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EC145: A novel targeted agent for adenocarcinoma of the lung

机译:EC145:一种针对肺腺癌的新型靶向药物

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Introduction: EC145 is a folate receptor (FR)-targeted vinca alkaloid conjugate currently under development as an anticancer agent. The FR is overexpressed on a number of major malignancies including adenocarcinoma of the lung and ovarian cancer. A companion diagnostic radiopharmaceutical, EC20, allows for non-invasive determination of the presence of functionally active FR. Areas covered: This review will discuss the rationale for the FR as a target for anticancer agents, the pharmacology of EC145 and the preclinical and clinical results for EC145 and related compounds. In addition, it will discuss the utility of a companion imaging diagnostic, EC20, for the selection of patients who might benefit from EC145. Expert opinion: EC145 is a first in class, novel agent with a unique target. The companion diagnostic, EC20 may allow for enrichment of the patient population, and therefore accelerate development of the drug. The drug has demonstrated benefit in preliminary reports of trials in ovarian cancer. If similar benefit is demonstrated in lung cancer, the drug is likely to have significant use in lung cancer and other malignancies with overexpression of FRs.
机译:简介:EC145是针对叶酸受体(FR)的长春花生物碱结合物,目前正在开发中,用作抗癌剂。 FR在许多主要的恶性肿瘤中过表达,包括肺癌和卵巢癌。伴随诊断性放射性药物EC20允许以无创方式确定功能性活性成分FR的存在。涵盖的领域:这篇综述将讨论将FR作为抗癌药靶点的基本原理,EC145的药理作用以及EC145和相关化合物的临床前和临床结果。此外,还将讨论伴随影像诊断仪EC20在选择可能受益于EC145的患者方面的实用性。专家意见:EC145是一流,新颖的代理商,具有独特的目标。伴随诊断EC20可以增加患者的数量,从而加速药物的开发。该药物已在卵巢癌试验的初步报告中显示出益处。如果在肺癌中显示出相似的益处,则该药物可能会在肺癌和FRs过表达的其他恶性肿瘤中有重要用途。

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