Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects[1][2][3].
Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor used to treat HIV and chronic Hepatitis B.
HBV Seq2 aa:28-39 is a HBsAg peptide, which binds to major histocompatibility complex (MHC) class I molecules[1][2].
HBV-IN-9 is a potent HBsAg (HBV Surface antigen) inhibitor (IC50=10 nM) and HBV DNA production inhibitor (IC50=0.15 nM in HepG2.2.15 cells)[1]. From patent WO2018001952A1, example 20.
Alamifovir (LY582563; MCC-478), a purine nucleotide analogue prodrug, shows potent activity against wild type and lamivudine resistant hepatitis B virus (HBV). Alamifovir has high activity against HBV replication and sustained antiviral effect[1][2].
Junceellolide C is a transcription inhibitor of cccDNA. Junceellolide C inhibits HBV DNA replication and significantly decreases the level of supernatant HBV RNA with EC50 values of 5.19, 3.52 μM respectively in HepAD38 cells. Junceellolide C is a potent anti-HBV agent[1].
Bicyclol(SY 801) is a anti-hepatitis drug.Target: HBVOral administration of bicyclol normalized the elevated serum transaminases (ALT, AST) by approximately 50% in chronic viral hepatitis B and C, and also showed certain level of inhibiting HBV and HCV replication. No noticeable adverse reaction has been observed. In combination therapy of bicyclol with interferon alpha, lamivudine and adefovir dipivoxil in HBV or HCV, bicyclol may potentiate the anti-viral efficacy and reduce YMDD mutant and side effects. In 2004 China FDA issued license to manufacture bicyclol. Since then bicyclol has been widely used to treat chronic HBV and HCV in China [1].
AB-506 is a small-molecule inhibitor targeting HBV core protein, inhibits viral replication in vitro (IC50=77 nM).AB-506 binds to HBV core protein, accelerates capsid assembly and inhibits HBV pgRNA encapsidation.AB-506 blocks cccDNA establishment in HBV-infected HepG2-hNTCP-C4 cells and primary human hepatocytes, leading to inhibition of viral RNA, HBsAg, and HBeAg production (EC50=0.64-1.52 uM).AB-506 demonstrated activity across HBV genotypes A-H and maintains antiviral activity against nucleostide analog-resistant variants in vitro.AB-506 showed an 8 to 20-fold increase in EC50 values against L30F, L37Q, and I105T substitutions.AB-506 exhibits good oral bioavailability, systemic exposure, and higher liver to plasma ratios in rodents.
HBV-IN-19 inhibits hepatitis B virus (HBV) infection. Inhibiting HBsAg secretion and/or production is a strategy for the treatment of HBV infection, including chronic HBV infection[1].
Sophoranol is an alkaloid that can be isolated from S. flavescens, with antiviral activity. Sophoranol has anti-HBV (hepatitis B virus) activity. Sophoranol shows potent antiviral activities against respiratory syncytial virus (RSV) with an IC50 of 10.4 μg/mL[1][2].
FNC-TP is the intracellular active form of FNC. FNC is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV[1].
Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses[1][2][3].
GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM.GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools[1].
Elebsiran is an antiviral agent[1].
Bay 41-4109 less active enantiomer shows less activity than Bay 41-4109. BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.
Schisantherin C exhibits anti-HBV activity with potency against HBsAg and HBeAg secretion by 59.7% and 34.7% at 50μg/mL[1].
Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV[1][2][3].
Lagociclovir(MIV-210) is a prodrug of 3'-fluoro-2',3'-dideoxyguanosine with high oral bioavailability in humans and potent activity against HBV. IC50 value:Target: Anti-HBV compoundOral administration of MIV-210 at 20 or 60 mg/kg of body weight/day induced a rapid virological response in chronically infected woodchucks, reducing serum WHV DNA levels by 4.75 log10 and 5.72 log10, respectively, in 2 weeks. Further, a daily dose of 10 mg/kg decreased the serum WHV load 400-fold after 4 weeks of treatment, and a dose of 5 mg/kg/day was sufficient to maintain this antiviral effect during the following 6-week period. MIV-210 at 20 or 60 mg/kg/day reduced the liver WHV DNA load 200- to 2,500-fold from pretreatment levels and, importantly, led to a 2.0 log10 drop in the hepatic content of WHV covalently closed circular DNA.
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains[1].
HBV-IN-31 is a potent cccDNA (covalently closed circular DNA) inhibitor. HBV-IN-31 shows anti-HBV activity with an IC50 value of 0.13 µM for HBsAg. HBV-IN-31 inhibits cell growth[1].
L-Fd4A is an adenine derivative. L-Fd4A has anti-human immunodeficiency virus (HIV) (EC50=1.5 μM) and anti-hepatitis B virus (HBV) (EC50=1.7 μM) activity. L-Fd4A has low cytotoxicity[1].
HBV-IN-22 (Compound LC5f) is an inhibitor of HBV DNA replication with IC50 values of 0.71 µM and 0.84 µM against wild-type and drug resistant HBV strains, respectively[1].
Mulberrofuran G protects ischemic injury-induced cell death via inhibition of NOX4-mediated ROS generation and ER stress[1]. Mulberrofuran G shows moderate inhibiting activity of hepatitis B virus (HBV) DNA replication with the
Bulevirtide (Myrcludex B) is a NTCP inhibitor, a linear lipopeptide of 47 amino acids. Bulevirtide inhibits HBV and HDV entry into liver cells, blocks HBV infection in hepatocytes, and participates in HBV transcriptional suppression. Bulevirtide can be used in HDV infection and compensated cirrhosis research[1][2].
Hepatitis b virus pre-s region (120-145) is a preS2 peptide that inhibits the binding of single-chain Fv fragment (scFv) or IgG to r-HBsAg[1].
Fosclevudine alafenamide (Compound EIDD-02173) is an antiviral agent with an EC50 of 1.71 μM against HBV[1].
HBV-IN-16 is a potent inhibitor of covalently closed circular DNA (cccDNA). cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-16 is a quinoline derivative. HBV-IN-16 has the potential for the research of HBV infection (extracted from patent WO2019121357A1, compound 1)[1].
Helioxanthin (ACH126447) and its analogues exhibit significant in vitro antiviral activity against hepatitis B virus (HBV, EC50=1 uM) and flavivirus.IC50 value: 1/3/2 uM (EC50, HBV/HCV/HSV-1) [1]Target: Anti-HBV; Anti flavivirusin vitro: Helioxanthin and its analogues decreased cellular RNA levels of HBV and antigen expression as well as selective inhibition of HBV replication in a cell culture model [2]. Helioxanthin analogue 8-1 exhibited anti-DHBV activity as demonstrated by quantification of viral DNA, RNA, covalently closed circular DNA and protein synthesis. Analogue 8-1 did not affect the stability of cellular macromolecules and did not have a sustained antiviral effect after drug removal. When DHBV replication was induced, virus-harbouring cells were more susceptible to the cytotoxicity of 8-1 than non-induced cells [3].
Firzacorvir is a cyclic sulfamide compound and modulates HBV core protein. Firzacorvir has anti-HBV activity with EC50 < 1 μΜ[1].
Dihydrodehydrodiconiferyl alcohol 9-O-β-D-xylopyranoside is an anti-hepatitis B virus (anti-HBV) agent. Dihydrodehydrodiconiferyl alcohol 9-O-β-D-xylopyranoside inhibits HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) secretion on Hep G2.2.15 cell line, with IC50 values of 1.67 and >2.15 mM, respectively[1].