antibioticsbooks

Integrase Inhibitors
Agents: raltegravir (RAL)
Combinations: elvitegravir (EVG)/cobicistat/
emtricitabine/tenofovir (Stribild)
A new and promising class of antiretrovirals is the
integrase inhibitors (often abbreviated as INSTI
for integrase strand transfer inhibitors). Their novel
mechanism of action provides a new option for
treatment-experienced patients. For treatmentnaïve
patients, raltegravir is appealing for its good
tolerability and limited drug interactions, while
the newest agent elvitegravir is available as part of
a once-daily combination pill.
Mechanism of Action
After the HIV reverse transcriptase enzyme creates
a strand of viral DNA, a viral protein called
integrase facilitates the transfer of the HIV DNA
into the host cell’s genome. The INSTIs inhibit this
enzyme, preventing the viral DNA from becoming
a part of the host cell enzyme, an important step in
HIV replication.
Spectrum
Only current clinical use is for HIV.
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