Darolutamide (odm-201), A Better Topical Than Enzalutamide? | HairLossTalk Forums

Darolutamide (odm-201), A Better Topical Than Enzalutamide?

Discussion in 'Antiandrogens - Propecia, Dutasteride, etc.' started by JLF, May 4, 2017.

  1. JLF

    JLF Established Member My Regimen

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    After reading a lot of thread on different forums, a few testimonials from certain persons pop out.
    I'm referring to Swiss Temples and his PG protocol for instance.
    But last i stumbled upon the story of Xandrus on baldtruthtaIk.
    He used topical MDV3100, also known as Enzalutamide or Xtandi.

    This substance has a very long half-life.
    As far as I have read, this is supposed to be a bad thing.
    It can go systemic and continue working for days on places you don't want it having working. (correct me if I'm wrong)
    The substance can also cross the blood-brain barrier.

    Then I came across Darolutamide (ODM-201).
    It works very similar to Enzalutamide but has a shorter half-life.
    It also (almost) doesn't cross the blood-brain barrier.

    It seems that this would be a better topical than Enzalutamide.
    I'm not a scientist nor a chemist so please share your knowledge if you are.
    Any thoughts?
     
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  2. whatevr

    whatevr Senior Member My Regimen

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    We have a thread on enzalutamide here:
    https://www.hairlosstalk.com/intera...mide-superstrong-antiandrogen-topical.105093/

    MDV-3100 seems to have some unique mechanisms of action though:
    http://www.avacor.com/blog/hair-regrowth/the-future-of-hair-regrowth-part-2-–-next-generation-ar-antagonists/
    It acts in three different ways upon the AR which makes it extremely powerful.
    I don't know if ODM-201 shares all of those properties.

    Also, good luck getting ODM-201 anywhere. They don't even sell that on Alibaba yet.
     
    #2 whatevr, May 4, 2017
    Last edited: May 4, 2017
  3. JLF

    JLF Established Member My Regimen

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    Hi whatevr

    Yeah I've read that thread and saw the info on avacor indeed but didnt want to go off-topic.
    Thanks for adding the links.
    I thought it would be good to start a new discussion about ODM-201.
    It is for sale on Alibaba, I have a few suppliers but it's more expensive than Enza due to them not producing large quantities.
    If someone has some more insights about ODM, it would make things clearer if this extra cost is worth it compared to Enza.
    Enza isn't that expensive considering how little you need imo.

    Thanks!
     
    #3 JLF, May 4, 2017
    Last edited: May 4, 2017
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  4. JLF

    JLF Established Member My Regimen

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    more info here:
    ncbi.nlm.nih.gov/pmc/articles/PMC4490394/
     
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  5. JLF

    JLF Established Member My Regimen

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    here is Xandrus his (short) story by the way...
    baldtruthtaIk.com/threads/23023-My-treatment-works-only-RU58841-5-10-and-MDV3100-2
     
  6. kawnshawn

    kawnshawn Established Member

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    If you're going to buy it off Alibaba make sure you do ALOT of research from the company you're buying it from and try to get it tested. A lot of these company's are extremely shady and you never know what you are getting. My general rule of thumb is that if the rep can't type in proper English then find another source.
    Currently trying to buy enza off alibaba
     
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  7. whatevr

    whatevr Senior Member My Regimen

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    Please let us know if you find a reliable source, I'd be interested in attempting to obtain some of this stuff somewhere down the line.
     
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  8. JLF

    JLF Established Member My Regimen

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    Thanks for the warning.
    I was indeed planning on having it tested.

    How do you think penetration would be of ODM-201?
    The molar mass is 398.84616 g/mol according to wikipedia.
     
  9. whatevr

    whatevr Senior Member My Regimen

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    Under 500 dalton I think even just Ethanol + PG do the job fine.
    Xandrus used:

    Alcohol 40-45 %
    methylidene glycerol 35%
    destillated water 25%

    I think maybe 96% ethanol, some isopropanol and PG would probably be more than good enough. But I'm no chemist.
     
  10. Dench57

    Dench57 Senior Member My Regimen

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    maybe in a few years. way too expensive atm
     
  11. JLF

    JLF Established Member My Regimen

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    yeah... I found $350 / g
    question is a of course how much do you need
    because of the shorter half-life, you will need more than enzalutamide
     
  12. whatevr

    whatevr Senior Member My Regimen

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    Rather try enzalutamide if you want to mess with these types of things. Won't be a while until we can get ODM-201 reasonably.
     
  13. kawnshawn

    kawnshawn Established Member

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    Pretty sure I found a good source but I'll know for sure in a few weeks. I'll make sure to post lab results.
     
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  14. chusler

    chusler New Member

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    mdv-3100 is powerfull and i know that it will work (a bit risky even topical), but odm-201 can be a real cure with a right topical vehichle :

    Taken from: https://newdrugapprovals.org/2016/03/12/odm-201/

    “ODM-201 is a new-generation, potent and selective androgen receptor (AR) inhibitor which is potential useful for treatment of castration-resistant prostate cancer (CRPC). ODM-201 is a full and high-affinity AR antagonist that, similar to second-generation antiandrogens enzalutamide and ARN-509, inhibits testosterone-induced nuclear translocation of AR. Importantly, ODM-201 also blocks the activity of the tested mutant ARs arising in response to antiandrogen therapies, including the F876L mutation that confers resistance to enzalutamide and ARN-509. In addition, ODM-201 reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model. ODM-201 overcomes resistance to AR-targeted therapies by antagonizing both overexpressed and mutated ARs. ODM-201 is currently in a phase 3 trial in CRPC”



    Relative to enzalutamide (MDV3100 or Xtandi) and apalutamide (ARN-509), two other recent non-steroidal antiandrogens, ODM-201 shows some advantages.

    [3] ODM-201 appears to negligibly cross the blood-brain-barrier.[3] This is beneficial due to the reduced risk of seizures and other central side effects from off-target GABAA receptor inhibition that tends to occur in non-steroidal antiandrogens that are structurally similar to enzalutamide.[3]

    Moreover, in accordance with its lack of central penetration, ODM-201 does not seem to increase testosterone levels in mice or humans, unlike other non-steroidal antiandrogens.[3]

    Another advantage is that ODM-201 has been found to block the activity of all tested/well-known mutant ARs in prostate cancer, including the recently-identified clinically-relevant F876L mutation that produces resistance to enzalutamide and ARN-509.[3] Finally, ODM-201 shows higher affinity and inhibitory efficacy at the AR (Ki = 11 nM relative to 86 nM for enzalutamide and 93 nM for ARN-509; IC50 = 26 nM relative to 219 nM for enzalutamide and 200 nM for ARN-509) and greater potency/efficaciousness in non-clinical models of prostate cancer.
     
    #14 chusler, Jul 12, 2017
    Last edited: Jul 12, 2017
  15. chusler

    chusler New Member

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    i read Fgf-11' s(his firs nickname was : god) comments on hairloscure2020 last year, This dude is right , i believe in his theory, it really makes sense for me. Please read his theory here, even you read it b4. There are xyz123's comments too which are so important to understand fgf-11's theory.

    he also is talkin about odm-201 and mdv3100 when he explains his theory

    The link: https://www.baldtruthtaIk.com/threads/22187-I-think-I-ve-hacked-it

    Thanks to Fgf-11, whatevr, xandurus and JlF...
     
    #15 chusler, Jul 12, 2017
    Last edited: Jul 12, 2017
  16. Kevand

    Kevand Established Member

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    I believe the increase of testosterone is a good thing to compensate for the systemic anti-androgenetic exposure. Another concern with this compound if wiki is right its a pro-drug, which means it needs to be converted probably in liver to be fully active. However darolutamide as a substance on its own could be comparable to enzalutamide.
     
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  17. Kevand

    Kevand Established Member

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    I wonder if they specifically mean ODM-201 with the results or if it also concerns it's main active metabolite.
     
  18. whatevr

    whatevr Senior Member My Regimen

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    Yes, it's a shame he was chased away by the illiterate brain-dead retards at BTT with their "omg snake oil give us the cure" mentality.
    His post is like a glimpse into the future. The things he writes about will be common in 30 years, and he experimented with them right now.
    Everything he wrote makes sense and is very interesting, far ahead of its time, actually. No wonder it went over everyone's head.
     
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  19. chusler

    chusler New Member

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    Oncology Meeting Innovations(Omi)
    Next-generation anti-androgen therapy: ARN-509 and ODM-201 - Emmanuel Antonarakis


    Link:

    at 13:35 odm-201 toxicity and side effects , odm-201 ' s safety is amazing.
     
  20. Ramsey

    Ramsey New Member My Regimen

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    I've been following the enzalutamide thread, very interesting to read through it.

    I'm curious, did anyone follow up on darolutamide? In comparison to enzalutamide, it seems that it's hard to buy, expensive, and at least the source I found seems dodgy so I'd also test it for sure (and it's not like enzalutamide is so easy to buy either). But I've been thinking about the darolutamide. I like that it only shows "negligible brain penetrance"; maybe would make it better for long-term, higher-dose use than enzalutamide?
     
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