Antifilarial activity of oral CGP 6140 against subperiodic Brugia malayi in the leaf-monkey (Presbytis cristata)

Abstract

CGP 6140, the methyl-piperazine derivative of amoscanate was tested for its filaricidal activity against experimentally infected subperiodic Brugia malayi in the leaf-monkey, Presbytis cristata. The leaf-monkeys were each given the compound orally at 50 mg/kg body weight daily x 5 days or 25 mg/kg body weight daily x 5 days. Geometric mean microfilarial counts (GMMFC) at 5 to 8 weeks post-treatment were substantially higher than pre-treatment counts in animals in the treated and control groups. final GMMFCs compared to that of pre-treatment were 189.1% in animals given 250 mg/kg total dose, 8035.2% in those given 125 mg/kg total dose, and 15459.1% in the control group. At autopsy, 1 % of the infective dose was recovered as live adult worms from the group of animals given the higher drug dose compared to 6.5% from the control group and 9.9% in the group given the lower drug dosage. No substantial biochemical changes were observed in treated and control animals. The study showed that CGP 6140 has no microfilaricidal action, but has some adulticidal activity against subperiodic B. Vltllayi in the leaf-monkeys, at a total oral dose of 250 mg/kg.