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Pfizer\'s "RU58841" being researched......?


#1

Someone posted this someplace else, but I thought some of you might be interested in this:

Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.J Med Chem. 2008 Nov 13;51(21):7010-4. Epub 2008 Oct 16.

Li JJ, Iula DM, Nguyen MN, Hu LY, Dettling D, Johnson TR, Du DY, Shanmugasundaram V, Van Camp JA, Wang Z, Harter WG, Yue WS, Boys ML, Wade KJ, Drummond EM, Samas BM, Lefker BA, Hoge GS, Lovdahl MJ, Asbill J, Carroll M, Meade MA, Ciotti SM, Krieger-Burke T.

Department of Chemistry, Michigan Laboratories, Pfizer Global Research & Development, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA.

4-((1 R,2 R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile [PF-0998425, (-)- 6a] is a novel, nonsteroidal androgen receptor antagonist for sebum control and treatment of androgenetic alopecia. It is potent, selective, and active in vivo. The compound is rapidly metabolized systemically, thereby reducing the risk of unwanted systemic side effects due to its primary pharmacology. (-)- 6a was tested negative in the 3T3 NRU assay, validating our rationale that reduction of conjugation might reduce potential phototoxicity.

PMID: 18921992


#2

I’d love to see it come to market.

But I think it would still be basically a disappointment compared to its hype. Even the guys who start out raving about it, they all still seem to report it lost a lot of effectiveness within a year or two.

(“Bad batch” this, “unstable storage” that, whatever. Regardless of the details of each story, the real BOTTOM LINE never changes - nobody ever gets RU to keep working in the long term.)

These stories, taken along with the complaints about Fin lose effectiveness after 4-7 years . . . I think maybe it all points to a limit to how much lifetime-total hair protection we can ever get from androgen suppression in any form.

It’s almost as if our follicles have a built-in limit to how much they’ll withstand (before mutating to get stimulation from other hormones?), and RU58841 is just a faster way to max-out the gains from androgen suppression. It gives the gains in a year or two that Fin would spread out over half a decade, and then its potential to help your hair has been mostly exhausted just like with longer-term Fin.

Once an area of our scalp has been sensitized to DHT, we need real hair multiplication to fix things. Anything else is just putting off the problem temporarily IHMO.


#3

there is someone selling what seems to be an RU topical…Would love to see all of your opinions…

http://www.androvex.com

he says its stable due to the ingrediants…whats the concensus


#4

» there is someone selling what seems to be an RU
» topical…Would love to see all of your opinions…
»
» http://www.androvex.com
»
» he says its stable due to the ingrediants…whats the concensus

Nice find,good question,come on someone - advice wanted!


#5

» » there is someone selling what seems to be an RU
» » topical…Would love to see all of your opinions…
» »
» » http://www.androvex.com
» »
» » he says its stable due to the ingrediants…whats the concensus
»
» Nice find,good question,come on someone - advice wanted!

Nice to see you back in the HM section. I thought you gave up on us quote/unquote “dreamers”.


#6

» » » there is someone selling what seems to be an RU
» » » topical…Would love to see all of your opinions…
» » »
» » » http://www.androvex.com
» » »
» » » he says its stable due to the ingrediants…whats the concensus
» »
» » Nice find,good question,come on someone - advice wanted!
»
» Nice to see you back in the HM section. I thought you gave up on us
» quote/unquote “dreamers”.

Sorry,yes I did say that,but at same time I still check hairsite several times a week,I have just got no real input anymore.We never know Intercytex might still come up with the goods

I must be in a dreaming hoping mood today.I’ve not shaved my head for a few days.I’m letting it grow out for a few more days,just to see if I have gained or not,since using spectral dmc-l.I know I gained a little,but not sure how much yet,until its grown out a little bit more.

My big dream is to have a proper hairline (What a dream,haha).

Anyway the question is still wanting an answer “Androvex = RU58841?..advise required”.


#7

blahblah - I’ve posted this Androvex = RU58841 question over on the Topicals forum.We might get a better responce on the right forum


#8

» blahblah - I’ve posted this Androvex = RU58841 question over on the
» Topicals forum.We might get a better responce on the right forum

Well, one person posting about Androvex seems to have been exposed as a scammer. I don’t know if its true, of course, but some valid points were raised in that thread:

  1. Their website is allegedly behind a proxy.
  2. Their address was allegedly registered a week ago even though they claim to have been around for years.
  3. The moderator there says he has received information that someone is registering multiple accounts on various hairloss realted sites and posting questions to himself about Androvex.

Needless to say, I haven’t verified anything, I’m just relaying the information.

/p


#9

In their “results” section, Patient A looks somewhat familiar - it looks like the results posted from clinical trials on either Dutasteride or Fina.

It is also funny to note that, according to their “timeline”, patients will experience an “uproar” of regrowth at 6 to 12 months.:smiley:


#10

» » blahblah - I’ve posted this Androvex = RU58841 question over on the
» » Topicals forum.We might get a better responce on the right forum
»
» Well, one person posting about Androvex seems to have been exposed as a
» scammer. I don’t know if its true, of course, but some valid points were
» raised in that thread:
»
» 1. Their website is allegedly behind a proxy.
» 2. Their address was allegedly registered a week ago even though they
» claim to have been around for years.
» 3. The moderator there says he has received information that someone is
» registering multiple accounts on various hairloss realted sites and posting
» questions to himself about Androvex.
»
» Needless to say, I haven’t verified anything, I’m just relaying the
» information.
»
» /p

that is started by maneless under a different name, stay away from ru scam.


#11

» In their “results” section, Patient A looks somewhat familiar - it looks
» like the results posted from clinical trials on either Dutasteride or
» Fina.
»
» It is also funny to note that, according to their “timeline”, patients
» will experience an “uproar” of regrowth at 6 to 12 months.:smiley:

those result pictures made it seem too good to be true…were those really from the dutas/fin trials? because ive never seen such good regrowth.

man, i was so happy when i first saw that posted, i felt like a cloud was lifted especially after seeing the results page. That was one of the better scams ive seen posted. :frowning:


#12

» It’s almost as if our follicles have a built-in limit to how much they’ll
» withstand (before mutating to get stimulation from other hormones?),
and
» RU58841 is just a faster way to max-out the gains from androgen
» suppression. It gives the gains in a year or two that Fin would spread out
» over half a decade, and then its potential to help your hair has been
» mostly exhausted just like with longer-term Fin.

I read in research study(I think the one about ASCJ-9) that overtime genetic mutation occurs and that is the reason why current anti-androgens loose their effectiveness after few years. I just can’t find any info about curcumin, I’m planning on using daily curcumin supplement as an anti-androgen - hopefully, the body won’t mutate and adopt to it?


#13

I’m also hoping that about the androgen receptors, that they won’t mutate or whatever and find a way around the lack of androgens.

It makes sense to me at least in theory.

The body devised a method of fighting the fluctuating hormone levels because that fluctuation is a natural normal occurrence. So the body uses androgen receptors that can change sensitivity to fit the situation.

But the body never devised a way (that I know of) to compensate for the androgen receptors themselves being influenced by external methods. I see no natural reason that the body would have ever originally needed to devise anything along those lines. I don’t know of any natural life factors that would be artificially suppressing the AR activity like what we’re talking about doing. I really don’t see how the body’s hormone system & hair follicles would even know what was happening. The ARs are the body’s actual “sensors” for androgen stimulation as I understand it.


#14

» » It’s almost as if our follicles have a built-in limit to
» how much they’ll
» » withstand (before mutating to get stimulation from other hormones?),
»
and
» » RU58841 is just a faster way to max-out the gains from androgen
» » suppression. It gives the gains in a year or two that Fin would spread
» out
» » over half a decade, and then its potential to help your hair has been
» » mostly exhausted just like with longer-term Fin.
»
»
» I read in research study(I think the one about ASCJ-9) that overtime
» genetic mutation occurs and that is the reason why current anti-androgens
» loose their effectiveness after few years. I just can’t find any info about
» curcumin, I’m planning on using daily curcumin supplement as an
» anti-androgen - hopefully, the body won’t mutate and adopt to it?

First , we are not talking about something live like Bacterias , some guys think that all the meds have the same problem that the antibiotics ( Bacterias overtime genetic mutation ) .
Secon , is really a overtime genetic mutation occurs , and if this conver the antiandrogen lets potente cause it could not be added to the androgen receptor , that will also happen with the DHT or the testosterone cause the antiandrogen is simple a molecule similar to dht or testosterone with more affinity that this ones and that is why the antiandrogen accept it ! .
This thing , simple , do not happen .