Novel integrase inhibitors for HIV

Abstract

Importance of the field: Integrase inhibitors are the newest class of antiretroviral agents developed to treat HIV-1 infection. Raltegravir (RAL), the only integrase inhibitor (INI) currently approved for the treatment of HIV-infected patients, has proven to be a potent and well-tolerated antiretroviral (ARV) agent. It is currently approved and used for the treatment of both ARV-experienced and ARV-naive patients. Nevertheless, the relatively low genetic barrier for resistance of RAL encourages the search for new INIs with different mechanisms of actions and resistance profiles.

Areas covered in this review: Here we review the data available about INI that are currently being tested in clinical trials or are in preclinical development: elvitegravir (EVG), S/GSK1349572, S/GSK1265744 and LEDGINs. We focus on their clinical efficacy, pharmacokinetic, safety and resistance profiles.

What the reader will gain: Up-to-date overview on the currently available, clinically relevant INIs and promising preclinical inhibitors at all phases of development.

Take home message: Integrase inhibitors represent the newest therapeutic class available to treat HIV-1 infection. There are a variety of compounds either available in the clinic (RAL), advancing to Phase III trials (EVG), or in earlier phases of development. Taken together, this class offers new treatment options for the HIV-infected individual.

Keywords::

• elvitegravir
• HIV-1
• integrase
• integrase inhibitor
• LEDGF/p75
• raltegravir
• S/GSK1265744
• S/GSK1349572

Notes

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