Development of everolimus, a novel oral mTOR inhibitor, across a spectrum of diseases
Development of everolimus, a novel oral mTOR inhibitor, across a spectrum of diseases
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DOI：
10.1111/nyas.12122
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发表时间：
2013-01-01
期刊：
影响因子：
--
通讯作者：
Berg, William
中科院分区：
文献类型：
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作者：
Lebwohl, David;Anak, Oezlem;Berg, William
依维莫司是一种有效的口服雷帕霉素哺乳动物靶蛋白（mTOR）抑制剂，自1996年以来已在多个临床开发项目中进行了研究。学术和制药专家之间的独特合作促进了研究的快速进展，同时发现了多种肿瘤类型的适应症。依维莫司最初开发用于预防器官移植排斥反应，已证明其治疗各种类型癌症（肾细胞癌、胰腺源性神经内分泌肿瘤和乳腺癌）患者以及成人和儿童结节性硬化症患者的有效性和安全性。FDA批准依维莫司用于这些疾病已经解决了几个未满足的医疗需求，并被治疗选择可能有限的医学界广泛接受。正在进行一项广泛的临床开发计划，以确定依维莫司作为单药治疗或与其他药物联合治疗广谱恶性肿瘤的作用。
Everolimus is a potent, oral inhibitor of the mammalian target of rapamycin (mTOR) that has been investigated in multiple clinical development programs since 1996. A unique collaboration between academic and pharmaceutical experts fostered research that progressed rapidly, with simultaneous indication findings across numerous tumor types. Initially developed for the prophylaxis of organ transplant rejection, everolimus has demonstrated efficacy and safety for the treatment of patients with various types of cancer (renal cell carcinoma, neuroendocrine tumors of pancreatic origin, and breast cancer) and for adult and pediatric patients with tuberous sclerosis complex. The FDA approval of everolimus for these diseases has addressed several unmet medical needs and is widely accepted by the medical community where treatment options may be limited. An extensive clinical development program is ongoing to establish the role of everolimus as monotherapy, or in combination with other agents, in the treatment of a broad spectrum of malignancies.