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Therapeutic Trials of a Dihydroxynaphthalene (377C54) Against Plasmodium Falciparum and Plasmodium Vivax Infections in Human Volunteers

Burroughs-Wellcome 377C54 was tested for therapeutic efficacy against 3 strains of Plasmodium falciparum (S. Rhodesian, Colombian, Thai) and the Chesson strain of P. vivax. The dosage regimen was 300 mg every 12 hours for 4 doses; i.e., a total of 1200 mg in 36 hours.

Of 14 volunteers with falciparum malaria given an initial treatment with this drug, only 4 were cleared of parasites in the circulating blood. All 4 experienced a reappearance of parasites in 6 to 21 days after treatment.

All 15 volunteers with vivax infections, whether induced by sporozoites (mosquito bite) or the intravenous inoculation of parasitized blood, had parasites removed from the circulating blood in from 2 to 4 days, with a median of 3 days. Parasites reappeared in all but 2 of the 15 in from 10 to 39 days. Of interest is the fact that 2 of the recurrences were in blood-induced infections, which indicates inadequate therapy.

It would appear from these results that this compound, even in the high-dosage regimen used here, is not as efficacious as chloroquine or other commonly employed antimalarials.