Discovery and development of integrase inhibitors

The first human immunodeficiency virus (HIV) case was reported in the United States in the early 1980s. Many drugs have been discovered to treat the disease, but mutations in the virus and resistance to the drugs make development difficult. Integrase is a viral enzyme that integrates retroviral DNA into the host cell genome. Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral drugs used in the treatment of HIV. Since the approval of the first INSTI, raltegravir, in 2007, five INSTIs have been introduced: raltegravir, elvitegravir, dolutegravir, bictegravir, and cabotegravir. Second-generation INSTIs — dolutegravir and bictegravir — are now the globally preferred backbone of first-line antiretroviral therapy, recommended by the World Health Organization (WHO), the National Institutes of Health (NIH), and other major clinical guidelines. As of 2024, more than 25 million people worldwide are receiving dolutegravir-based regimens. Key things to verify after pasting:

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