Jc. Craig et al., ANTIVIRAL SYNERGY BETWEEN INHIBITORS OF HIV PROTEINASE AND REVERSE-TRANSCRIPTASE, Antiviral chemistry & chemotherapy, 4(3), 1993, pp. 161-166
Ro 31-8959, a potent and specific inhibitor of HIV proteinases, is sho
wn to interact synergistically in combination with nucleoside analogue
inhibitors of HIV reverse transcriptase (AZT, ddC, 2'-FddC). Ninety p
er cent inhibition endpoints (IC90), obtained from checkerboard titrat
ions of compound mixtures on CEM-T4 cells infected with HIV-1 strain G
B8, have been further analysed. Compared with concentrations needed wh
en inhibitors are used individually, reductions of between 2- and 30-f
old were observed in combination, depending on the nucleoside analogue
and the ratio of concentrations employed. The results suggest that co
mbinations of AZT or ddC with Ro 31-8959 should be considered for deve
lopment as candidate antiviral treatments of patients with HIV infecti
on.