Van Nieuwenhove S, Schechter P J, Declercq J, Boné G, Burke J, Sjoerdsma A
Trans R Soc Trop Med Hyg. 1985;79(5):692-8. doi: 10.1016/0035-9203(85)90195-6.
Difluoromethylornithine (DFMO), a specific, irreversible inhibitor of polyamine biosynthesis shown to be curative in animal models inoculated with various Trypanosoma spp., was evaluated in the Southern Sudan in a preliminary open clinical field trial in patients infected with Trypanosoma brucei gambiense. 20 patients were studied including 18 with late-stage disease involving the central nervous system, 16 of whom were refractory to arsenical treatment. In late-stage disease monotherapy with oral DFMO doses of about 400 mg/kg/day for five to six weeks was associated with disappearance of parasites from cerebrospinal fluid (CSF), decreased CSF WBC counts and protein concentrations and reversal of clinical signs. Side effects associated with this dose regimen included diarrhoea, abdominal discomfort and anaemia, but were seldom sufficiently severe to prompt discontinuing therapy. In early-stage patients about 200 mg/kg/day for six weeks appears adequate to eliminate parasites and reverse clinical symptoms and is well tolerated. Three cases of late-stage sleeping sickness and two of early-stage disease followed up for approximately one and a half to two years after treatment indicated that DFMO monotherapy can be curative. Additional studies are needed to define optimal posology. Inhibition of polyamine biosynthesis is a promising new approach to therapy of trypanosomiasis.
二氟甲基鸟氨酸(DFMO)是一种特异性、不可逆的多胺生物合成抑制剂,在接种了各种锥虫属的动物模型中显示出有治愈效果。在苏丹南部,对感染布氏冈比亚锥虫的患者进行了一项初步开放性临床现场试验,对DFMO进行了评估。研究了20名患者,其中18名患有累及中枢神经系统的晚期疾病,其中16名对砷剂治疗无效。在晚期疾病中,口服DFMO剂量约为400mg/kg/天,持续五至六周的单一疗法与脑脊液(CSF)中寄生虫消失、CSF白细胞计数和蛋白质浓度降低以及临床体征逆转相关。与该剂量方案相关的副作用包括腹泻、腹部不适和贫血,但很少严重到促使停止治疗。在早期患者中,约200mg/kg/天,持续六周似乎足以消除寄生虫并逆转临床症状,且耐受性良好。三例晚期昏睡病患者和两例早期疾病患者在治疗后随访了大约一年半到两年,表明DFMO单一疗法可以治愈。需要进一步研究来确定最佳剂量。抑制多胺生物合成是治疗锥虫病的一种有前景的新方法。