Deleobuvir

Deleobuvir (formerly known as BI 207127) is an experimental antiviral medication that was under investigation for the treatment of Hepatitis C virus (HCV) infection. Deleobuvir is a non-nucleoside inhibitor of the HCV NS5B polymerase, a key enzyme necessary for the replication of the hepatitis C virus. Despite initial promise in early clinical trials, development of deleobuvir for the treatment of hepatitis C was discontinued due to issues with efficacy and the emergence of better treatment options.

Mechanism of Action

Deleobuvir inhibits the HCV NS5B RNA-dependent RNA polymerase. By binding to this enzyme, deleobuvir prevents the replication of the hepatitis C virus's RNA genome, which is a critical step in the virus's life cycle. As a non-nucleoside inhibitor, it binds to a site on the NS5B polymerase that is distinct from the active site, leading to a conformational change that reduces the enzyme's activity.

Clinical Trials

Deleobuvir was studied in several phase II and phase III clinical trials, often in combination with other antiviral agents such as ribavirin and protease inhibitors. These studies aimed to evaluate the efficacy, safety, and optimal dosing regimen of deleobuvir in various patient populations, including those with different HCV genotypes and treatment histories.

Despite showing some level of efficacy in reducing HCV RNA levels in infected patients, deleobuvir's development was ultimately halted. The decision was influenced by the comparative effectiveness and safety profiles of other direct-acting antivirals that became available, which offered higher cure rates and better tolerability.

Adverse Effects

During its clinical development, deleobuvir was associated with several adverse effects. Commonly reported side effects included fatigue, headache, nausea, and rash. In some cases, elevated liver enzymes were observed, indicating potential liver toxicity. The safety profile of deleobuvir, in combination with its efficacy results, contributed to the decision to discontinue its development.

Current Status

As of the last update, the development of deleobuvir for the treatment of hepatitis C has been discontinued. The focus of HCV treatment has shifted towards highly effective and well-tolerated direct-acting antivirals that can cure the majority of infections with shorter durations of therapy and fewer side effects.

See Also

• Hepatitis C virus
• Antiviral drug
• RNA polymerase inhibitor
• Direct-acting antiviral