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GSK3968866
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Subcutaneous
01
Overview
GSK3968866 is a GalNAc-conjugated antisense oligonucleotide (ASO) being developed by GSK for the treatment of chronic hepatitis B (CHB). It is the second-generation, hepatocyte-targeted version of bepirovirsen (GSK3228836). By utilizing N-acetylgalactosamine (GalNAc) conjugation, the drug specifically targets the asialoglycoprotein receptor (ASGPR) on the surface of liver cells, allowing for efficient uptake and potentially lower systemic exposure. Once inside the cell, the ASO binds to a conserved region of the HBV RNA transcripts, leading to their degradation via RNase H. This mechanism results in the reduction of viral proteins, most notably the hepatitis B surface antigen (HBsAg), which is a key factor in the persistence of chronic infection and the suppression of the host immune response.
- Other names
- GalNAc-conjugated bepirovirsen
02
Targets
ASGPR (Asialoglycoprotein Receptor 1)
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