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Integrase Inhibitor
Mar 30, 2005

Dr. Young, I am very interested to hear your thoughts on Integrase Inhibitors. -Do you think they will be successful in developing one? -Do you think it can be potentially used as a monotherapy? -Generally what are your thoughts?

Response from Dr. Young

Thanks for your questions.

Inhibitors of HIV integrase have been under investigation for some time, though none are currently in advanced clinical trials. There have been a couple of aborted candidate compounds, one from Merck, another from GSK-Shionogi. Neither of these compounds had the needed characteristics to develop further.

Will we eventually see an integrase inhibitor? I'd like to think so, but it's far too early to tell. As for monotherapy, I don't think that this will be the case (but I could be wrong), since the integrase protein is encoded on the same highly mutable HIV genome as other HIV drug targets.

Integrase is an attractive target since prevention of viral genome integration into the human genome might limit the number of CD4 cells that become chronically infected and because any new class of medications offers renewed hope for viral suppression for those who have highly drug resistant virus.

Thanks for reading. BY



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