Human immunodeficiency virus-1 (HIV-1) integrase inhibitors İnsan İmmünoyetmezlik Virüsü-1 (HIV-1) İntegraz İnhibitörleri

Erkekoğlu P., Koyuncu N.

Hacettepe University Journal of the Faculty of Pharmacy, vol.37, no.1, pp.29-51, 2017 (Scopus) identifier


© 2017, Hacettepe University, Faculty of Pharmacy. All rights reserved.Human immunodeficiency virus-1 (HIV-1) requires protease, reverse transcriptase and integrase (IN) for replication. In the last decades, HIV-1 IN is gaining popularity as a target for the antiviral therapy of acqired immunodeficiency syndrome (AIDS). Substantial work focusing on IN has been performed and three new drugs (raltegravir, elvitegravir and dolutegravir) received approval from Food and Drug Administration (FDA). These drugs can be used in single or combined dose regimens to obtain better reduction in HIV DNA copies. The efficacy and safety of these three drugs in treatment-naïve and experienced HIV-infected patients have been established by multiple studies. Based on the current practice guidelines, IN inhibitor-based drug regimens are considered as one of the first-line therapies for treatment-naïve HIV-infected patients. There are also several new IN inhibitors (natural or synthetic) in development. These efficiancies and side effects of these substances are now being investigated by different studies. The most important goals of these studies are to increase the efficacy, to improve the resistance profiles and to decrease the frequency of drug administration and side effects. This review will focus on the pharmacology and toxicology of IN inhibitors in use and the newly discovered IN inhibitors.