TABLE 1.
Antiviral effects of PIKfyve inhibitors against influenza isolates in MDCK cells, evaluated by CPE a
| Virus strain | Apilimod mesylate | YM201636 | Ribavirin | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| IC50 (µM) | IC90 (µM) | CC50 (µM) | SI | IC50 (µM) | IC90 (µM) | CC50 (µM) | SI | IC50 (µM) | IC90 (µM) | CC50 (µM) | SI | ||
| H1N1 | A/California/07/2009 (exp1) | 9.5 | 27.8 | >54 | >5.7 | 3.0 | 21.4 | >21.4 | >7.1 | 11.1 | |||
| H1N1 | A/California/07/2009 (exp 2) | 9.2 | 31.1 | >54 | >5.9 | −b | − | − | − | 25.0 | 221.1 | >4095 | >164 |
| H1N1 | A/Hong Kong/2369/2009 | 6.1 | 22.9 | >54 | >8.9 | − | − | − | − | 28.7 | 151.5 | >4095 | >143 |
| H1N1 | A/Massachusetts/15/2013 | 10.8 | 31.1 | >54 | >5.0 | − | − | − | − | 21.7 | 118.8 | >4095 | >189 |
| H1N1 | A/Louisiana/08/2013 | 6.7 | 29.5 | >54 | >8.0 | − | − | − | − | 29.5 | 176.1 | >4095 | >139 |
| H1N1 | A/Pennsylvania/30/2009 | 24.6 | 47.5 | >54 | >2.2 | − | − | − | − | 24.6 | 139.2 | >4095 | >167 |
| H1N1 | A/Michigan/45/2015 | 10.6 | 34.4 | >54 | >5.1 | − | − | − | − | 24.6 | 86.0 | >4095 | >167 |
| H3N2 | A/Ohio/88/2012v(H3N2) | 3.8 | 18.0 | >54 | >14 | − | − | − | − | 15.6 | 86.0 | >4095 | >263 |
| H3N2 | Perth/16/2009 | 5.1 | 19.6 | >54 | >11 | 0.7 | 3.4 | >21.4 | >29 | 4.9 | 32.3 | 7272 | 1480 |
| H5N1 | Duck/MN/1525/81 | 4.7 | 19.6 | >54 | >11 | 5.6 | 14.8 | >21.4 | >3.8 | 13.5 | 73.7 | 6220 | 460 |
| FluB | Florida/4/2006 | 16.4 | 47.5 | >54 | >3.3 | >21.4 | >21.4 | >21.4 | ND | 6.1 | 33.6 | 6220 | 1013 |
a
IC50 IC90 = concentration required for 50% and 90% inhibition, respectively, CC50 = concentration to show 50% of cell death, SI: safety index = CC50/IC50.
b
"-": not done.