Taelman H, Schechter P J, Marcelis L, Sonnet J, Kazyumba G, Dasnoy J, Haegele K D, Sjoerdsma A, Wery M
Am J Med. 1987 Mar 23;82(3 Spec No):607-14. doi: 10.1016/0002-9343(87)90107-0.
Recent studies have shown DL-alpha-difluoromethylornithine (eflornithine), an inhibitor of polyamine biosynthesis, to be curative in various Trypanosoma species infections of laboratory animals. Five patients are described with Gambian trypanosomiasis treated in Belgium with difluoromethylornithine, using various intravenous and oral dosage schedules. Three patients had late-stage and two had early-stage disease. Difluoromethylornithine treatment was associated with clearing of parasites from blood within one to four days, a trend towards normalization of all altered biologic values associated with the disease, and marked amelioration of clinical symptoms. Side effects of difluoromethylornithine, including loose stools in three patients and both anemia, and a decrease in auditory acuity in one patient, were mild, transient, and never required interruption of drug treatment. The presence of difluoromethylornithine in cerebrospinal fluid, determined in three patients, demonstrated that difluoromethylornithine penetrates into the central nervous system. In three patients, follow-up of at least 24 months after treatment demonstrated a continued healthy state without evidence of relapse. These promising, albeit preliminary, results of difluoromethylornithine therapy, even in patients with central nervous system involvement, indicate that extended clinical trials are warranted to determine the optimal dosage regimen in patients with early- and late-stage disease.
近期研究表明,多胺生物合成抑制剂DL-α-二氟甲基鸟氨酸(依氟鸟氨酸)可治愈实验动物的多种锥虫感染。本文描述了5例在比利时接受依氟鸟氨酸治疗的冈比亚锥虫病患者,采用了不同的静脉和口服给药方案。3例患者处于晚期,2例处于早期。依氟鸟氨酸治疗使患者在1至4天内血液中的寄生虫清除,所有与疾病相关的生物学指标有恢复正常的趋势,临床症状明显改善。依氟鸟氨酸的副作用包括3例患者出现腹泻,1例患者同时出现贫血和听力下降,均较轻微且短暂,从未需要中断药物治疗。对3例患者脑脊液中依氟鸟氨酸的检测表明,依氟鸟氨酸可穿透进入中枢神经系统。3例患者治疗后至少随访24个月,显示持续健康状态,无复发迹象。依氟鸟氨酸治疗的这些虽初步但有前景的结果,即使是对于中枢神经系统受累的患者,也表明有必要进行进一步的临床试验,以确定早期和晚期疾病患者的最佳给药方案。