Deleobuvir: Difference between revisions

Latest revision as of 03:55, 13 February 2025

Deleobuvir[edit]

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[edit]

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[edit]

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[edit]

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[edit]

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[edit]

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.

Related Pages[edit]

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-'''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.
+== Deleobuvir ==
-==Mechanism of Action==
+[[File:Deleobuvir.svg|thumb|right|Chemical structure of Deleobuvir]]
-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''' 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.
-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.
+== Mechanism of Action ==
-==Adverse Effects==
+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.
-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==
+== Clinical Development ==
-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==
+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.
-* [[Hepatitis C virus]]
+== 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.
+== Related Pages ==
+* [[Hepatitis C]]
 * [[Antiviral drug]]
-* [[RNA polymerase inhibitor]]
+* [[RNA polymerase]]
-* [[Direct-acting antiviral]]
+* [[NS5B protein]]
 [[Category:Antiviral drugs]]
 [[Category:Hepatitis C]]
-{{medicine-stub}}