Integrase strand transfer inhibitor

What are Integrase strand transfer inhibitor?

Integrase strand transfer inhibitors block the action of integrase, a viral enzyme of the human immunodeficiency virus Type 1 (HIV-1), that is involved in integrating viral DNA into the host chromosome. Integration of the viral DNA into the host DNA is necessary for viral replication. Integrase strand transfer inhibitors is not a cure for HIV or AIDS but is used to prevent human immunodeficiency virus from multiplying in the host.

Integrase (IN) strand transfer inhibitors (INSTIs) are recent compounds in the antiretroviral arsenal used against HIV. INSTIs work by blocking retroviral integration, an essential step in the viral lifecycle that is catalyzed by the virally encoded IN protein within a nucleoprotein assembly called an intasome.

Four oral integrase strand transfer inhibitors (INSTIs)—bictegravir (BIC), dolutegravir (DTG), elvitegravir (EVG), and raltegravir (RAL)—are approved for use in people with HIV as their initial ARV treatment.

Integrase inhibitors are a new class of ARVs that prevent this process from occurring, which in turn prevents viral replication. The drawback with integrase inhibitors as microbicides is that their mechanism of action occurs after transcription of the viral RNA, which is relatively late in the life cycle.