The evolution of HIV-1 IN strand transfer inhibitors has been one of the most significant advances in the field of HIV/AIDS chemotherapy over the past decade. The progression of scaffold designs from early DKAs to heterocyclic replacements and eventually into clinical candidates that are beginning to deliver benefit for patients is a tribute to the many researchers that appear in the accompanying citations. While the accomplishment of the first INIs has been monumental, it would be naïve to think that the field is complete and no more can be done to improve patient's lives. The emergence of IN resistance has already begun and the need for convenient dosing regimens and tolerable next generation inhibitors cannot be overstated. It appears that the field is again poised to raise the bar to a new level with exciting data for investigational drugs such as S/GSK1349572 and possibly others yet to come.
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