{"title":"B-Raf-Mutated黑色素瘤","authors":"Sarah E Fenton, J. Sosman, S. Chandra","doi":"10.5772/intechopen.86615","DOIUrl":null,"url":null,"abstract":"Until fairly recently, treatment options for advanced melanoma have been relatively limited. Fortunately, the last decade has seen dramatic improvements in response rates and duration of overall survival after the introduction of checkpoint inhibitors and targeted therapies against mutations in the B-isoform of Raf (B-Raf) in metastatic or inoperable melanoma. This book chapter will discuss the role of wild type B-Raf in the cell, the changes induced by mutations in this protein, and current FDA approvals for targeted therapies against B-Raf, both as a monotherapy and in combination with MEK inhibitors. We will also summarize mechanisms of resistance against these targeted therapies as well as novel therapeutic regimens proposed to bypass resistance.","PeriodicalId":221207,"journal":{"name":"Cutaneous Melanoma [Working Title]","volume":"13 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2020-04-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"B-Raf-Mutated Melanoma\",\"authors\":\"Sarah E Fenton, J. Sosman, S. Chandra\",\"doi\":\"10.5772/intechopen.86615\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Until fairly recently, treatment options for advanced melanoma have been relatively limited. Fortunately, the last decade has seen dramatic improvements in response rates and duration of overall survival after the introduction of checkpoint inhibitors and targeted therapies against mutations in the B-isoform of Raf (B-Raf) in metastatic or inoperable melanoma. This book chapter will discuss the role of wild type B-Raf in the cell, the changes induced by mutations in this protein, and current FDA approvals for targeted therapies against B-Raf, both as a monotherapy and in combination with MEK inhibitors. We will also summarize mechanisms of resistance against these targeted therapies as well as novel therapeutic regimens proposed to bypass resistance.\",\"PeriodicalId\":221207,\"journal\":{\"name\":\"Cutaneous Melanoma [Working Title]\",\"volume\":\"13 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2020-04-27\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Cutaneous Melanoma [Working Title]\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.5772/intechopen.86615\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Cutaneous Melanoma [Working Title]","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.5772/intechopen.86615","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
摘要
直到最近,晚期黑色素瘤的治疗选择相对有限。幸运的是,在过去十年中,在引入检查点抑制剂和针对转移性或不能手术的黑色素瘤中Raf b -亚型突变的靶向治疗后,在反应率和总生存期方面有了显着改善。本章将讨论野生型B-Raf在细胞中的作用,这种蛋白质突变引起的变化,以及目前FDA批准的针对B-Raf的靶向治疗,无论是作为单一疗法还是与MEK抑制剂联合使用。我们还将总结对这些靶向治疗的耐药机制以及提出的绕过耐药的新治疗方案。
Until fairly recently, treatment options for advanced melanoma have been relatively limited. Fortunately, the last decade has seen dramatic improvements in response rates and duration of overall survival after the introduction of checkpoint inhibitors and targeted therapies against mutations in the B-isoform of Raf (B-Raf) in metastatic or inoperable melanoma. This book chapter will discuss the role of wild type B-Raf in the cell, the changes induced by mutations in this protein, and current FDA approvals for targeted therapies against B-Raf, both as a monotherapy and in combination with MEK inhibitors. We will also summarize mechanisms of resistance against these targeted therapies as well as novel therapeutic regimens proposed to bypass resistance.