Differences in polyamine metabolism between parasites and their vertebrate hosts have been exploited to develop new drugs specifically designed to control the extension of proliferative processes (infectious, parasitic and neoplasic). Since 1990 the irreversible inhibitor of ornithine decarboxylase, α-difluoromethylornithine (DFMO) was included in the pharmacopea of African trypanosomiasis (sleeping sickness) against early and late CNS disease. Pentamidine, a cationic diamidine, is used as second line drug against trypanosomiasis and leishmaniasis. Due to its polyamine resembling structure, pentamidine interferes in spermidine biosynthesis and polyamine uptake in the parasite cell, and displaces spermidine from macromolecules. More potent diamidines are now under trial. CGP040215A a pentamidine analog, has shown good biochemical profiles, and phase I trials are going on. This review offers a general scope on the work done about this subject.
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