Table 3.
DRC analysis of reference inhibitors and confirmed novel early and late HBV life cycle inhibitors.
| Early HBV life cycle inhibitors |
Late HBV life cycle inhibitors |
|||||
|---|---|---|---|---|---|---|
| MyrB | Pranlukast | Cytochalasin D | Lamivudine | Fludarabine | Dexmedetomidine | |
| EC50 (μM) | 0.005 | 4.3 | 0.07 | 0.02 | 0.1 | 6.23 |
| CC50 (μM) | >0.8 | >50 | 1.4 | >10 | 13.4 | >50 |
| Imax (%) | 99 | 92 | 86 | 98 | 96 | 82 |
| TI | >10 | >12 | 20 | >333 | >117 | >8.0 |
| Published EC50 (μM) | 0.001–0.005 | No | No | 0.006–0.03 | No | No |
| Cellular target, drug use | HBV entry/NTCP inhibitor | Leukotriene receptor-1 antagonist, bronchospasm | Actin polymerisation inhibitor | Cytidine analogue, antiviral (HBV, HIV) | Purine analogue, blood cancer therapy | A2 adrenergic agonist |
| HBV proposed MoA | HBV–NTCP binding | HBV–NTCP binding | Actin-dependent HBV internalisation | HBV pol (RT) | HBV RT DNA synthesis | NR |
Calculated values of DRC regression analyses of EC50, CC50, %Imax, and TI for various classes of HBV inhibitors are presented. Information on EC50 values obtained in different published cell culture systems are provided. %Imax, percent maximum inhibition; CC50, 50% cytotoxic concentration; DRC, dose–response curve; MoA, mechanism of action; MyrB, myrcludex B; NR, not reported; NTCP, sodium taurocholate cotransporting polypeptide; RT, reverse transcription; TI, therapeutic index.