Benjamin David J, Mita Alain C
Hoag Family Cancer Institute, 1 Hoag Drive, Building 41, Newport Beach, CA, 92663, USA.
Target Oncol. 2025 Jan;20(1):1-11. doi: 10.1007/s11523-024-01119-z. Epub 2024 Dec 17.
Fibroblast growth factor receptor (FGFR) 2/3 alterations have been implicated in tumorigenesis in several malignancies, including urothelial carcinoma. Several FGFR inhibitors have been studied or are in development, and erdafitinib is the sole inhibitor to achieve regulatory approval. Given the rapidly evolving treatment landscape for advanced urothelial carcinoma, including regulatory approvals and withdrawals, determining the most appropriate treatment strategies and sequencing for FGFR-altered urothelial carcinoma is becoming increasing critical. However, the clinical efficacy of FGFR inhibitors is limited by acquired resistance similar to that seen with other tyrosine kinase inhibitors. Additional challenges to the clinical use of FGFR inhibitors include treatment-related adverse events and the financial costs associated with treatment. In this review, we describe known mechanisms of FGFR inhibitor resistance, including gatekeeper mutations, domain mutations, and the development of new mutations. In addition, we discuss management strategies, including ongoing clinical trials evaluating FGFR inhibitors, antibody-drug conjugates, and combination therapies with immune checkpoint inhibitors that may provide additional treatment options for localized and metastatic urothelial carcinoma.
成纤维细胞生长因子受体(FGFR)2/3改变与包括尿路上皮癌在内的多种恶性肿瘤的肿瘤发生有关。几种FGFR抑制剂已被研究或正在研发中,厄达替尼是唯一获得监管批准的抑制剂。鉴于晚期尿路上皮癌的治疗格局迅速演变,包括监管批准和撤药情况,确定FGFR改变的尿路上皮癌最合适的治疗策略和治疗顺序变得越来越关键。然而,FGFR抑制剂的临床疗效受到获得性耐药的限制,这与其他酪氨酸激酶抑制剂类似。FGFR抑制剂临床应用的其他挑战包括治疗相关不良事件以及治疗相关的财务成本。在这篇综述中,我们描述了FGFR抑制剂耐药的已知机制,包括守门基因突变、结构域突变和新突变的发生。此外,我们讨论了管理策略,包括正在进行的评估FGFR抑制剂、抗体药物偶联物以及与免疫检查点抑制剂联合治疗的临床试验,这些试验可能为局部和转移性尿路上皮癌提供更多治疗选择。