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Thread: exemestane

  1. #1

    exemestane

    i've been reading about the anti E exemestane.
    now it says that exemestane is an irreversible, steroidal aromatase inactivator.
    now what do thay mean by "irreversable". does that mean that it will permanantly bind to the aromatase enzyme or forever stop the conversion of estrogens.
    and if that is true wouldn't that be unhealthy since you want all your hormones/enzymes to return to their natural state/balance after a cycle?

  2. #2
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    Quote Originally Posted by bgrisbtr
    i've been reading about the anti E exemestane.
    now it says that exemestane is an irreversible, steroidal aromatase inactivator.
    now what do thay mean by "irreversable". does that mean that it will permanantly bind to the aromatase enzyme or forever stop the conversion of estrogens.
    and if that is true wouldn't that be unhealthy since you want all your hormones/enzymes to return to their natural state/balance after a cycle?
    No, it is not permanent after discontinuation. It's structurally related to the natural substrate androstenedione, which acts as a false substrate for the aromatase enzyme. It is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as “suicide inhibition.”

    So it's mechanism of action is irreversible, but it does not permanently inactivate binding affinity

  3. #3
    so would you recomend this product over arimidex or femera, and could you take nolva while taking exemestane or there is no need?

  4. #4
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    Their should not be a need for Nolva alongside Aromasin(the brand name)

    The whole purpose of using Nolva alongside L-dex, is to get some SERM benefits to HDL. Aromasin, being an inactivator, as opposed to an inhibitor, should not have the adverse effects on cholesterol that inhibitors possibly do.

    I have seen one study that showed lipid negatives with exemestane, but other variables could of played a role.

    Using Nolva wouldn't hurt, but it's not the neccessity, like with L-dex

  5. #5
    thanks for your reply but can u explain what do you mean by lipid negatives. i have no clue what that means.

  6. #6
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    Aromatase inhibitors can possibly lower HDL(good cholesterol). SERMs such as Nolva mimick bone and liver estrogen, which can help in alleviating this effect

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