Integrase Inhibitors

Elvitegravir

Products Elvitegravir is commercially available as film-coated tablets in fixed combination with other antiretroviral agents and cobicistat (Stribild, successor: Genvoya). It has been approved in many countries since 2013. Stribild: elvitegravir, cobicistat, emtricitabine, and tenofovirdisoproxil. Genvoya: elvitegravir, cobicistat, emtricitabine and tenofoviralafenamide. Structure and properties Elvitegravir (C23H23ClFNO5, Mr = 447.9 g/mol) is a dihydroquinolone derivative. It … Elvitegravir

Bictegravir

Products Bictegravir was approved in the United States and EU in 2018 and in many countries in 2019 in fixed combination with emtricitabine and tenofoviralafenamide in the form of film-coated tablets (Biktarvy). Structure and properties Bictegravir (C21H18F3N3O5, Mr = 449.4 g/mol) exists as a white to yellowish substance. Effects Bictegravir (ATC J05AR20) has antiviral properties. … Bictegravir

Dolutegravir

Products Dolutegravir was approved in the United States and EU in 2013 in film-coated tablet form (Tivicay). It was registered in many countries in 2014. A fixed-dose combination with dolutegravir, abacavir, and lamivudine is also available (Triumeq). In 2017, a combination product with rilpivirine was launched in the US (Juluca). It was approved in the … Dolutegravir

Raltegravir

Products Raltegravir is commercially available as film-coated tablets and chewable tablets (Isentress). It was approved in the United States in 2007 and in many countries in 2008 as the first integrase inhibitor. Structure and properties Raltegravir (C20H21FN6O5, Mr = 444.4 g/mol) is a hydroxypyrimidinone carboxamide. It is present in drugs in the form of the … Raltegravir