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[摘要]：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. |
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