Translational Laboratory in Genetic Medicine, Agency for Science, Technology and Research, Singapore (A*STAR), Singapore.
Teva Pharmaceutical Industries Ltd., Petach Tikva, Israel.
JCI Insight. 2017 Dec 7;2(23):95665. doi: 10.1172/jci.insight.95665.
Pridopidine is currently under clinical development for Huntington disease (HD), with on-going studies to better characterize its therapeutic benefit and mode of action. Pridopidine was administered either prior to the appearance of disease phenotypes or in advanced stages of disease in the YAC128 mouse model of HD. In the early treatment cohort, animals received 0, 10, or 30 mg/kg pridopidine for a period of 10.5 months. In the late treatment cohort, animals were treated for 8 weeks with 0 mg/kg or an escalating dose of pridopidine (10 to 30 mg/kg over 3 weeks). Early treatment improved motor coordination and reduced anxiety- and depressive-like phenotypes in YAC128 mice, but it did not rescue striatal and corpus callosum atrophy. Late treatment, conversely, only improved depressive-like symptoms. RNA-seq analysis revealed that early pridopidine treatment reversed striatal transcriptional deficits, upregulating disease-specific genes that are known to be downregulated during HD, a finding that is experimentally confirmed herein. This suggests that pridopidine exerts beneficial effects at the transcriptional level. Taken together, our findings support continued clinical development of pridopidine for HD, particularly in the early stages of disease, and provide valuable insight into the potential therapeutic mode of action of pridopidine.
普里多吡啶目前正在进行亨廷顿病 (HD) 的临床开发,正在进行研究以更好地描述其治疗效果和作用模式。普里多吡啶在疾病表型出现之前或在 YAC128 亨廷顿病小鼠模型的疾病晚期给药。在早期治疗队列中,动物接受 0、10 或 30 mg/kg 普里多吡啶治疗 10.5 个月。在晚期治疗队列中,动物接受 0 mg/kg 或递增剂量的普里多吡啶(10 至 30 mg/kg 分 3 周给予)治疗 8 周。早期治疗改善了 YAC128 小鼠的运动协调能力,并减少了焦虑和抑郁样表型,但未能挽救纹状体和胼胝体萎缩。相反,晚期治疗仅改善了抑郁样症状。RNA-seq 分析显示,早期普里多吡啶治疗逆转了纹状体转录缺陷,上调了已知在 HD 期间下调的疾病特异性基因,这一发现在此实验中得到了证实。这表明普里多吡啶在转录水平发挥有益作用。总之,我们的发现支持继续开发普里多吡啶治疗 HD,特别是在疾病的早期阶段,并为普里多吡啶的潜在治疗作用模式提供了有价值的见解。