Eaton-Peabody Laboratories, Department of Otolaryngology, Massachusetts Eye and Ear, Boston, MA, 02114, USA.
Program in Speech and Hearing Bioscience and Technology, Harvard Medical School, Boston, MA, 02115, USA.
Sci Rep. 2018 Apr 3;8(1):5437. doi: 10.1038/s41598-018-23609-7.
The computational repositioning of existing drugs represents an appealing avenue for identifying effective compounds to treat diseases with no FDA-approved pharmacotherapies. Here we present the largest meta-analysis to date of differential gene expression in human vestibular schwannoma (VS), a debilitating intracranial tumor, and use these data to inform the first application of algorithm-based drug repositioning for this tumor class. We apply an open-source computational drug repositioning platform to gene expression data from 80 patient tumors and identify eight promising FDA-approved drugs with potential for repurposing in VS. Of these eight, mifepristone, a progesterone and glucocorticoid receptor antagonist, consistently and adversely affects the morphology, metabolic activity, and proliferation of primary human VS cells and HEI-193 human schwannoma cells. Mifepristone treatment reduces VS cell viability more significantly than cells derived from patient meningiomas, while healthy human Schwann cells remain unaffected. Our data recommend a Phase II clinical trial of mifepristone in VS.
现有药物的计算重定位代表了一种有吸引力的方法,可以识别出有效化合物来治疗没有 FDA 批准的治疗方法的疾病。在这里,我们呈现了迄今为止最大的人类前庭神经鞘瘤(VS)差异基因表达的荟萃分析,这是一种使人衰弱的颅内肿瘤,并利用这些数据为该肿瘤类别中基于算法的药物重新定位的首次应用提供信息。我们将开源计算药物重定位平台应用于 80 名患者肿瘤的基因表达数据,鉴定出 8 种有希望重新用于 VS 的 FDA 批准药物。在这 8 种药物中,米非司酮是一种孕激素和糖皮质激素受体拮抗剂,它一致且不利地影响原发性人 VS 细胞和 HEI-193 人神经鞘瘤细胞的形态、代谢活性和增殖。米非司酮治疗使 VS 细胞活力降低的程度明显高于源自患者脑膜瘤的细胞,而健康的人 Schwann 细胞不受影响。我们的数据建议对 VS 进行米非司酮的 II 期临床试验。