Drug intelligence / Profile preview

dolutegravir + telaprevir

Development stage
Unknown
Lead developer
ViiV Healthcare
Modality
Small Molecules
Administration
Oral
01

Overview

Dolutegravir + telaprevir is a combination of two antiviral small molecule drugs: dolutegravir, an HIV-1 integrase strand transfer inhibitor, and telaprevir, a hepatitis C virus (HCV) NS3/4A protease inhibitor. Dolutegravir inhibits HIV integrase by binding at the active site and blocking the strand transfer step of retroviral DNA integration, which is essential for HIV replication. Telaprevir inhibits the HCV NS3/4A serine protease, thereby blocking viral polyprotein cleavage and HCV replication. Although not available as a fixed-dose combination product, clinical studies have shown this combination can be safely coadministered in the context of HIV/HCV coinfection, resulting in no clinically significant drug–drug interactions or required dose adjustments, and offers an option for treating patients coinfected with HIV and HCV[1][2].

02

Targets

NS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)Integrase allosteric pocket (HIV)

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