Molecular Parasitology, Lindsey F. Kimball Research Institute, New York Blood Center, New York, New York, United States of America.
Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, California, United States of America.
PLoS Negl Trop Dis. 2021 Feb 18;15(2):e0009064. doi: 10.1371/journal.pntd.0009064. eCollection 2021 Feb.
Several issues have been identified with the current programs for the elimination of onchocerciasis that target only transmission by using mass drug administration (MDA) of the drug ivermectin. Alternative and/or complementary treatment regimens as part of a more comprehensive strategy to eliminate onchocerciasis are needed. We posit that the addition of "prophylactic" drugs or therapeutic drugs that can be utilized in a prophylactic strategy to the toolbox of present microfilaricidal drugs and/or future macrofilaricidal treatment regimens will not only improve the chances of meeting the elimination goals but may hasten the time to elimination and also will support achieving a sustained elimination of onchocerciasis. These "prophylactic" drugs will target the infective third- (L3) and fourth-stage (L4) larvae of Onchocerca volvulus and consequently prevent the establishment of new infections not only in uninfected individuals but also in already infected individuals and thus reduce the overall adult worm burden and transmission. Importantly, an effective prophylactic treatment regimen can utilize drugs that are already part of the onchocerciasis elimination program (ivermectin), those being considered for MDA (moxidectin), and/or the potential macrofilaricidal drugs (oxfendazole and emodepside) currently under clinical development. Prophylaxis of onchocerciasis is not a new concept. We present new data showing that these drugs can inhibit L3 molting and/or inhibit motility of L4 at IC50 and IC90 that are covered by the concentration of these drugs in plasma based on the corresponding pharmacological profiles obtained in human clinical trials when these drugs were tested using various doses for the therapeutic treatments of various helminth infections.
目前针对传播的控制措施(即采用大规模药物治疗,简称 MDA),仅以伊维菌素为药物来消除盘尾丝虫病,但这一方案存在若干问题。作为消除盘尾丝虫病的更全面策略的一部分,需要替代和/或补充治疗方案。我们假设在目前的杀微丝蚴药物和/或未来的杀成虫治疗方案的工具包中添加“预防性”药物或可用于预防性策略的治疗性药物,不仅将提高实现消除目标的机会,还可能加速消除时间,并且还将支持实现盘尾丝虫病的持续消除。这些“预防性”药物将针对盘尾丝虫的感染性第三期(L3)和第四期(L4)幼虫,从而不仅可以预防未感染者,还可以预防已感染者建立新的感染,从而减少成虫总负荷和传播。重要的是,有效的预防性治疗方案可以利用已纳入盘尾丝虫病消除方案的药物(伊维菌素)、正考虑用于 MDA 的药物(莫昔克丁)和/或正在临床开发的潜在杀成虫药物(奥芬达唑和埃莫司汀)。盘尾丝虫病的预防并不是一个新概念。我们提供了新的数据,表明这些药物可以抑制 L3 蜕皮和/或在 IC50 和 IC90 抑制 L4 的运动,这些 IC50 和 IC90 涵盖了这些药物在血浆中的浓度,这些浓度基于在人体临床试验中获得的相应药理学特征,这些药物在用于治疗各种寄生虫感染的各种剂量时进行了测试。