Drug intelligence / Profile preview

GSK2485852 + ritonavir

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK2485852 + ritonavir is an investigational combination therapy developed for the treatment of chronic hepatitis C virus (HCV) infection. GSK2485852 is a non-nucleoside inhibitor targeting the NS5B polymerase at site IV of the HCV replication complex, thereby inhibiting viral RNA synthesis[2]. Ritonavir is a protease inhibitor primarily used as a pharmacokinetic booster; it inhibits cytochrome P450 3A4 (CYP3A4), increasing plasma concentrations and prolonging the activity of co-administered drugs[5][6]. In this combination, ritonavir serves to enhance exposure to GSK2485852 by reducing its metabolic clearance. The development status for this combination in HCV was terminated after early-phase clinical trials[3].

02

Targets

CYP3A4 (Cytochrome P450 3A4)NS5B (Hepatitis C virus non-structural protein 5B (NS5B) RNA-dependent RNA polymerase)PR (Progesterone receptor)

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