Rafii Michael S, Skotko Brian G, McDonough Mary Ellen, Pulsifer Margaret, Evans Casey, Doran Eric, Muranevici Gabriela, Kesslak Patrick, Abushakra Susan, Lott Ira T
Alzheimer's Therapeutic Research Institute (ATRI) at University of Southern California, San Diego, CA, USA.
Department of Neurosciences, University of California, San Diego, CA, USA.
J Alzheimers Dis. 2017;58(2):401-411. doi: 10.3233/JAD-160965.
ELND005 (scyllo-Inositol; cyclohexane-1,2,3,4,5,6-hexol) has been evaluated as a potential disease-modifying treatment for Alzheimer's disease (AD). Individuals with Down syndrome (DS) have an increased risk for developing AD dementia.
To evaluate the safety and tolerability of ELND005 and to determine its pharmacokinetics (PK) and relationship between PK parameters, safety outcome measures, and exploratory efficacy outcome measures in young adults with DS without dementia.
This was a prospective, randomized, double-blind, placebo-controlled, parallel-group, three-arm, multicenter Phase II study of the safety and pharmacokinetics of ELND005 administered orally for 4 weeks (ClinicalTrials.gov NCT01791725). Participants who met study eligibility criteria were randomly assigned in a 2 : 1:1 ratio to receive ELND005 at either 250 mg twice daily (BID) or 250 mg once daily (QD) or matching placebo for 4 weeks.
There were no apparent treatment group-related trends on cognitive or behavioral measures and there were no SAEs and no deaths in the study. Overall, mean changes from baseline in clinical laboratory parameters, vital sign measurements, electrocardiogram results, and other physical findings were unremarkable. ELND005 accumulation averaged approximately 2-fold with QD dosing, and 3- to 4-fold with BID dosing.
Overall, treatment of adults with DS with ELND005 at both doses was well tolerated, achieved measurable blood levels and demonstrated no safety findings. Further studies will be needed to test efficacy.
ELND005( scyllo-肌醇;环己烷-1,2,3,4,5,6-己醇)已被评估为治疗阿尔茨海默病(AD)的一种潜在的疾病修饰疗法。唐氏综合征(DS)患者患AD痴呆症的风险增加。
评估ELND005的安全性和耐受性,并确定其药代动力学(PK)以及在无痴呆的年轻DS成年人中PK参数、安全性结局指标和探索性疗效结局指标之间的关系。
这是一项前瞻性、随机、双盲、安慰剂对照、平行组、三臂、多中心II期研究,旨在评估口服ELND005 4周的安全性和药代动力学(ClinicalTrials.gov NCT01791725)。符合研究纳入标准的参与者按2∶1∶1的比例随机分配,接受每日两次250mg或每日一次250mg的ELND005或匹配的安慰剂治疗4周。
在认知或行为指标方面没有明显的与治疗组相关的趋势,研究中没有严重不良事件(SAE),也没有死亡。总体而言,临床实验室参数、生命体征测量、心电图结果和其他体格检查结果与基线相比的平均变化不显著。每日一次给药时ELND005的蓄积平均约为2倍,每日两次给药时为3至4倍。
总体而言,DS成年患者使用两种剂量的ELND005治疗耐受性良好,达到了可测量的血药浓度,且未发现安全性问题。需要进一步研究来测试其疗效。