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厄达替尼作为转移性尿路上皮癌治疗选择的临床应用概述:我们处于何种地位。

Overview of the clinical use of erdafitinib as a treatment option for the metastatic urothelial carcinoma: where do we stand.

机构信息

Department of Biology and Biochemistry, University of Bath , Bath, UK.

Department of Health Sciences, University of Florence, Section of Pathological Anatomy, University Hospital of Florence , Florence, Italy.

出版信息

Expert Rev Clin Pharmacol. 2020 Oct;13(10):1139-1146. doi: 10.1080/17512433.2020.1823830. Epub 2020 Oct 6.

Abstract

INTRODUCTION

Erdafitinib is the first orally administered pan-fibroblast growth factor receptor (FGFR) kinase inhibitor approved by the Food and Drug Administration (FDA).

AREAS COVERED

Specifically binding to FGFR family (FGFR-1 to FGFR-4), erdafitinib leads to reduced cell signaling and cellular apoptosis. Coupled with the ability to bind to vascular endothelial growth factor 2 (VEGFR-2), KIT, Fms-related tyrosine kinase 4 (FLT4), platelet-derived growth factor receptor α and β (PDGFR-α and PDGFR-β), RET and colony-stimulating factor 1 receptor (CSF-1 R), erdafitinib has further reported antitumor features causing cell killing.

EXPERT OPINION

In this review, we provide a comprehensive overview of erdafitinib chemical structure, pharmacologic properties, and current knowledge of clinical efficacy in the treatment of locally advanced or metastatic urothelial carcinoma. This treatment, recently approved in the U.S., is available for adult patients harboring FGFR2/FGFR3 genetic alterations who progressed within 12 months of an adjuvant or neoadjuvant chemotherapy regimen including platinum or progressed during or after prior a chemotherapy regimen including platinum.

摘要

简介

厄达替尼是首个获得美国食品和药物管理局(FDA)批准的口服泛成纤维细胞生长因子受体(FGFR)激酶抑制剂。

涵盖领域

厄达替尼特异性结合 FGFR 家族(FGFR-1 至 FGFR-4),导致细胞信号转导减少和细胞凋亡。此外,它还能与血管内皮生长因子 2(VEGFR-2)、KIT、Fms 相关酪氨酸激酶 4(FLT4)、血小板衍生生长因子受体 α 和 β(PDGFR-α 和 PDGFR-β)、RET 和集落刺激因子 1 受体(CSF-1R)结合,具有进一步的抗肿瘤作用,导致细胞杀伤。

专家意见

在这篇综述中,我们全面概述了厄达替尼的化学结构、药理特性以及在治疗局部晚期或转移性尿路上皮癌方面的临床疗效的现有知识。这种治疗方法最近在美国获得批准,适用于在含铂辅助或新辅助化疗方案后 12 个月内进展或在含铂化疗方案期间或之后进展的携带 FGFR2/FGFR3 基因突变的成年患者。

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