PS-15 is a novel biguanide folate antagonist that is metabolized in vi
vo to WR99210, a metabolite that is extremely active in vitro against
multi-drug resistant strains of Plasnodium falciparum. When PS-15 was
administered in combination with sulfamethoxazole to healthy Saimiri s
ciureus monkeys, the serum antimalarial activity was considerably grea
ter than that observed in monkeys that received PS-15 alone. Further s
tudies should be carried out to determine the value of PS-15/sulfonami
de combinations in the treatment of human malaria infections and in pr
eventing the emergence of drug-resistant parasites.