TABLE 1.
Inhibition of recombinant HIV integrase and HIV replication by GSK1265744
| INSTIa | Integrase inhibition, strand transfer IC50 (nM) | Antiviral activity |
|||
|---|---|---|---|---|---|
| PBMC EC50 (nM) | Potency shift with 100% HS (FC)b | PA-EC50 (nM) | PA-EC90 (nM) | ||
| GSK1265744 | 3.0 | 0.25c | 408 | 102 | 408 |
| Dolutegravir | 2.7 | 0.51 | 75 | 38 | 152 |
| Raltegravir | 3.3 | 2.0 | 4.7 | 5.6 | 23 |
| Elvitegravir | 6 | 2.0 | 22 | 20 | 78 |
a
Data for dolutegravir, raltegravir, and elvitegravir are from reference 14.
b
Protein-binding fold shift (FC, fold change) was estimated from antiviral activity with various concentrations of human serum and extrapolated to a 100% human serum condition.
c
Mean from 11 experiments with HIV-1 strain Ba-L and 5 experiments with HIV-1 NL432.