Drug intelligence / Profile preview

peginterferon alfa-2a + entecavir

Development stage
Preclinical
Lead developer
Roche
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Cytokines & Interferons → Recombinant Proteins and Enzymes
Administration
Oral, Subcutaneous
01

Overview

Peginterferon alfa-2a + entecavir is a combination therapy used primarily in the treatment of chronic hepatitis B and has been studied for chronic hepatitis D. Peginterferon alfa-2a is a pegylated recombinant form of interferon alpha that exerts both immunomodulatory and antiviral effects by binding to type 1 interferon receptors, leading to activation of intracellular signaling pathways that enhance the immune response against viral infections[1][6]. Entecavir is a potent nucleoside analogue that selectively inhibits hepatitis B virus (HBV) polymerase, blocking three key steps in HBV DNA replication: priming, reverse transcription of negative-strand DNA, and synthesis of positive-strand DNA[5]. The combination aims to improve virologic response rates by targeting different aspects of viral replication and host immunity. This regimen has been evaluated for efficacy and safety in patients with chronic HBV infection (including pediatric populations) as well as in clinical trials for chronic hepatitis D; however, some studies have shown limited additional benefit over monotherapy with peginterferon[4][5].

Brand names
PegasysBaraclude
Other names
PEG-IFNα-2a + entecavirPegasys + entecavir
02

Targets

IFNAR (Immune system modulation via type I interferon receptor)HBV Pol (Hepatitis B virus polymerase)

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