Preliminary Clinical Trials with Hycanthone, a new Antischistosomal Agent

Naftale Katz Instituto Nacional de Endemias Ruais, Hospital da Polićia Militar and Departamento de Clínica Médica, Faculdade de Medicine, Belo Horizonte, Brazil

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J. Pellegrino Instituto Nacional de Endemias Ruais, Hospital da Polićia Militar and Departamento de Clínica Médica, Faculdade de Medicine, Belo Horizonte, Brazil

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M. T. Ferreira Instituto Nacional de Endemias Ruais, Hospital da Polićia Militar and Departamento de Clínica Médica, Faculdade de Medicine, Belo Horizonte, Brazil

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C. A. Oliveira Instituto Nacional de Endemias Ruais, Hospital da Polićia Militar and Departamento de Clínica Médica, Faculdade de Medicine, Belo Horizonte, Brazil

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C. B. Dias Instituto Nacional de Endemias Ruais, Hospital da Polićia Militar and Departamento de Clínica Médica, Faculdade de Medicine, Belo Horizonte, Brazil

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Summary

From Miracil D® (lucanthone), a hydroxymethyl derivative (hycanthone), can be obtained through the biological activity of the microorganism spergillus sclerotiorum. This compound was claimed to be the antischistosomal metabolite of Miracil D and was found very active when administered to mice, hamsters, and Cebus monkeys experimentally infected with Schistosoma mansoni.

Clinical trials with hycanthone were performed on 52 patients with active schistosomiasis mansoni. The drug was administered, per os, at the dosage levels of 2 and 3 mg per kg per day with an antacid preparation, twice a day, for 5 consecutive days. In all but two patients treatment could be completed. Nausea, vomiting, anorexia, vertigo, and headache were the commonest side-effects. Therapeutic activity could be evaluated in 44 cases by repeated stool examination (four to six) or by one rectal biopsy performed at least 4 months after treatment, or by both. The percentages of patients considered as cured were 83.3 and 80.0 for the schedules of 2 and 3 mg per kg, respectively.

Laboratory and clinical data on the antischistosomal activity of hycanthone obtained so far emphasize the need for further clinical trials with this compound.

Author Notes

Instituto Nacional de Endemias Rurais, C. Postal 1743, Belo Horizonte, Brazil.

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