Drug intelligence / Profile preview

mericitabine

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

Overview

Mericitabine is an orally bioavailable nucleoside analog polymerase inhibitor that was developed for the treatment of chronic hepatitis C virus (HCV) infection. It acts as a prodrug of PSI-6130 (2-deoxy-2-fluoro-2-methylcytidine). Once inside the host cell, it is phosphorylated into its active triphosphate form, which competes with natural cytidine triphosphate for incorporation into the viral RNA strand by the HCV NS5B RNA-dependent RNA polymerase. This incorporation leads to premature chain termination of the viral RNA, effectively inhibiting viral replication. Developed through a collaboration between Pharmasset and Roche, mericitabine was evaluated in various clinical trials, often in combination with other direct-acting antivirals or standard-of-care interferon-based regimens. However, development was ultimately discontinued in favor of more potent second-generation HCV inhibitors.

Other names
2-Deoxy-2-fluoro-2-methylcytidine diisobutyratePSI-6130 prodrugPSI6130 prodrugPSI 6130 prodrug
02

Targets

NS5B (Hepatitis C virus non-structural protein 5B (NS5B) RNA-dependent RNA polymerase)

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