): Also known as fluridil. Marketed as a topical medication for the treatment of pattern hair loss (androgenic alopecia) in the Czech Republic and Slovakia. Limited availability and lack of an oral formulation for systemic use make it a very little-known drug.
https://en.wikipedia.org/wiki/Topilutamide

Quotes from various threads:
@xaragedom finasteride is a 5ar inhibitor while eucapil is working by blocking androgen receptor so you can use both at the same time although I dont know if eucapil give you any effects. Never saw an improvment with it.
@el_duterino on paper its great, in practice its very weak, and i tried like 3 times the amount per day for months not worth your money or time no side effects but no effects on hair
@mannyFJ Probably 4 months and still on fence if its helping
@TK421 The only topical compound I know of that supposedly binds directly to androgen receptors and has no side effects is Fluridil (topilutamide). However, after using for 8 months I can say that it wasn't strong enough for me. I noticed a decrease in shedding for maybe the first month but then shedding went back to normal. I definitely lost ground the past few months. Are the two compounds you posted available?

The reviews aren't very promising...
So, the safest NSAAs is Topilutamide, unfortunately, it is also very weak in terms of efficacy.


How does Bicalutamide compare with second-generation NSAAs such as Apalutamide, Enzalutamide Darolutamide?

What about RU58841 it is better/safer than the rest of NSAAs?

Relative to other NSAAs, nilutamide is unique in its potential to produce side effects such as vision impairment and lung damage (interstitial pneumonitis). It is also worth noting that while human clinical trials have not been run on RU-58841, similar side effects have been reported anecdotally. RU-58841 is similar in chemical structure to nilutamide, certainly suggesting the possibility for those side effects to occur. Therefore, one might to first order assume that RU-58841 shares a similar side effect profile to that of nilutamide.

https://en.wikipedia.org/wiki/Nilutamide#Side_effects

Nilutamide

RU-58841