Drug intelligence / Profile preview

GS-9131 + bictegravir + darunavir + ritonavir

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of four antiretroviral drugs used for HIV-1 treatment, particularly considered for patients with resistance to nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs): - **GS-9131 (rovafovir etalafenamide):** A novel nucleotide reverse transcriptase inhibitor (NRTI), developed as a phosphonoamidate prodrug of GS-9148. It exhibits potent activity against wild-type and multiple NRTI-resistant HIV-1 strains, including those with K65R, L74V, and M184V mutations. GS-9131 shows low cytotoxicity, favorable pharmacokinetics, and a unique resistance profile conducive to salvage therapy in treatment-experienced populations[1][2][3][4][5][6][7][8]. - **Bictegravir:** An integrase strand transfer inhibitor (INSTI), inhibits HIV integrase and prevents viral DNA integration into the host genome. - **Darunavir:** A protease inhibitor (PI), blocks HIV protease and prevents maturation of infectious virions. - **Ritonavir:** Used at low doses as a pharmacokinetic enhancer to boost darunavir exposure by inhibiting CYP3A-mediated metabolism. This combination is not a standard marketed therapy but could represent a regimen under investigation or in clinical use for highly treatment-experienced patients with multidrug-resistant HIV-1[1][4].

Other names
rovafovir etalafenamide + bictegravir + darunavir + ritonavir
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)Integrase allosteric pocket (HIV)PR (Progesterone receptor)

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