Stibophen is a potent antiparasitic agent effective against Litomosoides carinii, Dipetalonema witei, and Brugia pahangi. It inhibits lactate accumulation and phosphofructokinase (PFK) activity in adult filarial worms. Additionally, Stibophen suppresses PFK activity in Ascaris and Hymenolepis diminuta, without affecting mammalian liver PFK. It is utilized in studies of schistosomiasis and filarial infections.

Stibophen (0-2×10^-3 M) demonstrates potent inhibition of PFK activity in filarial homogenates at a concentration of 2×10^-5 M, whereas the sensitivity in Syrian hamster liver PFK is approximately 1000 times lower. Stibophen (1.6×10^-4 M; 30 minutes) reduces lactate production in whole filarial parasites, achieving about 40% inhibition for B. pahangi, D. witei, and L. carinii. Administered at concentrations between 1.6×10^-5 and 1.6×10^-4 M for 75 minutes, Stibophen induces the accumulation of hexose phosphates (G-6-P and F-6-P) within whole filarial parasites, concurrent with reduced levels of fructose-1,6-bisphosphate, suggesting PFK inhibition. At 1.6×10^-4 M over 1 hour, Stibophen inhibits lactate production from glucose and fructose-1,6-bisphosphate (FDP) in filarial homogenates; however, aldolase can reverse the FDP-dependent inhibition. Within the range of 1.6×10^-5 to 5×10^-3 M, Stibophen strongly inhibits PFK and aldolase in filarial homogenates. Stibophen (1.6×10^-4 M) inhibits PFK activity in worm homogenates but does not affect rat liver preparations, indicating selective toxicity towards parasite enzymes.