Integrase inhibitors: first clear success in human trial.
HIV uses at least three enzymes to reproduce--reverse transcriptase, protease, and integrase. These enzymes are obvious targets for designing anti-HIV drugs that block them (but enzymes are certainly not the only targets; there are many more steps in the HIV life cycle that drugs might attack). AZT and many other approved drugs block reverse transcriptase. Protease inhibitors came into use around 1996 and revolutionized AIDS treatment (although highly effective HAART combinations without protease inhibitors are also possible). Integrase inhibitors have been the hardest to develop, partly because different protease inhibitors were already used in other areas of medicine, while anti-HIV integrase inhibitors had to be developed from scratch. An earlier integrase inhibitor, S-1360, developed by Shionogi & Co. and GlaxoSmithKline, had to be discontinued because of poor bioavailability.
The new Merck trial clearly shows that an integrase inhibitor can work in people to lower HIV viral load.
For More Information
Information about this drug will change rapidly, and we do not know which Web or other information will be best. You might check first with the treatment-information sources you already use.
For general news you might try http://news.google.com/--search for "integrase" (quotation marks not necessary). Or for more focus on AIDS-related news, try http://www.aegis.org/search/--"integrase" returns hundreds of articles, mostly very technical, so try "MK-0518" (or any newer drug name that Merck may use in the future).
(1.) Morales-Ramirez J.O., Teppler H., Kovacs C., and others, Protocol 004 Team (USA, Canada, Australia). Antiretroviral effect of MK-0518, a novel HIV-1 integrase inhibitor, in ART-naive HIV-1 infected patients. 10th European AIDS Conference / EACS, November 17-20, 2005, Dublin, Ireland [abstract # LBPS1/6].
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|Author:||James, John S.|
|Publication:||AIDS Treatment News|
|Date:||Oct 1, 2005|
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