Formestane vs Erase

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  1. Quote Originally Posted by Bry17 View Post
    In rat:

    The metabolism of the aromatase inhibitor-4-hydroxyandrostenedione (4-OHA) was studied in vitro and in vivo in the rat. To accomplish this, deuterium- and tritium-labeled 4-OHA were prepared from 4-hydroxyandrosta-4, 6-dione-3,17-dione. The latter was synthesized from 4-androstene-3,17-dione. Using deuterated 4-OHA in in vitro incubations of rat ovarian microsomes, 4-hydroxytesterone (4-OHT) was identified by gas chromatography/mass spectroscopy as the major metabolite. 4-OHT constituted approximately 20% of the total radioactivity from [6,7-3H]-4-OHA in the ovarian microsomal incubations. Conversion of [6,7-3H]-4-OHA to 4-hydroxyesterone was approximately 0.1%. The major metabolite of [6, 7-3H]-4-OHA in vivo identified in the free, neutral fraction of rat blood was 3 beta-hydroxyandrostane-4,17-dione. The metabolite accounted for approximately 5% of the total radio-activity in the blood, Whereas 4-OHT accounted for only 0.1%, 4-OHT inhibited in vitro ovarian aromatization by 59%, but 3 beta-hydroxyandrostane-4-17-dione had little effect. It was concluded that the in vivo effects of 4-OHA previously reported are largely due to its own activity although additional effects of its metabolic products cannot be excluded.

    In human:

    4-Hydroxyandrost-4-ene-3,17-dione is a second generation, irreversible aromatase inhibitor and commonly used as anti breast cancer medication for postmenopausal women. 4-Hydroxytestosterone is advertised as anabolic steroid and does not have any therapeutic indication. Both substances are prohibited in sports by the World Anti-Doping Agency, and, due to a considerable increase of structurally related steroids with anabolic effects offered via the internet, the metabolism of two representative candidates was investigated. Excretion studies were conducted with oral applications of 100mg of 4-hydroxyandrostenedione or 200mg of 4-hydroxytestosterone to healthy male volunteers. Urine samples were analyzed for metabolic products using conventional gas chromatography-mass spectrometry approaches, and the identification of urinary metabolites was based on reference substances, which were synthesized and structurally characterized by nuclear magnetic resonance spectroscopy and high resolution/high accuracy mass spectrometry. Identified phase-I as well as phase-II metabolites were identical for both substances. Regarding phase-I metabolism 4-hydroxyandrostenedione (1) and its reduction products 3beta-hydroxy-5alpha-androstane-4,17-dione (2) and 3alpha-hydroxy-5beta-androstane-4,17-dione (3) were detected. Further reductive conversion led to all possible isomers of 3xi,4xi-dihydroxy-5xi-androstan-17-one (4, 6-11) except 3alpha,4alpha-dihydroxy-5beta-androstan-17-one (5). Out of the 17beta-hydroxylated analogs 4-hydroxytestosterone (18), 3beta,17beta-dihydroxy-5alpha-androstan-4-one (19), 3alpha,17beta-dihydroxy-5beta-androstan-4-one (20), 5alpha-androstane-3beta,4beta,17beta-triol (21), 5alpha-androstane-3alpha,4beta,17beta-triol (26) and 5alpha-androstane-3alpha,4alpha,17beta-triol (28) were identified in the post administration urine specimens. Furthermore 4-hydroxyandrosta-4,6-diene-3,17-dione (29) and 4-hydroxyandrosta-1,4-diene-3,17-dione (30) were determined as oxidation products. Conjugation was diverse and included glucuronidation and sulfatation.

    ^don't see any mention of 4-oht in bolded.
    Thats because you forgot to bold it
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  2. Quote Originally Posted by nattydisaster View Post
    Thats because you forgot to bold it
    nvm. thats right. i thought 4-oht was tested seperate there.
    Antaeus Rep

  3. ok, not identified in rats much, but in humans yes. my mistake.
    Antaeus Rep

  4. I dont really know what the argument is here...formestane may or may not convert to 4-OHT, So what if it does or doesnt? That doesnt change its effects as an AI

    The other claims by Formestane need to be examined by application. For instance I have seen formestane transdermal products claim it will lower SHBG. Studies show that oral formestane lowers SHBG but not injection, which leads me to believe the metabolites are very different when taken through each route and transdermal as well.

    Which makes sense considering how many enzymes are in the skin. Not really any way to know...but transdermal is probably more close to injection that oral...which is why form is supplied this way
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  5. What needs to happen is someone needs to release sterile formestane acetate...
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  6. Quote Originally Posted by Bry17 View Post
    ok, not identified in rats much, but in humans yes. my mistake.
    No worries B1 (i officially approve you as B1 of 3 on the CEL team)
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  7. Erase is strong for an oral, maybe the strongest oral out there. I like both, I think Formestane might have a slight edge when used on cycle but I can't really say that for sure. I thnk Formestane has a greater risk for estro rebound and you need to taper off on dosing... When you take cost into consideration erase is going to be the less expensive choice.

  8. I like both to be honest. I wish I had more Formestane. That said I have a number of Erase bottles so I will be using that for my next stackaholics meeting.

  9. Good ref.
    shows oral forma 125mg once a day is 72% effective. I wouldnt want much more than that

    http://www.ncbi.nlm.nih.gov/pmc/arti...99/table/tbl1/
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  10. Going to go with erase

  11. Comparing apples and oranges in terms of AIs. Form is usually found in a transdermal carrier, and can produce mild anabolic activity. It's estrogen suppression was by far the strongest on the market based on scientific data and blood tests. Saying this, the newerase is a great oral product that effectively reduces estrogen. I wouldd pick the erase because it's oral, it's effective at reducing estrogen, and blood results (mine) prove that it reduces estrogen but does not crush it like form
    Cancer Survivor and Fighter--Chemo round 3 06/2015
  

  
 

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