Kythera Acquires Rights to PGD2 Inhibitor

[heyhowareyou47]

im definitely in for the group buy. i've been lurking for a while, but i have to speak up now. i want in.

 

[BiqqieSmalls]

I received an email response from Kane, he seems to really pushing OC in place of Set. I'm assuming it would cost him some money to develop Set oppose to selling already his prepared OC solution. At least that's what I took from the email response. We should contact a few sites, increase competition, should get us a cheaper price.

Nice going. I think we should go after Set instead of OC though. Could you post his response so we can perhaps dissect it?

 

[kirk]

This is the response I received from Kane.


dear friend,


thanks for your contact.


We discussed with our engineers as to investigate this research chemical. its very similar chemical structure to OC000459, however less potent for research purpose. OC000459-ethanol its Superior to Setipiprant.




1).this research chemical won't dissolve in ethanol, its developed for oral consumption it'll dissolve in acidic stomach as looking to the chemical structure "ACT-129968, 2-(2-(1-naphthoyl)-8-fluoro-3,4-
dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid"


2).Setipiprant its about 250% less potent as Its competitor OC000459. 1 gram vs 400MG pls see literature below.


3). its production price estimated to equal OC000459 we'll confirm after our Chinese holiday once we're back in office 27-feb. Custom production is very expensive. its not economical at small quantities.




Setipiprant

source- http://download.springer.com/static...998_8da2e34a144aa22767476426b3b767c7&ext=.pdf


Setipiprant (ACT-129968, 2-(2-(1-naphthoyl)-8-fluoro-3,4-
dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid)
1. it does not dissolve in ethanol.
2. Higher doses required for your labatory research purpose
Preclinical data showed that setipiprant potently inhibits
migration of eosinophils towards PGD2 in vitro as well as
in an in vivo rat model of lung eosinophilia (Actelion
Pharmaceuticals Ltd, data on file). In the entry-into-man
study in healthy male subjects, single and multiple doses of
setipiprant of up to 1,000 mg twice daily (bid) for 6 days
showed excellent tolerability and a favorable pharmacokinetic
profile (Sidharta et al., unpublished data)
All subjects received a single dose of 1,000 mg setipiprant administered as four capsules of 250 mg



OC000459
Source- http://www.ersj.org.uk/content/41/1/46.full
The limited pharmacokinetic analysis performed in this study showed stable levels of plasma drug concentrations at 12 h post-dose after 7 and 14 days’ dosing. These data indicate adequate systemic exposure to OC000459 using a dosing regimen of 200 mg twice daily. The mean inhibitory concentration (IC50) of OC00459 for inhibition of PGD2-mediated activation of eosinophils in human whole blood is 35 ng·mL−1 (personal communication) and so the plasma levels of drug achieved in this study were well in excess of this level. We also showed that the systemic exposure caused functional antagonism of blood eosinophils ex vivo using a well established eosinophil shape change assa

 

[Hairismylife]

I think they are just pushing us to buy the OC.

 

[KiNGTyreZe]

I think they are just pushing us to buy the OC.

I like the oral consumption more though.

This is so expensive. If we have to use 200 mg twice daily then this will just hold for 2.5 days lol.

 

[Hairismylife]

I like the oral consumption more though.

This is so expensive. If we have to use 200 mg twice daily then this will just hold for 2.5 days lol.

Too expensive. Must consider only topical to use minimum locally.

 

[psyhotria]

Basically Kane told you. Setip. will not be a miracle drug. If you want to assess its postential, you can use OC now. However, if Setip. cannot be used locally it will likely perform worse than OC. Also keep in mind that PGD2 is downstream of 5-ar and AR, so, if you already use 5-ar inhibitors or androgen receptor antagonists or (preferably) both concurrently, PGD2 antagonists may have no (or no big) additional effect. But possibly one can substitute PGD2 antagonists for 5-ar/AR inhibitors/antagonists, if it makes sense that is, if there's less (less severe) systemic side effects. Or at least that Setip. will be cheaper than OC, but I doubt that Kythera will sell it for cheap, if they bring it to market anyway.

 

[Dikek]

We should contact cotsarelis and ask the truth, or the pharma they need to motivate and def their investment i'm curious what they say about the potential cure

 

[Hairismylife]

Basically Kane told you. Setip. will not be a miracle drug. If you want to assess its postential, you can use OC now. However, if Setip. cannot be used locally it will likely perform worse than OC. Also keep in mind that PGD2 is downstream of 5-ar and AR, so, if you already use 5-ar inhibitors or androgen receptor antagonists or (preferably) both concurrently, PGD2 antagonists may have no (or no big) additional effect. But possibly one can substitute PGD2 antagonists for 5-ar/AR inhibitors/antagonists, if it makes sense that is, if there's less (less severe) systemic side effects. Or at least that Setip. will be cheaper than OC, but I doubt that Kythera will sell it for cheap, if they bring it to market anyway.

Maybe think in this way: antiandrogen is a first guard, Set is a second guard. So it should have some, if not big, additional effect. If you have enough guard in two gates, hairloss should be completely halted.
If antiandrogen cause too much sides, we can just decrease its dose and increase Set.
But still, we nay need growth agent for regrowth. So I always pray for Bim.

 

[kirk]

I guess we wont know for sure til we buy and try. Anyways that's what this forum is famous for. lol!

 

[bilboswaggins]

We should contact cotsarelis and ask the truth, or the pharma they need to motivate and def their investment i'm curious what they say about the potential cure

yep because cotsarelis and his crew are so sympathetic to the plight of balding men that they will jeopardise their profits so that we dont pointlessly raise our hopes for this product. Let's not kid ourselves. Even if setipirant does jack squat, they will try to milk as much out of it as they can before consumers realise it has efficacy comparable to snake oil. I'm really hoping this is not the case

 

[Dikek]

I agree with you but a basic question like what's the difference between competitor product like oc and seti in term of cosmetic expectations is the key, he cannot just tell us a bunch of bull****, we will notice it

Anyway we dont really know what oc does to our hairs. We need something like 2k dollars for some weeks of real treatment lol

 

[BiqqieSmalls]

I think they are just pushing us to buy the OC.

Yep, it sounds like it and I don't appreciate it.

 

[Parsia]

Yep, it sounds like it and I don't appreciate it.

I don't like the idea either , We asked to buy Seti not OC , from which evidence or study they say OC is much more effective? Doesn't make sense at all.

Lets don't waste the money for them.

 

[hellouser]

If Kane doesnt supply Setipiprant that is also LEGIT, we'll need to find another reliable/trusted supplier.

 

[Helios]

Is there no Heisenberg amongst us?

 

[BiqqieSmalls]

The following are a couple options:
1) http://www.keyorganics.net/bionet/setipiprant-mfcd23136043-c24h19fn2o3-1.html .. This is a trusted site when confirming with ScamAdvisor.com
2) https://www.molport.com/shop/moleculelink/IHAXLPDVOWLUOS-UHFFFAOYSA-N/35395269 .. This is a bit more expensive than the first link and is also a trusted site.

I don't think we should go with OC from Kane. Can someone contact the people from these two websites to ask about buying a large quantity?

 

[hellouser]

The following are a couple options:
1) http://www.keyorganics.net/bionet/setipiprant-mfcd23136043-c24h19fn2o3-1.html .. This is a trusted site when confirming with ScamAdvisor.com
2) https://www.molport.com/shop/moleculelink/IHAXLPDVOWLUOS-UHFFFAOYSA-N/35395269 .. This is a bit more expensive than the first link and is also a trusted site.

I don't think we should go with OC from Kane. Can someone contact the people from these two websites to ask about buying a large quantity?

Anyone who does so, cannot just ask randomly as a 'joe schmoe' it needs to look like the inquirer is part of a lab or something that wont get hassled with questions as to WHY we want it.

 

[BiqqieSmalls]

Anyone who does so, cannot just ask randomly as a 'joe schmoe' it needs to look like the inquirer is part of a lab or something that wont get hassled with questions as to WHY we want it.

Hmm, if I provided you the contact details for the above sites, could you contact them, as you seem to have a good idea on how to handle this?

 

[Avacfc]

I have just tried to order with the key organics site and got right through to payment without them asking for any information on why i need this drug.

Theres nothing stopping us buying straight from this site as a guest from what i can see plus its not a bad price.