Eflornithine

Eflornithine (a-difluoromethylornithine, DFMO, ornidyl) is an irreversible suicide inhibitor of ornithine decarboxylase, which catalyzes the rate-limiting step in the biosynthesis of polyamines. Polyamines are required for cell division and normal cell differentiation. In trypanosomes, spermidine also is required for the synthesis of trypanothione, a conjugate of spermidine and glu-tathione that replaces many functions of glutathione in the parasite. Eflornithine is used to treat trypanosomiasis caused by T. brucei gambiense. The drug usually is curative even for late CNS stages of infection resistant to arsenicals but is largely ineffective for East African trypanosomiasis. Its high cost, production shortages, and difficult treatment regimen have limited use. Eflornithine is no longer available for systemic use in the U.S. but is available for treatment of Gambian trypanosomiasis by special request. The structure of eflornithine is:

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