Integrase strand transfer inhibitors (INSTIs) belong to a novel class of antiretroviral agents that have
emerged as the new first-line treatments. Three such compounds are currently available, raltegravir, elvitegravir,
dolutegravir and two more under development, bictegravir and cabotegravir. These compounds share the same
mode of action but exhibit different pharmacokinetic/ pharmacodynamic properties, and drug-drug interactions. A
series of studies in the past decade have established their efficacy compared to previous regimens, both in treatment-
naïve and experienced patients. INSTIs have demonstrated a favorable safety profile with fewer adverse
events and low rates of virological failure. Emergence of resistance to these agents, however, is a worrying concern,
particularly for elvitegravir and raltegravir that display a lower genetic barrier than dolutegravir. On-going
trials aim at establishing INSTIs as part of dual-drug HIV treatments or even monotherapy. New long-acting,
injectable formulations are under investigation for treatment or prevention.
Keywords: Integrase strand transfer inhibitors, HIV, pharmacokinetics, efficacy, resistance, adherence, tolerability.
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