Kintor's Pyrilutamide outcompetes RU-58841 (insane binding affinity)+ potential compound reveal?

[FollicleGuardian]

There has been a lot of positive updates from Kintor Pharmaceuticals. Pyrilutamide is looking to be the first anti androgen that will be approved for Androgenetic Alopecia. However the negative aspect of Kintor is the frustrating amount of secrecy from the company in terms of their drug candidates.

This is their patent https://patentimages.storage.googleapis.com/8d/2c/d6/f2d27c0a778e9a/CA2772579C.pdf

In the patent they reveal a few interesting things:

1) Pyrilutamide has an insane binding affinity (IC50)= 0.28 uM, almost 4x RU-58841 (1.1 approx)

2) Pyrilutamide outcompeted RU-5881 in their mouse study in terms of hair growth (RU score= 1.9, Pyrilutamide score= 3.7)

3) This is their "Compound 12", which was the only compound that they go into detail about that it outcompeted RU-58841 in their study:

 

[Tom4362]

This is the best news in years!!

 

[FollicleGuardian]

This is the best news since years

Yes it seems very promising!

 

[FollicleGuardian]

However I don't know if my dissection of the patent is acceptable. But I tried my best to present my findings. I hope this is right. If it is then it's insane!

 

[FollicleGuardian]

Would be great if @pegasus2 @John Difool could verify the findings. This patent is a monster.

 

[Frenchboy]

Kintor are going so fast, this is crazy!

 

[FollicleGuardian]

Kintor are going so fast, this is crazy!

Yes these guys don’t f**k around.

 

[whatevr]

And that's their 'weak' topical AR antagonist molecule. Imagine the androgen receptor degrader.

 

[FollicleGuardian]

And that's their 'weak' topical AR antagonist molecule. Imagine the androgen receptor degrader.

Hahah excactly my thought, jesus christ

 

[Tom4362]

And that's their 'weak' topical AR antagonist molecule. Imagine the androgen receptor degrader.

Isn't this (Pyrilutamide) the solution you have been waiting for since you cannot tolerate finasteride?

 

[whatevr]

Isn't this (Pyrilutamide) the solution you have been waiting for since you cannot tolorate finasteride?

Well, I am probably going to let a couple of others guinea pig this before I jump on.

 

[ElToso]

Kintor is testing these dosages:
2,5mg BID
5mg/day
5mg BID

 

[Gegen]

Cassiopea staff is probably scared with all these news coming from kintor, wtf, they probably already ate their fingers.

 

[nick123]

Cassiopea staff is probably scared with all these news coming from kintor, wtf, they probably already ate their fingers.

It's Cassiopea's own fault, they have wasted enough time.

 

[el_duterino]

This is a 10 year old patent filing, not sure if moving fast is the right word here.

But, since this is a Chinese company, we could imagine them moving faster than the Western ones.

I find it odd that they mention prostate cancer AND androgenic alopecia in the same document, or are they referring to two entirely different molecules ? for PC you need a long serum half life, for AA you want no serum life at all, or you will be facing heavy side effects.

And yes, a 1 year study on males on side effects would be needed, no doubts that this anti androgen will work for hair loss as most anti androgen work fine, the real questions are the side effects...only a long term large study on males can confirm this for approval.

For RU, the first studies in the mid 1990's on hamster flanks showed that the drug has no systemic effect on hair growth (on the other hamster flank side), and no prostate gland size change effect so it was concluded that the compound must have no side effects, but we know now its just no the case in men.

I guess they forgot to look at those hamster dicks..ha!

 

[FollicleGuardian]

Kintor is testing these dosages:
2,5mg BID
5mg/day
5mg BID

Very low dosages!

 

[FollicleGuardian]

This is a 10 year old patent filing, not sure if moving fast is the right word here.

But, since this is a Chinese company, we could imagine them moving faster than the Western ones.

I find it odd that they mention prostate cancer AND androgenic alopecia in the same document, or are they referring to two entirely different molecules ? for PC you need a long serum half life, for AA you want no serum life at all, or you will be facing heavy side effects.

And yes, a 1 year study on males on side effects would be needed, no doubts that this anti androgen will work for hair loss as most anti androgen work fine, the real questions are the side effects...only a long term large study on males can confirm this for approval.

For RU, the first studies in the mid 1990's on hamster flanks showed that the drug has no systemic effect on hair growth (on the other hamster flank side), and no prostate gland size change effect so it was concluded that the compound must have no side effects, but we know now its just no the case in men.

I guess they forgot to look at those hamster dicks..ha!

Regarding the patent including PC. This is pretty standard to cover all potential uses for a compound. They also mention it’s potential use as a male contraceptive, although it’s pretty obvious it will never be used for that.

 

[Gegen]

It's Cassiopea's own fault, they have wasted enough time.

Cassiopea has the same problem as western countries :

They are resting on their laurels, and meanwhile the emerging powers are taking it all.

 

[el_duterino]

Regarding the patent including PC. This is pretty standard to cover all potential uses for a compound. They also mention it’s potential use as a male contraceptive, although it’s pretty obvious it will never be used for that.

There is no mention of PC in the CB or RU patent. To mention both applications is just a potential hidden red flag for side effects.

 

[FollicleGuardian]

There is no mention of PC in the CB or RU patent. To mention both is just a potential hidden red flag for side effects.

None of those are potent enough for PC, especially CB haha. One of the example compounds of KX-826 tested here has a 0.12 uM IC50, which is insane. Probably plan to use that orally.