Drug intelligence / Profile preview

danoprevir + ritonavir + RO5024048 + ribavirin

Development stage
Phase 2
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination regimen consisting of four direct-acting antivirals (DAAs) used in the treatment of chronic hepatitis C virus (HCV) infection, specifically genotype 1. - **Danoprevir** is a macrocyclic inhibitor targeting the HCV NS3/4A protease, essential for viral replication. - **Ritonavir** acts as a pharmacokinetic enhancer ("booster") by inhibiting cytochrome P450 3A4, thereby increasing danoprevir plasma concentrations. - **RO5024048** (also known as mericitabine) is an HCV NS5B polymerase inhibitor (nucleoside analogue), which impedes viral RNA synthesis. - **Ribavirin** is a nucleoside analogue antiviral that interferes with viral RNA metabolism and is often combined with other agents for enhanced antiviral effect. This combination has been evaluated in clinical trials for efficacy and safety in HCV genotype 1 chronic infection, including in populations that have failed previous protease inhibitor therapies[1][3][8]. The combination has not received market approval and was investigated primarily under the sponsorship of Hoffmann-La Roche[8].

Other names
danoprevir + ritonavir + RO5024048 + ribavirin
02

Targets

CYP3A (CYP3A family)NS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)NS5B (Hepatitis C virus non-structural protein 5B (NS5B) RNA-dependent RNA polymerase)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)CYP3A4 (Cytochrome P450 3A4)

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