TABLE 2.
Antiviral potency of ruxolitinib and tofacitinib against various NRTI-resistant HIV-1 strains in primary human lymphocytes
| HIV strain or mutant virus | Antiviral potency (EC50/EC90)a |
||||||||
|---|---|---|---|---|---|---|---|---|---|
| AZT | (−)−FTC | 3TC | Tofacitinib | Ruxolitinib | d4T | ddI | EFV | TDF | |
| xxLAI | 0.03 ± 0.007/0.1 ± 0.08 | 0.09 ± 0.02/0.8 ± 0.4 | 0.8 ± 0.4/3.1 ± 1.2 | 2.6 ± 1.3/28.4 ± 16.7 | 0.3 ± 0.3/6.1 ± 7.6 | 1.0 ± 0.5/6.4 ± 0.4 | 11.5 ± 6.6/55.4 ± 23.0 | 0.02 ± 0.03/0.2 ± 0.3 | 0.2 ± 0.2/0.9 ± 0.8 |
| M184V | 0.01 ± 0.02/0.02 ± 0.01 | 10.1 ± 7.3/41.3 ± 29.3 | >10/>10 | 1.6 ± 0.7/27.1 ± 15.7 | 0.3 ± 0.3/3.2 ± 2.3 | 0.6 ± 0.8/2.6 ± 2.5 | 11.5 ± 9.1/44.9 ± 26.2 | 0.01 ± 0.006/0.08 ± 0.08 | 0.09 ± 0.03/0.5 ± 0.3 |
| K65R | 0.04 ± 0.02/0.3 ± 0.1 | 0.5 ± 0.4/2.4 ± 1.4 | 2.5 ± 3.0/6.0 ± 5.3 | 1.8 ± 0.8/81.2 ± 26.7 | 0.2 ± 0.3/8.5 ± 8.1 | 1.5 ± 0.6/7.9 ± 0.3 | 21.2 ± 18.3/86.7 ± 0.8 | 0.007/0.02 ± 0.01 | 0.4 ± 0.1/1.6 ± 0.5 |
| L74V | 0.02 ± 0.02/0.2 ± 0.1 | 0.2 ± 0.2/1.3 ± 1.0 | 0.6 ± 0.8/2.9 ± 2.9 | 0.9 ± 1.0/47.7 ± 45.3 | 0.1 ± 0.2/3.2 ± 2.6 | 0.9 ± 0.8/9.8 ± 2.4 | 13.2 ± 8.5/80.9 ± 16.6 | 0.06 ± 0.07/0.2 ± 0.3 | 0.2 ± 0.1/0.2 ± 0.1 |
| A62V/V75I/F77L/F116Y/Q151M | 4.6 ± 7.7/41.2 ± 50.2 | 0.4 ± 0.3/2.1 ± 1.6 | 0.5 ± 0.7/2.7 ± 1.7 | 0.2 ± 0.2/8.9 ± 8.8 | 0.03 ± 0.02/1.5 ± 1.5 | 6.8 ± 5.7/70.3 ± 51.4 | 40.5 ± 52.1/83.5 ± 28.6 | 0.2 ± 0.3/0.44 ± 0.6 | 0.7 ± 0.8/3.6 ± 2.2 |
| 4×AZT (D67N/K70R/T215Y/K219Q) | 0.1 ± 0.1/53.3 ± 66.1 | 0.2 ± 0.1/1.2 ± 0.1 | 0.7 ± 0.8/3.4 ± 1.1 | 0.3 ± 0.2/17.1 ± 4.5 | 0.09 ± 0.1/2.4 ± 2.0 | 27.8 ± 37.1/53.2 ± 66.3 | 35.5 ± 31.0/77.1 ± 32.4 | 0.07 ± 0.04/0.2 ± 0.2 | 0.2 ± 0.3/1.2 ± 1.1 |
a
Data are means and standard deviations calculated from at least four independent experiments, with pooled cells from eight donors and duplicates in each experiment.