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RO7445482 + RO7020531 + nucleos(t)ide

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules, Chemically Modified siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Conjugated siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
Administration
Subcutaneous, Oral
01

Overview

This combination drug consists of **RO7445482** (xalnesiran, a small interfering RNA targeting the Hepatitis B surface antigen (HBsAg) coding region of the HBV genome), **RO7020531** (ruzotolimod, an oral prodrug of a Toll-like receptor 7 agonist), and a **nucleos(t)ide analogue (NUC)**, which refers to oral antiviral agents such as entecavir or tenofovir commonly used in the treatment of chronic hepatitis B. - RO7445482 functions as an siRNA to silence viral antigen production and promote immune clearance. - RO7020531 (prodrug: RG7854; active: RO7011785) activates TLR7, stimulating both innate and adaptive immune responses to enhance viral clearance. - Nucleos(t)ide analogues inhibit HBV DNA polymerase, suppressing viral replication. The regimen is under investigation for the **functional cure of chronic hepatitis B** (CHB), aiming for Hepatitis B surface antigen (HBsAg) loss by combining direct antiviral activity with immunomodulation. Developed and investigated by Roche, the combination is being studied in phase 2 clinical trials for efficacy, safety, and the potential to achieve sustained HBsAg loss in people with CHB[1][2][3][4][5].

Other names
RG6346 + RG7854 + nucleos(t)ide analogue
02

Targets

HBV Pol (Hepatitis B virus polymerase)TLR7 (Toll-like receptor 7)

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