Drug intelligence / Profile preview

ledipasvir + sofosbuvir + asunaprevir

Development stage
Unknown
Lead developer
Humanity and Health Research Centre
Modality
Small Molecules
Administration
Oral
01

Overview

This is an investigational triple combination therapy consisting of three direct-acting antivirals (DAAs): ledipasvir, sofosbuvir, and asunaprevir. Ledipasvir is an HCV NS5A inhibitor, sofosbuvir is an HCV NS5B RNA-dependent RNA polymerase inhibitor, and asunaprevir is an HCV NS3-4A protease inhibitor. The combination was evaluated by the Humanity and Health Research Centre in collaboration with the 302 Hospital in Beijing to evaluate an ultra-short (3-week) treatment regimen for non-cirrhotic patients with chronic hepatitis C virus (HCV) genotype 1b infection. The rationale was that adding a protease inhibitor to the dual NS5A/NS5B regimen would enhance antiviral efficacy enough to significantly shorten the treatment duration. In a phase 2 proof-of-concept study, patients who achieved an ultrarapid virological response by day 2 and completed the 3-week triple therapy achieved a 100% sustained virological response at 12 weeks (SVR12).

Other names
ledipasvir/sofosbuvir + asunaprevirLDV/SOF + ASV
02

Targets

NS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)NS5A (Hepatitis C virus nonstructural protein 5A (genotype 1b))NS5B (Hepatitis C virus non-structural protein 5B (NS5B) RNA-dependent RNA polymerase)

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