The activity against Trypanosoma cruzi and cutaneous leishmaniasis, and toxicity, of moxipraquine (349C59).
A novel 8-aminoquinolone compound, 8(6-4' 3-hydroxybutyl)piperazin-1'-ylhexylamino)-6-methoxyquinoline di(hydrogen maleate), moxipraquine, 349C59, was shown to be active against experimental infections with Trypanosoma cruzi. It was effective in suppressing parasitaemia but did not eradicate the infection from mice or guinea-pigs. Other clinically tested drugs, including nifurtimox, were likewise incapable of eradicating the parasite from infected mice. Moxipraquine was less potent against mouse infections with strain Peru than it was against other strains of T. cruzi. In limited tests, moxipraquine was effective on experimental infections of Leishmania major, L. mexicana mexicana and L. brasiliensis panamensis but not L.b. brasiliensis. Significant foetal toxicity, observed experimentally in rats and rabbits, resulted in the termination of clinical trials.
D000634:Aminoquinolines / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D000818:Animals; D014355:Chagas Disease / Q000188:drug therapy*; D046508:Culture Techniques; D005260:Female; D005333:Fetus / Q000187:drug effects; D005664:Furazolidone / Q000627:therapeutic use; D006168:Guinea Pigs; D007896:Leishmaniasis / Q000188:drug therapy*; D007928:Lethal Dose 50; D008431:Maternal-Fetal Exchange / Q000187:drug effects; D051379:Mice; D009547:Nifurtimox / Q000627:therapeutic use; D009583:Nitrofurazone / Q000627:therapeutic use; D011247:Pregnancy; D011319:Primaquine / Q000627:therapeutic use; D011817:Rabbits; D051381:Rats; D013997:Time Factors
D000634:Aminoquinolines; D005664:Furazolidone; C027300:moxipraquine; D009547:Nifurtimox; D011319:Primaquine; D009583:Nitrofurazone