Stibophen Explained

Stibophen is an anthelmintic originally developed by Bayer that is used as a treatment for schistosomiasis^[1] by intramuscular injection. It is classified as a trivalent antimony compound. Brand names include Fouadin/Fuadin (named in honor of Fuad I of Egypt, who had enthusiastically supported its research and development).^{[2] [3]}

Mechanism of action

Stibophen inhibits the enzyme phosphofructokinase, which the worms need for glycolysis,^[4] at least partly by binding to the sulfhydryl (–SH) group of the enzyme.^[5] Inhibiting glycolysis paralyzes the worms, which lose their hold on the wall of mesenteric veins and undergo hepatic shift, die, and are phagocytosed by liver cells.

Notes and References

1. Miller MJ, Lyon HP . Treatment of vesical schistosomiasis with stibophen . The American Journal of Tropical Medicine and Hygiene . 4 . 6 . 1049–56 . November 1955 . 13268811 . 10.4269/ajtmh.1955.4.1049 .
2. Khalil M, Betache MH . Treatment of Bilharziasis With a New Compound 'Fouadin.' . Lancet . 215 . 5553 . 234–35 . February 1930 . 10.1016/S0140-6736(00)87344-4 .
3. Williamson TV, Dodson AI . The Specific Effect of 'Fouadin' (Fuadin) on Granuloma Inguinale: Preliminary Report . JAMA . 100 . 21 . 1671–76 . May 1933 . 10.1001/jama.1933.02740210019007 .
4. Bueding E, Mansour JM . The relationship between inhibition of phosphofructokinase activity and the mode of action of trivalent organic antimonials on Schistosoma mansoni . British Journal of Pharmacology and Chemotherapy . 12 . 2 . 159–65 . June 1957 . 13446367 . 1509678 . 10.1111/j.1476-5381.1957.tb00114.x .
5. Su JG, Mansour JM, Mansour TE . Purification, kinetics and inhibition by antimonials of recombinant phosphofructokinase from Schistosoma mansoni . Molecular and Biochemical Parasitology . 81 . 2 . 171–8 . October 1996 . 8898332 . 10.1016/0166-6851(96)02702-8 . free .