Deleobuvir

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Deleobuvir

Chemical structure of Deleobuvir

Deleobuvir is an investigational antiviral drug that was developed for the treatment of hepatitis C virus (HCV) infection. It is a non-nucleoside inhibitor of the HCV RNA polymerase, specifically targeting the NS5B protein, which is essential for viral replication.

Mechanism of Action

Deleobuvir functions by binding to the NS5B RNA-dependent RNA polymerase of the hepatitis C virus. This binding inhibits the polymerase activity, thereby preventing the replication of the viral RNA. Unlike nucleoside inhibitors, which mimic the natural substrates of the polymerase, non-nucleoside inhibitors like Deleobuvir bind to an allosteric site, inducing conformational changes that reduce the enzyme's activity.

Clinical Development

Deleobuvir was evaluated in several clinical trials to assess its efficacy and safety in combination with other antiviral agents. It was primarily tested in combination with pegylated interferon and ribavirin, as well as with other direct-acting antivirals. The goal was to achieve a sustained virologic response (SVR), which is indicative of a successful treatment outcome.

Pharmacokinetics

The pharmacokinetic profile of Deleobuvir includes its absorption, distribution, metabolism, and excretion. It is administered orally and undergoes hepatic metabolism. The drug's half-life and bioavailability are important factors in determining the dosing regimen.

Side Effects

Common side effects observed in clinical trials of Deleobuvir include fatigue, nausea, and headache. As with many antiviral therapies, the combination regimens can lead to more complex side effect profiles, necessitating careful monitoring of patients.

Discontinuation

Despite initial promise, the development of Deleobuvir was eventually discontinued. This decision was influenced by the emergence of more effective and better-tolerated antiviral agents for HCV, such as sofosbuvir and ledipasvir, which offered higher cure rates and shorter treatment durations.

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Contributors: Prab R. Tumpati, MD