Nelfinavir

Abstract

▴ Nelfinavir is a protease inhibitor which shows good inhibitory activity against HIV-1. The pattern of HIV-1 resistance to nelfinavir is different from that seen with other protease inhibitors. ▴ In healthy male volunteers, administration of single 400 and 800mg doses of nelfinavir with food resulted in area under the plasma concentration-time curve values that were 27 to 50% higher than those achieved in fasted volunteers who received the same doses of the drug. ▴ Reductions in plasma HIV RNA to below detectable levels (detection limit 500 copies/ml) were achieved in some patients (number not reported) after 28 days’ treatment with nelfinavir 500, 600 or 750mg twice daily, or 500, 750 or 1000mg 3 times daily. ▴ Combination therapy with nelfinavir and stavudine produced greater reductions in plasma HIV RNA levels than stavudine monotherapy in patients who had not previously received stavudine treatment; mean increases in CD4+ cell counts were also greater in the combination treatment group than in monotherapy recipients. ▴ Plasma HIV RNA decreased to below detectable levels in 11 of 12 patients with early onset HIV infection who received a triple regimen of nelfinavir, zidovudine and lamivudine for 16 weeks.