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ASC42 + entecavir + peginterferon alfa-2a

Development stage
Phase 2
Lead developer
Ascletis Pharma
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, Recombinant Proteins and Enzymes
Administration
Oral, Subcutaneous
01

Overview

This is a combination therapy consisting of three agents: - **ASC42**: A potent, selective, orally administered farnesoid X receptor (FXR) agonist developed by Ascletis Pharma. ASC42 uniquely inhibits the transcription of hepatitis B virus (HBV) covalently closed circular DNA (cccDNA) into HBV RNA, potentially reducing both HBV RNA and cccDNA stability. Its primary indication is chronic hepatitis B, where it may contribute to functional cure through antiviral activity at the level of HBV cccDNA transcription[1][3]. - **Entecavir**: A hepatitis B virus polymerase inhibitor nucleoside analogue, used for the treatment of chronic hepatitis B. It is an approved first-line therapy for HBV. - **Peginterferon alfa-2a**: A recombinant, pegylated interferon that acts as an immunomodulator and antiviral by binding to type I interferon receptors, activating the JAK/STAT pathway, and upregulating genes involved in antiviral responses. It is approved for the treatment of chronic hepatitis B and C[2][4][6]. This combination is being studied in Phase II clinical trials for the treatment of chronic hepatitis B, aiming for a functional cure by targeting viral replication, stability, and immune response[1][3].

Other names
entecavirpegylated interferon alpha-2aPEG-IFN-α-2a
02

Targets

FXR (Farnesoid x-activated receptor)HBV Pol (Hepatitis B virus polymerase)IFNAR (Immune system modulation via type I interferon receptor)IFNAR1 (Interferon alpha/beta receptor 1)IFNAR2 (Interferon alpha/beta receptor subunit 2)

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