TABLE 1.
Antiviral activity of AMD3451 against HIV strains in different cell linesa
| Strain | Phenotype (coreceptor use) | Cell type | AMD3451 IC50 (μM) |
|---|---|---|---|
| HIV-1 ADA | R5 | PBMC | 6.0 |
| HIV-1 BaL | R5 | HOS.CD4.CCR5 | 8.3 |
| U87.CD4.CCR5 | 17.6 | ||
| M/M | 23.9 | ||
| HIV-1 IIIB | X4 | MT-4 | 1.2 |
| HOS.CD4.CXCR4 | 3.2 | ||
| HIV-1 NL4.3 | X4 | MT-4 | 1.8 |
| HOS.CD4.CXCR4 | 6.9 | ||
| U87.CD4.CXCR4 | 17.6 | ||
| PBMC | 3.0 | ||
| HIV-1 | |||
| NL4.3AMD3100res | X4 | MT-4 | 9.7 |
| HIV-1 NL4.3CXCL12res | X4 | MT-4 | 6.1 |
| HIV-1 HE | R3, R5, X4 | MT-4 | 26.5 |
| HOS.CD4.CXCR4 | 7.9 | ||
| HOS.CD4.CCR5 | 6.1 | ||
| U87.CD4.CCR3 | >40 | ||
| HIV-2 ROD | R3, R5, X4 | MT-4 | 9.0 |
| U87.CD4.CCR3 | >40 |
a
Effect of AMD3451 on the replication of HIV strains in different cell lines, PHA-stimulated PBMCs, and M/M. The virus yield was monitored in the cell-free supernatant 4 to 14 days after infection by viral p24 HIV-1 Ag or p27 HIV-2 Ag ELISA. Results represent mean values of the results from at least three separate experiments. The phenotypes (coreceptor use) of the viruses were determined for their ability to replicate in U87.CD4 cells transfected with CCR3, CCR5, or CXCR4. The data shown are the mean IC50 of the results from at least three separate experiments.