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Table 1 Novel agents against HBV and phase of development

From: Upcoming pharmacological developments in chronic hepatitis B: can we glimpse a cure on the horizon?

Mode of action Target Drug Clinical phase
Direct acting antivirals
 Polymerase inhibition HBV polymerase Tenofovir alafenamide Phase 3
Besifovir Phase 3
 Entry inhibition NTCP Myrcludex-B Phase 2a
 Core inhibitors Nucleocapsid assembly NVR 3–778 Phase 2
AT-61, AT130, Bay 41–4109 Preclinical
 Cleavage of DNA ccc-DNA ZFNs,TALENs,CRISPR/Cas Preclinical
 Inhibition of ccc-DNA formation CCC-0975 and CCC-0346 Preclinical
 Non-cytolitic cccDNA degradation by inducing APOBEC3A and APOBEC3B Lymphotoxin-b receptor agonist Preclinical
 Apoptosis induction by inhibiting cIAPs CIAPs Birinapant Phase 1
 Knock down HBV RNA, viral proteins and HBV DNA HBV RNA ARC-520, ARC-521 Phase 2
 Block release of HBsAg REP-2139 Phase 2
 Antisense nucleotides Target RNA ASOs Preclinical
Host targeting agents
 Exogenous interferon stimulation Innate immunity TLR7 Toll-like receptor (TLR) agonist (GS-9620) Phase 2
 Stimulate IFN response Innate immunity RIG-I SB 9200 Phase 2
 Therapeutic vaccination Adaptive immunity GS-4774 (Tarmogen) Phase 2b
ABX203 Phase 2b
  1. APOBEC apolipoprotein B mRNA editing enzyme, catalytic polypeptide 3A and 3B, ASO antisense nucleotides, cccDNA covalently closed circular DNA, CIAPs Cellular inhibitor of apoptosis proteins, CRISPR/Cas clustered regulatory interspaced short palindromic repeats (CRISPR) and CRISPR associated (Cas) systems, NTCP sodium taurocholate co-transporting polypeptide, RIG-I Retinoic acid-inducible gene, TALENs transcription activator-like effector nucleases, ZFNs zinc-finger nucleases