Orm-15341: Darlutamides Active Metabolite (no Reason To Use Daro)

hemingway_the_mercenary

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ORM-15341 is the main active metabolite of Daro. While Daro has a 15.8hr half life, it converts to
ORM-15341 which has an additional 10hr half life. So in effect all of the drug which goes systemic will have a half life of nearly 26 hours which is not optimal.

However, ORM-15341 is just as strong as Daro

(Ki) of 8 nM and an IC50 of 38 nM for ORM-15341
(Ki) of 11 nM and an IC50 of 26 nM for Daro

For anyone using Darolutamde topically is would be more advantageous to switch to its metabolite. This would allow you to avoid systemic side effects to a higher extent while still receiving all of the topical benefits.

What was surprising to me was Gang Lou (the guy who supplies Daro) has this in stock as well. My theory is that @IdealForehead must have figured this out and asked Gang if he would be able to supply the metabolite to him instead. They are the same price from Gang so if anyone is looking to try Daro I recommend using this instead

Also heres a little cost calculation

At 2m Bicalutamide per day I got side effects but it was super effective for hairloss. Given this is around 16x stronger on a milligram basic 2mg is a very high dose, but I will use it to be conservative.

500mg costs $150USD
at 2mg/day 500mg last 250 days
$0.60 per day

Now some people were complaining that they didn't notice anything on Darolutamdie but that is because most people used the completely wrong vehicle. You need to have a lipophillic vehicle that will be able to get the drug to the hair follicle. I have had great results with K&B solutions for bicalutamide/finasteride/spirinolactone. I much recommend it over propylene glycol, for one its better, but 2 its much healthier for your scalp.
 
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peewee

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ORM-15341 is the main active metabolite of Daro. While Daro has a 15.8hr half life, it converts to
ORM-15341 which has an additional 10hr half life. So in effect all of the drug which goes systemic will have a half life of nearly 26 hours which is not optimal.

However, ORM-15341 is just as strong as Daro

(Ki) of 8 nM and an IC50 of 38 nM for ORM-15341
(Ki) of 11 nM and an IC50 of 26 nM for Daro

For anyone using Darolutamde topically is would be more advantageous to switch to its metabolite. This would allow you to avoid systemic side effects to a higher extent while still receiving all of the topical benefits.

What was surprising to me was Gang Lou (the guy who supplies Daro) has this in stock as well. My theory is that @IdealForehead must have figured this out and asked Gang if he would be able to supply the metabolite to him instead. They are the same price from Gang so if anyone is looking to try Daro I recommend using this instead

Also heres a little cost calculation

At 2m Bicalutamide per day I got side effects but it was super effective for hairloss. Given this is around 16x stronger on a milligram basic 2mg is a very high dose, but I will use it to be conservative.

500mg costs $150USD
at 2mg/day 500mg last 250 days
$0.60 per day

Now some people were complaining that they didn't notice anything on Darolutamdie but that is because most people used the completely wrong vehicle. You need to have a lipophillic vehicle that will be able to get the drug to the hair follicle. I have had great results with K&B solutions for bicalutamide/finasteride/spirinolactone. I much recommend it over propylene glycol, for one its better, but 2 its much healthier for your scalp.

Price and supplier of k&b? Other than Kane?
 

el_duterino

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10 hours while it's lower than 26 it's still enough to get sides

I got side on topical Flutamide which has a serum half life of 7 hours
 

hemingway_the_mercenary

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Hers how Daro compares with DHT and Testosterone for strength

ORM-15341: (Ki) of 8 nM and an IC50 of 38 nM
Darolutamide: (Ki) of 11 nM and an IC50 of 26 nM
DHT: (Kd) of 0.25 to 0.5 nM and an EC50 for activation of the AR is 0.13 nM
Testosterone: Kd = 0.4 to 1.0 nM and an EC50 of 0.66 nM

unfortunately there have been no SARMs developed yet that are able to bind to the AR with the power anywhere near of even just testosterone let alone DHT. This is why we have to play a hoping game when it comes to hairloss, because nothing can bind to the AR with the power anywhere near DHT, we always need to have higher levels of the anti-androgen in order to stand a chance.

This is why I believe those of you using weaker compounds stand no chance for regrowth, everyone always says "oh anti-androgens are not enough for regrowth, you need estrogen etc etc..." Well I believe thata major reason for that fact is that we dont have a drug anywhere near as strong as needed. Hopefully, in the future, they will be able to figure it out, for women there has been a drug for year now (Raloxifene) which binds to the ER at a much much stronger affinity than estradiol.

Well anyways, this is why I believe that for now we also need to rely on estradiol if you are someone with extremely aggressive androgenic alopecia. Estradiol binds very strongly to the ER and I have no research to comfirm this but I do believe that the ER and the AR of the hair follicle cells cant be activated at the same time (Im not sure). This would explain the regrowth that becomes possible with estradiol because it would be shutting down AR expression (if my theory is correct).

Cliffs:
If your male pattern baldness is aggressive you have no shot with Ru or similarly weak anti-androgens because they bind so much weaker to the AR the testosterone
 
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DavidsDome

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when I looked into the metabolite of Daro, I couldn't find them for sale anywhere.
Great to see things have changed!
Thanks for the update.
 

franzliszt

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could you make you're own darolutamide capsules using empty gelatin capsules? or are some of the filler ingredients in Nubeqa necessary for optimal absorbtion? An alternative could be to use a DMSO solution, does anyone have any experience with this?
 

AndrewBarnes

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could you make you're own darolutamide capsules using empty gelatin capsules? or are some of the filler ingredients in Nubeqa necessary for optimal absorbtion? An alternative could be to use a DMSO solution, does anyone have any experience with this?
When you say you want to make capsules, are you intending on taking daro orally? If so, be prepared for massive gyno
 
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