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Re: Effexor metabolite in Phase III testing

Posted by djmmm on July 12, 2003, at 16:12:18

In reply to Re: Effexor metabolite in Phase III testing, posted by SLS on July 10, 2003, at 16:16:16

> > I think they singled out the O-desmethylvenlafaxine metabolite because the N-desmethyl and N,O,-didesmethyl metabolites are less active (not as potent) as the parent drug
> Do you know if the ratio of potency for 5-HT versus NE reuptake inhibition is closer to 1:1?
> - Scott

Not likely...since the active metabolite version is only slightly (if you can even call it slightly) more potent than the parent drug..I think I read it's like .3 times as potent (Yes, that's POINT 3)....I don't know how that number would reflect any improvement over the partent drug....I think it has more to do with the extended half life then anything else. But who knows. I think were are only seeing this med because of duloxetine (which is more potent, and has a closer 5-ht/NE ratio)




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