Integrase inhibitors on trial

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Two HIV integrase inhibitors - one developed by Merck and one in a joint venture between Japanese firm Shionogi and GlaxoSmithKline (GSK) - are entering trials in human volunteers.
HIV is currently controlled by a combination of three or four of 16 approved antiretrovirals - which block the enzymes protease and reverse transcriptase. Now, drugs will soon be able to inhibit HIV's third enzyme - integrase.
Integrase inhibitors are particularly attractive because they can block an additional step in the HIV life cycle - the integration of the virus's DNA into the cell's chromosome.
Finding a molecule that successfully prevents integration would prevent HIV from infecting a host cell.
"It's been a difficult target," said Dr Daria Hazuda, Executive Director of Biological Chemistry at Merck. "You're starting completely from scratch."

HIV integrase: new drug target

Merck initially presented their findings at the Barcelona International Aids Conference. A total of six monkeys received the experimental drug L-870-812 as monotherapy for 75 days. Four of the monkeys had undetectable viral loads at the end of the treatment - and the other two who did not receive the optimal dose, still did not become ill.
It is hoped that the compound will be active against multi-drug resistant virus exposed to all currently available classes of antiretrovirals, and that it will be less prone to resistance than other classes.