Tegobuvir

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Tegobuvir is an investigational antiviral drug that was developed for the treatment of Hepatitis C (HCV) infection. It is a non-nucleoside inhibitor of the HCV NS5B polymerase, which is essential for viral replication.

Mechanism of Action

Tegobuvir acts by inhibiting the NS5B RNA-dependent RNA polymerase of the Hepatitis C virus. This enzyme is crucial for the replication of the viral RNA genome. By binding to a specific site on the NS5B polymerase, tegobuvir prevents the polymerase from synthesizing new viral RNA, thereby inhibiting viral replication.

Clinical Development

Tegobuvir was developed by Gilead Sciences, a biopharmaceutical company known for its work in antiviral therapies. It was evaluated in several clinical trials, often in combination with other antiviral agents such as Ribavirin and Peginterferon alfa-2a.

Phase I Trials

Initial studies focused on assessing the safety, tolerability, and pharmacokinetics of tegobuvir in healthy volunteers and HCV-infected patients. These studies demonstrated that tegobuvir was generally well-tolerated and showed antiviral activity.

Phase II Trials

In Phase II trials, tegobuvir was tested in combination with other antiviral agents. The results indicated that tegobuvir, when used in combination therapy, could enhance the antiviral response in patients with chronic HCV infection.

Phase III Trials

Despite promising results in earlier trials, tegobuvir did not advance to Phase III trials. The development was halted due to the emergence of more effective direct-acting antiviral agents that offered higher cure rates and shorter treatment durations.

Pharmacokinetics

Tegobuvir is administered orally. It is metabolized primarily in the liver and excreted in the urine and feces. The pharmacokinetic profile of tegobuvir supports once-daily dosing.

Adverse Effects

In clinical trials, tegobuvir was generally well-tolerated. The most common adverse effects reported were mild to moderate and included headache, fatigue, and nausea.

Current Status

As of the latest updates, tegobuvir is not approved for clinical use and is not currently being developed further. The focus has shifted to other antiviral agents with superior efficacy and safety profiles.

Also see

• Hepatitis C virus
• NS5B polymerase inhibitors
• Direct-acting antivirals
• Gilead Sciences