Raltegravir: first integrase inhibitor for the treatment of HIV infection

Raltegravir is the first of the integrase inhibitors to have been approved for treating HIV-1-infected adult patients who have evidence of viral replication and HIV-resistant restrains to multiple antiretroviral agents, in combination with other antiretroviral agents. Raltegravir is an inhibitor of strand transfer of reverse-transcribed viral DNA into the host genome, and is administered orally twice daily without boosting. Clinical and pharmacokinetic studies showed strong virological responses, with as yet unmet antiretroviral potency, as well as excellent metabolic tolerance, and a favorable drug-drug interaction profile, Further evaluation of possible indications and strategies are needed in terms of long-term tolerability, resistance, penetration in different anatomical compartments, effect on reservoirs, new antiretroviral combinations, first-line treatment, and switching to and treatment intensifications with raltegravir.