Table 1.
Direct-acting Antivirals for HBV in Development
| Compound | Mechanism and Target | Stage of Development | Sponsor | Reference and Clinicaltials.gov no |
|---|---|---|---|---|
| Besifovir | Polymerase | Phase 3, Approved in S. Korea | Il Dong Pharmaceutical; South Korea | 102; NCT01937806 |
| DA-2802 (tenofovir disoproxil orotate) | Polymerase | Phase 3 | Dong-A ST Co., Ltd.; South Korea | NCT02967939 |
| Metacavir | Polymerase | Phase 2 | Guangzhou Yipinhong Pharmaceutical, China | 103; NCT02965859 |
| CMX157 (tenofovir Exalidex) | Polymerase | Phase 2 | ContraVir Pharmaceuticals | NCT02710604 |
| RNase H inhibitors | RNaseH | Preclinical | Arbutus | sponsor’s web site |
| JNJ-379 (JNJ-56136379) |
Capsid | Phase 2 | Janssen Sciences, Belgium | NCT03361956 |
| GLS4 | Capsid | Phase2 | HEC Pham, China | 145; sponsor’s web site |
| ABI-H0731 | Capsid | Phase 1b/2a | Assembly | NCT03109730 |
| NVR 3–778 (AL-3778) |
Capsid | Phase 1/2 | Novira |
146; NCT02112799 NCT02401737 |
| Bay 41–4109 | Capsid | Phase 1 | AiCuris, Germany | 147; sponsor’s web site |
| RO7049389 | Capsid | Phase 1 | Roche, Switzerland | NCT02952924 |
| JNJ-440 | Capsid | Phase 1 | Alios Biopharma | NCT03439488 |
| AB-423 | Capsid | Phase 1 | Arbutus | sponsor’s web site |
| QL-007 | Capsid | Phase 1 | Qilu Pharmaceutical, China | NCT03244085 |
| AB-506 | Capsid | Preclinical | Arbutus | sponsor’s web site |
| ABI-H2158 | Capsid | Preclinical | Assembly | sponsor’s web site |
| ARB-1467 (TKM-HBV) |
siRNA | Phase 2 | Arbutus | NCT02631096 |
| ARO-HBV | siRNA | Phase 1/2 | Arrowhead | NCT03365947 |
| ALN-HBV | siRNA | Phase 1/2 | Alnylam | sponsor’s web site |
| LUNAR™-HBV | siRNA | Preclinical | Arcturus | sponsor’s web site |
| Hepbarna (BB-HB-331) | siRNA | Preclinical | Benitec, Australia | sponsor’s web site |
| ARC-520 | siRNA | Terminated | Arrowhead |
NCT02452528 NCT02604212 NCT02604199 NCT02738008 NCT02065336 NCT02577029 |
| ARC-521 | siRNA | Terminated | Arrowhead | NCT02797522 |
| ARB-1740 | siRNA | Terminated | Arbutus | sponsor’s web site |
| IONIS-HBVLRx (GSK3389404) |
Antisense oligonucleotide | Phase 2 | Ionis Pharmaceuticals, with GlaxoSmithKline, United Kingdom | NCT03020745 |
| IONIS-HBVRx (GSK3228836) |
Antisense oligonucleotide | Phase 2 | Ionis Pharmaceuticals, with GlaxoSmithKline, United Kingdom | NCT02981602 |
| RG6004 (RO7062931) |
Locked Nucleic Acid | Phase 1/2 | Roche, Switzerland | 148; NCT03038113 |
| AB-452 | RNA destabilizer | Preclinical | Arbutus | sponsor’s web site |
| EBT106 | CRISPR | Preclinical | Excision BioTherapeutics | sponsor’s web site |
| HBV | CRISPR | Preclinical | Intellia Therapeutics | sponsor’s web site |