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• W1722558419 abstract "Integration of the viral genome into the host cell chromatin is a central step in the replication cycle of HIV. Blocking the viral integrase (IN) enzyme therefore provides an attractive therapeutic strategy, as evidenced by the recent clinical approval of three IN strand transfer inhibitors. Dolutegravir is a therapy that is unique in its ability to evade HIV drug resistance in treatment-naïve patients.This review starts by providing a brief summary of the history of HIV-1 IN inhibitors. The authors follow this with details of the discovery and preclinical and clinical developments of dolutegravir. Finally, the authors provide details of dolutegravir's post-launch including the launch of the combination pill of dolutegravir, abacavir and lamivudine in August 2014.The launch of raltegravir, the first IN inhibitor from Merck & Co., has created new hopes for the patient. Indeed, pharmaceutical companies have not lost courage by attempting to address the major drawbacks of this first-in-class molecule. And while the drug elvitegravir has been inserted into a four-drug combination pill providing a once-daily dosing alternative, dolutegravir has demonstrated superiority in terms of its efficacy and resistance." @default.
• W1722558419 created "2016-06-24" @default.
• W1722558419 creator A5017363924 @default.
• W1722558419 creator A5034695969 @default.
• W1722558419 date "2015-09-07" @default.
• W1722558419 modified "2023-09-23" @default.
• W1722558419 title "The preclinical discovery and development of dolutegravir for the treatment of HIV" @default.
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• W1722558419 doi "https://doi.org/10.1517/17460441.2015.1064896" @default.
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