{"title":"fgfr改变的尿路上皮癌:抵抗机制和治疗策略。","authors":"David J Benjamin, Alain C Mita","doi":"10.1007/s11523-024-01119-z","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":22195,"journal":{"name":"Targeted Oncology","volume":" ","pages":"1-11"},"PeriodicalIF":4.4000,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"FGFR-Altered Urothelial Carcinoma: Resistance Mechanisms and Therapeutic Strategies.\",\"authors\":\"David J Benjamin, Alain C Mita\",\"doi\":\"10.1007/s11523-024-01119-z\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":22195,\"journal\":{\"name\":\"Targeted Oncology\",\"volume\":\" \",\"pages\":\"1-11\"},\"PeriodicalIF\":4.4000,\"publicationDate\":\"2025-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Targeted Oncology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1007/s11523-024-01119-z\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/12/17 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"ONCOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Targeted Oncology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1007/s11523-024-01119-z","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/12/17 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"ONCOLOGY","Score":null,"Total":0}
FGFR-Altered Urothelial Carcinoma: Resistance Mechanisms and Therapeutic Strategies.
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.
期刊介绍:
Targeted Oncology addresses physicians and scientists committed to oncology and cancer research by providing a programme of articles on molecularly targeted pharmacotherapy in oncology. The journal includes:
Original Research Articles on all aspects of molecularly targeted agents for the treatment of cancer, including immune checkpoint inhibitors and related approaches.
Comprehensive narrative Review Articles and shorter Leading Articles discussing relevant clinically established as well as emerging agents and pathways.
Current Opinion articles that place interesting areas in perspective.
Therapy in Practice articles that provide a guide to the optimum management of a condition and highlight practical, clinically relevant considerations and recommendations.
Systematic Reviews that use explicit, systematic methods as outlined by the PRISMA statement.
Adis Drug Reviews of the properties and place in therapy of both newer and established targeted drugs in oncology.