Vicriviroc maleate is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM. It also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
- Potent, selective, and oral bioavailable inhibitor of CCR5.
- Inhibits HIV-1 in PBMC cells.
- Demonstrates a mean IC50 and IC90 of 0.45 nM and 4 nM for a panel of HIV isolates.
- Exhibits good oral availability in rats and monkeys.
- No acute CNS or GI effects observed in rats.
- Shows weak activity against hERG (IC50, 5.8 μM).
- Inhibits chemotactic response to MIP-1α.
- Suppresses RANTES-induced signaling.
- Potently suppresses all tested viral isolates.