Raltegravir (Isentress – Merck), the first in a new class of oral HIV drugs called HIV-1 integrase strand transfer inhibitors (InSTI), has received accelerated FDA approval for use in combination therapy for treatment- experienced adults infected with HIV-1 strains resistant to multiple antiretroviral agents.1

Maraviroc (Selzentry – Pfizer), the first CCR5 (CC chemokine receptor 5) antagonist has received the same FDA approval but is restricted to use in adults with CCR5-tropic HIV-1 (“R5 virus”). A commercial assay is available for R5 tropism.

MECHANISM OF ACTION — HIV-1 integrase catalyzes the process that results in viral DNA insertion into the host cell genome. Raltegravir inhibits the enzyme’s activity, preventing viral DNA from integrating with cellular DNA. It is active against HIV strains resistant to ... more      

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