Table 1.
Relative indices of drug‐induced LQTS risk associated with repurposed drugs used for COVID‐19 treatment
| Drug name | IC50 IKr (µM) | Redfern 10 | K/Cmax a | K/Cmax freeb | Romero 13 | Colatsky 42 | CredibleMeds 12 | Long QT‐JT Index 16 | ||
|---|---|---|---|---|---|---|---|---|---|---|
| Azithromycin | 1,091 | NA | 996 | 1,993 | NA | NA | Known | Low | ||
| Chloroquine | 2.5 | CAT 4 | 2.14 | 5.48 | NA | NA | Known | Very high | ||
| Favipiravirc | 1 mM (IC10) | NA | ~6 | ~10 | NA | NA | NA | Very high | ||
| Hydroxychloroquine | 5 | NA | 3.7 | 7.3 | NA | NA | Known | Very high | ||
| Lopinavir/Ritonavir | 8.6/8.2 | NA/NA | 0.54/0.2 | 27/12 | NA | NA | Possible | Moder. | V. high | |
| Remdesivir | 28.9 | NA | 3.20 | 26.7 | NA | NA | NA | Moderate | ||
The colors used summarize among the various estimators the level of risk: very high risk (red), intermediate/moderate risk (dark yellow), slight risk (pale yellow), and low risk (green).
Cmax, peak plasma concentration; IC50, half‐maximal inhibitory concentration; IKr, rectifier cardiac potassium current; NA, not applicable.
K channel block IC50/Cmax. A value < 3 is considered at high risk of drug‐induced LQTS and a value > 30 as low risk.
K channel bloc IC50/Cmax free drug. A value < 30 is considered at high risk of drug‐induced LQTS and a value > 300 as low risk.
Calculations for the IC50 for IKr block were using 5‐times the value measured for an IC10 (8.1% diminution in IKr current).