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njmuscleguy
New member
Hey, I don't mean to hijack, but I was just reading a brief on patentstorm.com and saw this about 5-methyl-7-methoxy isoflavone (one of the major components of phyto-test)...
Eric, any thoughts on this to put our minds at ease?
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However, the effectiveness of the prodrug 5-methyl-7-methoxy isoflavone has been limited due to difficulties that the human body encounters in converting the prodrug to its parent isoflavone in vivo. In some instances, its conversion into the desired parent compound, 7-hydroxy-5-methyl-isoflavone, is limited, for example, because it is removed from the system through the "first pass effect," wherein the compound is metabolized by the liver prior to reaching general circulation. A large proportion of the prodrug also either does not undergo conversion or converts into undesirable products. It is estimated that approximately 50% of the prodrug 5-methyl-7-methoxy isoflavone administered to a human is converted in vivo to 7-hydroxy-5-methyl-isoflavone. Even where the desired bioconversion occurs, the rate of conversion can be sufficiently low that undesirably large quantities of the prodrug must be taken to achieve desired effects. This itself can have undesirable side effects.
It is advantageous in many instances to have a prodrug that may be administered in a convenient form, such as by oral, or sublingual administration. Many prodrugs have not been amenable to such administration, however, because they tend to be broken down prior to absorption in vivo when administered in this fashion.
Eric, any thoughts on this to put our minds at ease?
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However, the effectiveness of the prodrug 5-methyl-7-methoxy isoflavone has been limited due to difficulties that the human body encounters in converting the prodrug to its parent isoflavone in vivo. In some instances, its conversion into the desired parent compound, 7-hydroxy-5-methyl-isoflavone, is limited, for example, because it is removed from the system through the "first pass effect," wherein the compound is metabolized by the liver prior to reaching general circulation. A large proportion of the prodrug also either does not undergo conversion or converts into undesirable products. It is estimated that approximately 50% of the prodrug 5-methyl-7-methoxy isoflavone administered to a human is converted in vivo to 7-hydroxy-5-methyl-isoflavone. Even where the desired bioconversion occurs, the rate of conversion can be sufficiently low that undesirably large quantities of the prodrug must be taken to achieve desired effects. This itself can have undesirable side effects.
It is advantageous in many instances to have a prodrug that may be administered in a convenient form, such as by oral, or sublingual administration. Many prodrugs have not been amenable to such administration, however, because they tend to be broken down prior to absorption in vivo when administered in this fashion.
