TABLE 5.
Antiviral activity of ISL, TDF, AZT, 3TC, and FTC with GFP-expressing virus in PBMCs (single cycle assay)a
| HIV-1 variant | ISL |
TDF |
AZT |
3TC |
FTC |
|||||
|---|---|---|---|---|---|---|---|---|---|---|
| IC50 (nM) (n)b | FCc | IC50 (nM) (n)b | FCc | IC50 (nM) (n)b | FCc | IC50 (nM) (n)b | FCc | IC50 (nM) (n)b | FCc | |
| WT | 0.23 ± 0.04 (4) | 1 | 47.28 ± 6.77 (4) | 1 | 6.42 ± 2.37 (4) | 1 | 114.09 ± 29.10 (4) | 1 | 42.44 ± 9.18 (4) | 1 |
| A114S | 0.44 ± 0.07 (3) | 1.9 | 3.41 ± 0.64 (3) | 0.07 | 2.71 ± 0.53 (3) | 0.4 | 101.58 ± 28.03 (3) | 0.9 | 27.18 ± 7.28 (4) | 0.64 |
| M184V | 1.07 ± 0.67 (3) | 4.7 | 26.40 ± 4.13 (4) | 0.6 | 2.63 ± 0.49 (4) | 0.4 | >42,017.67 (3) | >368.3 | >42,017.67 ± 0.00 (3) | >990.0 |
| A114S/M184V | 5.70 ± 0.80 (3) | 24.8 | 1.64 ± 0.29 (3) | 0.03 | 2.46 ± 0.28 (3) | 0.4 | >42,017.67; >42,017.67 (2) | >368.3 | >42,017.67 ± 0.00 (3) | >990.0 |
a
3TC, lamivudine; AZT, zidovudine; FC, fold change; FTC, emtricitabine; HIV-1, human immunodeficiency virus type 1; IC50, half maximal inhibitory concentration; ISL, islatravir; TDF, tenofovir disoproxil fumarate; WT, wild-type.
b
IC50 (half maximal inhibitory concentration; nM) displayed as geometric mean ± standard deviation, and individual values are listed if the replicates <3.
c
FC is calculated as (IC50 against mutant isolate)/(IC50 against WT) for each test article.