Table 1.
DRC analysis of reference inhibitors.
| Early-phase inhibitors |
Early- and late-phase inhibitor |
Late-phase inhibitors |
|||||
|---|---|---|---|---|---|---|---|
| MyrB (nM) | MA18/07 (IU/ml) | CCC-0975 (μM) | Bay41-4109 (μM) | HID (μM) | LMV (μM) | TDF (μM) | |
| p1 infection | |||||||
| EC50 | 5.0 | 0.0008 | ~5.0 | 1.3 | >50 | >10 | >50 |
| CC50 | >50 | >50 | >10 | >20 | >50 | >10 | >50 |
| %Imax | 99 | 99 | 60 | 99 | ND | ND | ND |
| TI | >9.9 | >62,500 | >2.0 | >100 | ND | ND | ND |
| Published EC50 System PMID |
~1 HepG2-NTCP 24845614 |
ND | 10 HepDE19 22644022 |
ND | ND | ND | ND |
| p2 infection (after supernatant transfer) | |||||||
| EC50 | 1.6 | 0.00013 | ~8.0 | 0.16 | 3.1 | 0.017 | 4.0 |
| CC50 | >50 | >50 | >10 | >20 | >50 | >10 | >50 |
| %Imax | 99 | 99 | 70 | 99 | 99 | 93 | 81 |
| TI | >31.3 | >384,000 | >2.0 | >186 | >16.1 | >588 | >12.5 |
| Published EC50 System PMID |
ND | ND | ND | 202 HepG2.2.15 22162746 |
4.2 HepDES19 24858512 |
6.0 HepG2.2.15 15259898 |
1.1 HepG2.2.15 16801428 |
Calculated values of DRC regression analyses of EC50, CC50, %Imax, and TI for various classes of HBV inhibitors are represented for p1 and p2 cell infection. 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; HID, N-hydroxyisoquinolinedione; LMV, lamivudine; MyrB, myrcludex B; ND, no data; TDF, tenofovir disoproxil fumarate; Ti, therapeutic index.