Kintor Pharmaceutical Announced U.S. FDA Has Greenlighted Phase II Clinical Trial for Pyrilutamide to Treat Androgenetic Alopecia

Redgate

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For those who don't know what this is, read this thread.
Pyrilutamide and proxalutamide are very interesting, and they seem to be moving quite fast. Faster than other garbage biotech/pharma startups.
It's a good thing their entire pipeline is AR antagonists.
 

Chads don't bald

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It's an antagonist but it still has to compete with dht as dht has a high binding affinity.
I suppose it depends what percent of DHT is able to bind with this topical. If it's a negligble amount, then I would assume taking finasteride is useless. If not, then yes this topical + finasteride would have a synergistic effect.

Still though, it likely won't do much for new hair growth for someone who is already bald. I think the Wnt pathway is the right target for that. For example Ky19382
 

Diffused_confidence

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I suppose it depends what percent of DHT is able to bind with this topical. If it's a negligble amount, then I would assume taking finasteride is useless. If not, then yes this topical + finasteride would have a synergistic effect.

Still though, it likely won't do much for new hair growth for someone who is already bald. I think the Wnt pathway is the right target for that. For example Ky19382
Oh no doubt this is for prevention only. But lots of guys who aren't getting stabilization with finasteride alone could add this to their stack and have a better chance to maintain for a very long time.
 

trialAcc

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This might even cause some regrowth. Once you know your hairloss is not gonna get worse, and you are not gonna suffer major side effects you can actually get a serious hair transplant with peace of mind. It's the close to a cure in my book
It's not a cure, but it's going to be a good tool with some actual safety data behind it. Tons of people take RU right now, and no one is claiming that it is a cure for hairloss. This drug is stronger, but I still doubt it will completely halt hairloss on it's own in 100% of people.
 

trialAcc

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Maybe a somewhat stronger RU, nothing fancy.

If you can't tolerate current-gen antiandrogens this won't change anything for you.
Which is a pretty big deal for people who don't want to take grey market untested powder from China. This will change a lot for quite a few people who don't get maintenance of finasteride/dutasteride by themselves.
 

Diffused_confidence

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Which is a pretty big deal for people who don't want to take grey market untested powder from China. This will change a lot for quite a few people who don't get maintenance of finasteride/dutasteride by themselves.
Agreed. If this goes to market then I will definitely use it to maintain what I have and feel a lot more comfortable getting a hair transplant to bring me down to Norwood 1.5.
 

Chads don't bald

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Agreed. If this goes to market then I will definitely use it to maintain what I have and feel a lot more comfortable getting a hair transplant to bring me down to Norwood 1.5.
What are you at right now?

I'm about a NW1.5 with thinning all over and I plan to wait for the prlr antagonist + wnt agonist in combination with the AR antagonist. Those 3 combined could probably cure hair loss for someone not too far gone. And this is not even taking into account hair cloning.

I might still get a transplant to rock a NW0 lol. I can't believe that in like the next 10 years I might have better hair than I did in my teens
 

hemingway_the_mercenary

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There seems to be some misunderstanding in this thread unforutantely

Unless this drug has a potency somewhat similar to finasteride then it's topical use will not be anything near a cure much like CB, RU, etc, etc. After many years of experimantation and research I've come to realize that the main barrier to success with topicals AR blockers is their absorption to the follicle. No vehicle or method of delivery (topically) is going to change this unforutantly, speaking from experiance.

Their other drug proxalutamide for prostate cancer is one I've spoken about years ago. It too has a binding affinity somewhat similar to Enza and Darolutamide. None of these have been potent enought to half hair loss progression with the minimal scalp absorption we can create. If we were able to deliver even 3mg on an active drug to the follicles from the scalp then hair loss woul've been "cured" a long time ago with drugs like OH-Flut, CB, etc.

The problem is we can not. It's not easy delivering that much drug all the way to the deep dermis from topical application. So no, don't really have much hopes set on this. It certainly won't be a replacement for finasteride but it can be a nice add on like CB

HOWEVER, their other drug they have recently stared developing for topical application, GT20029 , has some REAL potential. It's an AR degrader using the modern ubiquitin-ligase degradation method which essentially means it makes your own cell target the AR once it's bound to it and degrade the entire protein complex (ie the AR). It means the molecule has to be much larger so absorption may be an issue BUT it increases its potency MASSIVELY to almost the same level as DHT and Testosterone for activating/degrading the AR.


Here's a little snipped of it, you can read more into it by doing your own research if you'd like:
"GT20029 is a topical androgen receptor ("AR") degrader developed by using Kintor's in-house Proteolysis Targeting Chimera ("PROTAC") platform. PROTAC is a small molecule composed of (i) a recruiting element for a protein of interest ("POI"); (ii) an E3 ubiquitin ligase recruiting element; and (iii) a linker bounding (i) and (ii). After the ternary complex is formed, by bridging the gap between a POI and an E3 ubiquitin ligase and inducing their proximity, PROTAC can induce the ubiquitination of the POI and then degrade the POI. As each PROTAC molecule can degrade multiple AR proteins, drugs based on PROTAC can achieve efficacy with a low dosage. In addition, as long as there are a small amount of PROTAC molecules in the cells, the efficacy of the drugs can be maintained, which can significantly reduce the dosing frequency as compared to other small molecule drugs."
 

Diffused_confidence

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There seems to be some misunderstanding in this thread unforutantely

Unless this drug has a potency somewhat similar to finasteride then it's topical use will not be anything near a cure much like CB, RU, etc, etc. After many years of experimantation and research I've come to realize that the main barrier to success with topicals AR blockers is their absorption to the follicle. No vehicle or method of delivery (topically) is going to change this unforutantly, speaking from experiance.

Their other drug proxalutamide for prostate cancer is one I've spoken about years ago. It too has a binding affinity somewhat similar to Enza and Darolutamide. None of these have been potent enought to half hair loss progression with the minimal scalp absorption we can create. If we were able to deliver even 3mg on an active drug to the follicles from the scalp then hair loss woul've been "cured" a long time ago with drugs like OH-Flut, CB, etc.

The problem is we can not. It's not easy delivering that much drug all the way to the deep dermis from topical application. So no, don't really have much hopes set on this. It certainly won't be a replacement for finasteride but it can be a nice add on like CB

HOWEVER, their other drug they have recently stared developing for topical application, GT20029 , has some REAL potential. It's an AR degrader using the modern ubiquitin-ligase degradation method which essentially means it makes your own cell target the AR once it's bound to it and degrade the entire protein complex (ie the AR). It means the molecule has to be much larger so absorption may be an issue BUT it increases its potency MASSIVELY to almost the same level as DHT and Testosterone for activating/degrading the AR.


Here's a little snipped of it, you can read more into it by doing your own research if you'd like:
"GT20029 is a topical androgen receptor ("AR") degrader developed by using Kintor's in-house Proteolysis Targeting Chimera ("PROTAC") platform. PROTAC is a small molecule composed of (i) a recruiting element for a protein of interest ("POI"); (ii) an E3 ubiquitin ligase recruiting element; and (iii) a linker bounding (i) and (ii). After the ternary complex is formed, by bridging the gap between a POI and an E3 ubiquitin ligase and inducing their proximity, PROTAC can induce the ubiquitination of the POI and then degrade the POI. As each PROTAC molecule can degrade multiple AR proteins, drugs based on PROTAC can achieve efficacy with a low dosage. In addition, as long as there are a small amount of PROTAC molecules in the cells, the efficacy of the drugs can be maintained, which can significantly reduce the dosing frequency as compared to other small molecule drugs."
I've been talking about gt20029 for awhile. My only fear about that one is potential side effects could be horrible beyond anything.
 

Dimitri001

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For those who don't know what this is, read this thread.
Pyrilutamide and proxalutamide are very interesting, and they seem to be moving quite fast. Faster than other garbage biotech/pharma startups.
It's a good thing their entire pipeline is AR antagonists.

I hope the biotech/pharma community becomes aware of the PRL angle soon, as it is infinitely superior to targeting the AR both in potency and in that it (seemingly) doesn't have the potential for terrible sides, as the AR angle always does. Hopefully in the future we see companies whose entire pipelines are PRL-related.
 

trialAcc

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There seems to be some misunderstanding in this thread unforutantely

Unless this drug has a potency somewhat similar to finasteride then it's topical use will not be anything near a cure much like CB, RU, etc, etc. After many years of experimantation and research I've come to realize that the main barrier to success with topicals AR blockers is their absorption to the follicle. No vehicle or method of delivery (topically) is going to change this unforutantly, speaking from experiance.

Their other drug proxalutamide for prostate cancer is one I've spoken about years ago. It too has a binding affinity somewhat similar to Enza and Darolutamide. None of these have been potent enought to half hair loss progression with the minimal scalp absorption we can create. If we were able to deliver even 3mg on an active drug to the follicles from the scalp then hair loss woul've been "cured" a long time ago with drugs like OH-Flut, CB, etc.

The problem is we can not. It's not easy delivering that much drug all the way to the deep dermis from topical application. So no, don't really have much hopes set on this. It certainly won't be a replacement for finasteride but it can be a nice add on like CB

HOWEVER, their other drug they have recently stared developing for topical application, GT20029 , has some REAL potential. It's an AR degrader using the modern ubiquitin-ligase degradation method which essentially means it makes your own cell target the AR once it's bound to it and degrade the entire protein complex (ie the AR). It means the molecule has to be much larger so absorption may be an issue BUT it increases its potency MASSIVELY to almost the same level as DHT and Testosterone for activating/degrading the AR.


Here's a little snipped of it, you can read more into it by doing your own research if you'd like:
"GT20029 is a topical androgen receptor ("AR") degrader developed by using Kintor's in-house Proteolysis Targeting Chimera ("PROTAC") platform. PROTAC is a small molecule composed of (i) a recruiting element for a protein of interest ("POI"); (ii) an E3 ubiquitin ligase recruiting element; and (iii) a linker bounding (i) and (ii). After the ternary complex is formed, by bridging the gap between a POI and an E3 ubiquitin ligase and inducing their proximity, PROTAC can induce the ubiquitination of the POI and then degrade the POI. As each PROTAC molecule can degrade multiple AR proteins, drugs based on PROTAC can achieve efficacy with a low dosage. In addition, as long as there are a small amount of PROTAC molecules in the cells, the efficacy of the drugs can be maintained, which can significantly reduce the dosing frequency as compared to other small molecule drugs."
Could easily be a replacement for finasteride, this is heavy bro science. The reason these topical AAs work is because they overload the AR and compete for T/DHT, this means that they still work even with a small percentage of reaching the follicle. Comparing this to CB is ridiculous as well, as its more then 100x stronger in it's binding affinity then CB. Many people also get maintenance on higher doses of RU, which would be no different then standard doses of KX.

The question is how long the effects can be maintained, but I see no reason why these results won't come back above baseline at 1 year's time.
 
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Diffused_confidence

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I hope the biotech/pharma community becomes aware of the PRL angle soon, as it is infinitely superior to targeting the AR both in potency and in that it (seemingly) doesn't have the potential for terrible sides, as the AR angle always does. Hopefully in the future we see companies whose entire pipelines are PRL-related.
I'm not aware of prl. Is that kintor?
 

hemingway_the_mercenary

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Could easily be a replacement for finasteride, this is heavy bro science. The reason these topical AAs work is because they overload the AR and compete for T/DHT, this means that they still work even with a small percentage of reaching the follicle. Comparing this to CB is ridiculous as well, as its more then 100x stronger in it's binding affinity then CB. Many people also get maintenance on higher doses of RU, which would be no different then standard doses of KX.

The question is how long the effects can be maintained, but I see no reason why these results won't come back above baseline at 1 year's time.
Ahhh I feel for you bro, you’re just going to be heavily disappointed

btw no one with any level of aggressive hairloss is maintaining on RU at all. They’re all combing it with finasteride, minx, dutasteride, etc etc

Where did they publish a comparison of this drugs binding affinity with CB? You also need to account for the ic50 and a bunch of other factors as well. Don’t get your hopes up too high
 
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