Quinfamide

Quinfamide (WIN-40014) is an orally active class of dichloroacetyl derivative with significant anti-intestinal protozoan, particularly mmoeba histolytica activity. Quinfamide exhibits antiamoebic activity under solvent-free conditions with an IC₅₀ of 28.15 μg/mL in a suspension condition. Quinfamide particles are actively engulfed by the amoebas, then cells are affected, and finally, amoebas are killed and lysed, and this process directly relies on the physical intake of the drug particles. Quinfamide can be used in the research of tropical parasitic infections such as amoebiasis and helminthiasis^[1][2][3]. In Vitro:Quinfamide inhibits propagation of E. histolytica in vitro at a concentration of 20 μg/mL^[2].
Quinfamide (0-72 h) granules are actively engulfed by the amoeba, and subsequently the amoeba's trophozoite cells become round, lose their motility, undergo cell lysis, and the integrity of the cell membrane is lost^[3].
Quinfamide has an IC₅₀ value against pathogenic strain of Trichomonas vaginalis (strain GT-13) of 214.7 μg/mL^[3].
In Vivo:Quinfamide (30 mg/kg, p.o., prepared as small pellets and mixed with feed, for 49 days) possesses a low anticoccidial efficacy, this is noticeably improved when prepared as pellets with Carbopol^[1].
Quinfamide (p.o.) exhibits ED₅₀ values against E. cricetid of 0.25 mg/kg/day (total dose 0.75 mg/kg) in multiple doses for 3 days and 0.9 mg/kg after a single dose^[2].
Quinfamide (p.o.) protect hamsters from re-infection with E. cricetid and has no significant toxicity in rodents (10 g/kg, single dose), monkeys (500 mg/kg, for 37 days), dogs (2 g/kg, single dose) and rats (500 mg/kg, for 31 days)^[2].