A quinoline methanol (WR 30090) for treatment of acute malaria.
WR 30090 at a dose of 230 mg every 8 hr for 6 days has proven to be a safe, well-tolerated compound with photosensitivity proving to be a minor consideration. WR 30090 was found to be an effective medication for the treatment of acute malaria caused by several strains of Plasmodium falciparum. At the dose of 230 mg every 8 hr for 6 days, all of six men infected with a chloroquine-susceptible strain (Uganda I) were cured, all of 13 subjects infected with moderately chloroquine-resistant strains (Malayan Camp, Malayan Taylor, and Philippine Per) were cured, and 19 of 23 subjects infected with strains highly resistant to chloroquine (Vietnam Smith and Vietnam Crocker) were cured. All of five subjects infected with the chloroquine-resistant Vietnam Marks strain were cured with only 3 days of therapy. Blood-induced P. vivax (Chesson strain) infection showed a mixed response. Six out of seven volunteers were cured when treated for 3 days with WR 30090. The one recrudescence responded to a repeated course of therapy for 3 days. However, recrudescence occurred in one volunteer treated for 6 days. Treatment with WR 30090 failed to cure sporozoite-induced P. vivax (Chesson strain) infection in any of four subjects. In all subjects treated, there was good suppression of parasitemia and relief of symptoms. The susceptibility of the strains of malaria to WR 30090 to some degree parallels their susceptibility to chloroquine.
D000962:Antimalarials / Q000009:adverse effects / Q000627:therapeutic use*; D002082:Butylamines / Q000009:adverse effects / Q000627:therapeutic use; D006801:Humans; D007214:Indonesia; D008288:Malaria / Q000188:drug therapy*; D000432:Methanol / Q000009:adverse effects / Q000627:therapeutic use; D010679:Philippines; D010963:Plasmodium falciparum / Q000145:classification*; D011804:Quinolines / Q000009:adverse effects / Q000627:therapeutic use*; D014454:Uganda; D014744:Vietnam
D000962:Antimalarials; D002082:Butylamines; D011804:Quinolines; D000432:Methanol