埃达非替尼治疗尿路上皮癌。

K. Hanna
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引用次数: 20

摘要

Erdafitinib是美国食品和药物管理局(FDA)批准的第一个口服泛成纤维细胞生长因子受体(FGFR)激酶抑制剂,与四种FGFR (FGFR-1至-4)结合,导致细胞信号传导减少和细胞凋亡。埃尔达非替尼还结合RET、集落刺激因子1受体(CSF-1R)、血小板衍生生长因子受体α和β (PDGFR-α和PDGFR-β)、fms相关酪氨酸激酶4 (FLT4)、KIT和血管内皮生长因子受体2 (VEGFR-2),显示出额外的抗肿瘤机制,导致细胞死亡。在这篇文章中,我们对erdafitinib的临床前和临床活性进行了全面的回顾,erdafitinib最近在美国被批准用于治疗局部晚期或转移性尿路上皮癌,伴有易感FGFR3/FGFR2遗传改变的成年患者,这些患者在至少一条含铂化疗期间或之后以及新辅助或辅助含铂化疗12个月内发生进展。厄达非替尼是尿路上皮癌患者的首选口服治疗方案。
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Erdafitinib to treat urothelial carcinoma.
Erdafitinib is the first Food and Drug Administration (FDA)-approved oral pan-fibroblast growth factor receptor (FGFR) kinase inhibitor that binds to four FGFRs (FGFR-1 to -4), leading to decreased cell signaling and cellular apoptosis. Erdafitinib also binds to RET, colony-stimulating factor 1 receptor (CSF-1R), platelet-derived growth factor receptor α and β (PDGFR-α and PDGFR-β), Fms-related tyrosine kinase 4 (FLT4), KIT and vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting additional antitumor mechanisms resulting in cell kill. In this article, we provide a comprehensive review of the preclinical and clinical activity of erdafitinib, which has been recently approved in the U.S. for the treatment of adult patients with locally advanced or metastatic urothelial carcinoma with susceptible FGFR3/FGFR2 genetic alterations following progression during or after at least one line of platinum-containing chemotherapy and within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy. Erdafitinib is the first oral treatment option for patients with urothelial carcinoma.
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