Avaliação da atividade anti-Trypanosoma cruzi do derivado triazólico Ravuconazol utilizando o cão como modelo experimental.

摘要: Ravuconazole is an experimental triazole derivative with potent and broad-spectrum antifungal activity also very in vitro anti-Trypanosoma cruzi activity. In this work, we investigated the vivo of ravuconazole against Y Berenice-78 T. strains using acutely infected dogs as hosts. was well tolerated no significant side effects were observed during treatment 6.0 mg/kg b.i.d (12mg/kg.d.) for up to 90 days. all treated animals parasitemia permanently suppressed by first day treatment, independently parasite strain. Blood culture performed post-treatment negative animals, confirming a marked reduction load induced drug. Consistently, T.cruzi blood PCR tests one month 3/5 2/5 strain strain, respectively. Treatment led on levels anti-T. antibodies while drug pressure maintained, but after end (IgG IgG2), though not those IgG1 subclass, raising slowly without reaching same level untreated controls, indicating that clearance achieved. However, despite being unable induce parasitological cure, cardiac lesions IFN-gamma m-RNA expression tissues IL-10 mRNA increased. We conclude has suppressive curative canine model acute Chagas disease, probably due unfavorable pharmacokinetic properties (half-life 8.8 hours). man, where profile more favorable 120 hours), it be expected efficacy should higher, making promising candidate specific disease chemotherapy.