- Reaction score
- 2,034
What would make this med superior chemically to some of the other topicals like spironolactone, RU, CB, Alfatraiol? I am interested in the science and chemical structure if anyone knows?
Kintor new AR degrader w/o side effects
- Thread starter FollicleGuardian
- Start date
-
- Tags
- ar degrader kintor
- Reaction score
- 2,034
Votre anglais est tres bon mais c'est quoi, AAG?
Some time ago the plan was commercialization in Q1 (or maybe it was H1) 2022. But that is already delayed. We can expect the phase 2 results within the next 6 months
Oh i'm so sorry ! It means male pattern baldness in the french way hahahaha, I edit now
- Reaction score
- 1,003
AR degradation, safe ? Only if it affect locally
- Reaction score
- 3,660
Theoretically that's possible. Without AR it shouldn't be possible to continue balding. However, my >6 years of experience in combating hair loss tells me that this drug is nothing to be excited about yet. There are still many, many unknowns.
For instance, aside from ASC-J9 (dimethylcurcumin), AR degraders have not been used against Androgenetic Alopecia thus far. ASC-J9 effect was marginal and poor, but it was not a very good product in the first place.
There was another recently discovered AR degrader (very strong) called ARD-69:
In fact, the mechanisms are very similar to this Kintor product:
"ARD-69 is a potent proteolysis-targeting chimera (PROTAC) degrader of the androgen receptor (AR) ... It contains an AR antagonist (reported in [1]) that binds the AR, joined by a small linker molecule to a second ligand (in this case a VHL ligand) that engages the E3 ubiquitin ligase system via Cullin-2.
"GT20029 is an AR degrader that degrades the AR protein. The mechanism of action of GT20029 is to recruit the AR protein to the E3 ubiquitin ligase for degradation."
I wonder if Kintor perhaps bought out the rights to ARD-69 and whether it is the same thing. Haven't looked that in-depth into it.
Either way if you look at the molecular structure of ARD you notice that this molecule is much more complex than a typical anti-androgen, although once the linker chain breaks you are still left with a sort of typical AA structure floating around. I guess it will depend on how exactly these drugs are metabolized but unless it completely loses its affinity for the AR (and doesn't fall apart into small molecules which have their own AR affinity) once it hits the bloodstream, then there is still the potential for systemic side effects.
What about Fluridil? I read somewhere that it also degrades the AR
People were using too low a dose with ASC-J9 to say its effect was marginal. Everyone I saw on here that used it was using the acne concentration. I used 7.5x that, and I think it worked well aiding my hairline regrowth. The only reason I stopped using it was because it stains everything.
Last edited:
el_duterino
Senior Member
- Reaction score
- 397
From the past failures of ASC-J9, fluridil, it turns out that "degrading" the AR is not an easy task in practice.
You would need to use a lot of the active ingredient to achieve a sufficient level of constant degradation in order to have the cosmetic effect, via a low efficient topical delivery, thus opening more potential side effects with all this large drug metabolites in blood.
AR are designed to bind, so its much easier to block them by binding another molecule with affinity that's why all the prostate cancer drugs use this mechanism and RU, CB work even at moderately low dosage.
But, lets see what comes out of this,
You would need to use a lot of the active ingredient to achieve a sufficient level of constant degradation in order to have the cosmetic effect, via a low efficient topical delivery, thus opening more potential side effects with all this large drug metabolites in blood.
AR are designed to bind, so its much easier to block them by binding another molecule with affinity that's why all the prostate cancer drugs use this mechanism and RU, CB work even at moderately low dosage.
But, lets see what comes out of this,
- Reaction score
- 218
sorry to bother you once again with that but accordin to your extensive experienc with both drugs what's the amount of cb in mg someone has to use to get the benefits of 25 mg of RU daily ? and havae you noticed any sides using kane cb so far?
- Reaction score
- 320
I don’t know if it 100 percent translates. If I understand correctly (which I may not) RU has a higher binding affinity than CB. That means that it would take a massive amount of CB to get the same result as RU, and it still may not be as effective
- Reaction score
- 614
Where is everyone getting the impression that Fluridil is an AR degrader? It isn't.
- Reaction score
- 1,336
It's possible to reverse engineer a drug. Of course that doesn't give you the right to commercialise it but that won't matter on the grey market.
el_duterino
Senior Member
- Reaction score
- 397
binding affinity is about the same for those 2
ru goes systemic so it is more effective but also gives side effects and has never been fully tested in humans so there is no reasons anymore to take such risks anymore
in my experience using both for extended times - RU 9 years and CB 3 years, without using finasteride or dutasteride at the same time, you need about 2 or 3 times the ru amount for cb to produce the same effect on hair but without any of RU the side effects and the who-knows-what-else
If this AR degrader makes into the market, it would be a perfect combo in synergy with CB..try to degrade some AR, then block what is left over..
Last edited:
* and thicken miniaturazed hairs. So basically regrow invisible hair lol.
Last edited:
- Reaction score
- 1,104
? Lol. In worst case it will maintain
- Reaction score
- 732
Exactly. This+hair transplant= Practically the cure.
- Reaction score
- 532
AR degraders have always been very promising imo especially ones that use ubiquitin ligase to tell your own cells to break down the AR protein complex because they can be significantly more potent
there have been a couple out for 1-2 years already though, ARV-110 and ARV-330 which were potent than testosterone at binding to the receptor but unfortunately the one with the shorter half life was considered less useful so it was cancelled and I don’t think the molecular structure was ever revealed. They opted to start the trails with the one that had a long half life as obv that was more desireable for prostate cancer
we also tried to do a gb of UT-155 which was the first discovered AR degrader but that one worked through destabilization so it was much less potent and turned out to be too expensive to manufacture for the dose we would need
If anyone is interested in experimenting with topical anti androgens beyond just RU then you can join our discord server where we do some crazy sh*t:
there have been a couple out for 1-2 years already though, ARV-110 and ARV-330 which were potent than testosterone at binding to the receptor but unfortunately the one with the shorter half life was considered less useful so it was cancelled and I don’t think the molecular structure was ever revealed. They opted to start the trails with the one that had a long half life as obv that was more desireable for prostate cancer
we also tried to do a gb of UT-155 which was the first discovered AR degrader but that one worked through destabilization so it was much less potent and turned out to be too expensive to manufacture for the dose we would need
If anyone is interested in experimenting with topical anti androgens beyond just RU then you can join our discord server where we do some crazy sh*t:
Discord - Group Chat That’s All Fun & Games
Discord is great for playing games and chilling with friends, or even building a worldwide community. Customize your own space to talk, play, and hang out.
discord.gg
Last edited: