oh, and these integrase mutations that are currently being produced by raltegravir (at about 25% of pts every 48 wks), are also likely to impact elvitegravir, the next integrase in line http://www.tibotec.com/content/congresses/www.tibotec.com/Goethals_virol_INIs.pdf
and also impact the next integrase in line from GSK S/GSK1349572: E138K/Q148K, 47- to 190-fold resistance S/GSK1349572: G140S/Q148H, 4.8- to 8.0-fold resistance; http://www.natap.org/2009/ICCAC/ICCAC_06.htm
but avexa's new patent integrases are 'surprisingly' effective!
woof!
>>>>thanks mr
in english, i think that means they have found some more very nice integrase inhibitors, that tibotec are about to get their hands on...
"The present inventors have now determined that a sub-class of these compounds are surprisingly effective (when compared to other members of the class) against viral variants containing the Q148H/G140S double mutation in integrase and the N155H/E92Q double mutation in integrase. This sub-class of compounds also shows surprising activity against the triple mutant Q148K/G140A/E138A."
I do like the reference to "surprising"...
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