DPC 684 is a potent and selective HIV-1 protease inhibitor with an IC90 of 5.7-40 nM and a Ki of 0.021 nM. It competitively inhibits HIV-1 protease, preventing viral polyprotein cleavage. Compared to cellular proteases, DPC 684 shows high selectivity for retroviral proteases. The compound exhibits low protein binding and offers broad-spectrum inhibition against various wild-type and mutant HIV-1 proteases, with an IC90 of 1.9-6.3 nM. DPC 684 is significant for HIV research.

HIV-1:0.021 nM (Ki)

DPC 684 (Compound DPC 684) exhibits broad-spectrum anti-HIV-1 activity, with an average concentration of 14.5 nM needed for 90% inhibition of viral replication in various cell models (MT-2: HIV-1 RF, IIIB strains, PBMC: HIV-1 IIIB, NL4-3 strains). The antiviral activity against both laboratory and clinical isolates is as follows: [IC 90: RF at 5.7 nM, 7.8 nM; HXB2 at 12 nM; NL4-3 at 20 nM; IIIB at 8.8 nM, 40 nM; Thai 9466 and Patient E at 11 nM; HIV-2 at 32 nM]. In MT-2 cells, DPC 684 remains effective against common clinical resistance mutations, maintaining an IC 90 of 8.8 with the D30N mutation without loss of potency. Under multiple mutations, the IC 90 is 26, indicating a twofold reduction in efficacy. At a concentration of 13 μM, DPC 684 shows no significant inhibition of 17 human proteases, including renin and pepsin, confirming its high selectivity for HIV protease.

DPC 684 (Compound DPC 684) demonstrated histological changes in the liver of rats and mild first-degree atrioventricular block in dogs during a 2-week safety assessment study. These findings indicate the need to closely monitor these target organs for potential risks in future research.