Description: |
A potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs; inhibits CCR5-mediated signaling events such as intracellular calcium mobilization, ERK phosphorylation, and CCR5 receptor internalization with IC50 values of 16, 3, and 1.5 nM, respectively; demonstrates anti-HIV-1 activity against R5 HIV-1 strains representing the major clades including A, B, C, D, E, F, G, and J with mean IC50 of 9 nM in PBMCs; also is a potent inhibitor of mutant HIV-1 variants that are resistant to other drugs including NRTIs, NNRTIs, PIs, and the fusion inhibitor T20.HIV InfectionPhase 1 Clinical |