{"title":"Avutometinib和Defactinib:首次批准。","authors":"Hannah A Blair","doi":"10.1007/s40265-025-02215-8","DOIUrl":null,"url":null,"abstract":"<p><p>Avutometinib and defactinib (AVMAPKI<sup>™</sup> FAKZYNJA<sup>™</sup> CO-PACK) is a co-packaged rapidly accelerating fibrosarcoma (RAF)/mitogen-activated protein kinase kinase (MEK) inhibitor (avutometinib) and focal adhesion kinase (FAK)/proline-rich tyrosine kinase-2 (Pyk2) inhibitor (defactinib) being developed by Verastem Oncology for the treatment of RAS/MAPK pathway-driven cancers. In May 2025, avutometinib and defactinib was approved in the USA for the treatment of adult patients with KRAS-mutated recurrent low-grade serous ovarian cancer (LGSOC) who have received prior systemic therapy. This article summarizes the milestones in the development of avutometinib and defactinib leading to this first approval for KRAS-mutated recurrent LGSOC.</p>","PeriodicalId":11482,"journal":{"name":"Drugs","volume":" ","pages":"1319-1327"},"PeriodicalIF":14.4000,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Avutometinib and Defactinib: First Approval.\",\"authors\":\"Hannah A Blair\",\"doi\":\"10.1007/s40265-025-02215-8\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Avutometinib and defactinib (AVMAPKI<sup>™</sup> FAKZYNJA<sup>™</sup> CO-PACK) is a co-packaged rapidly accelerating fibrosarcoma (RAF)/mitogen-activated protein kinase kinase (MEK) inhibitor (avutometinib) and focal adhesion kinase (FAK)/proline-rich tyrosine kinase-2 (Pyk2) inhibitor (defactinib) being developed by Verastem Oncology for the treatment of RAS/MAPK pathway-driven cancers. In May 2025, avutometinib and defactinib was approved in the USA for the treatment of adult patients with KRAS-mutated recurrent low-grade serous ovarian cancer (LGSOC) who have received prior systemic therapy. This article summarizes the milestones in the development of avutometinib and defactinib leading to this first approval for KRAS-mutated recurrent LGSOC.</p>\",\"PeriodicalId\":11482,\"journal\":{\"name\":\"Drugs\",\"volume\":\" \",\"pages\":\"1319-1327\"},\"PeriodicalIF\":14.4000,\"publicationDate\":\"2025-10-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drugs\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1007/s40265-025-02215-8\",\"RegionNum\":1,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/8/5 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drugs","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1007/s40265-025-02215-8","RegionNum":1,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/8/5 0:00:00","PubModel":"Epub","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
摘要
Avutometinib and defactinib (AVMAPKI™FAKZYNJA™CO-PACK)是一种共包装的快速纤维肉瘤(RAF)/丝裂原活化蛋白激酶(MEK)抑制剂(Avutometinib)和局点粘附激酶(FAK)/富含脯氨酸的酪氨酸激酶-2 (Pyk2)抑制剂(defactinib),由Verastem Oncology公司开发,用于治疗RAS/MAPK通路驱动的癌症。2025年5月,avutometinib和defactinib在美国被批准用于治疗既往接受过全身治疗的kras突变复发性低级别浆液性卵巢癌(LGSOC)的成年患者。本文总结了avutometinib和defactinib在kras突变的复发性LGSOC中首次获批的里程碑。
Avutometinib and defactinib (AVMAPKI™ FAKZYNJA™ CO-PACK) is a co-packaged rapidly accelerating fibrosarcoma (RAF)/mitogen-activated protein kinase kinase (MEK) inhibitor (avutometinib) and focal adhesion kinase (FAK)/proline-rich tyrosine kinase-2 (Pyk2) inhibitor (defactinib) being developed by Verastem Oncology for the treatment of RAS/MAPK pathway-driven cancers. In May 2025, avutometinib and defactinib was approved in the USA for the treatment of adult patients with KRAS-mutated recurrent low-grade serous ovarian cancer (LGSOC) who have received prior systemic therapy. This article summarizes the milestones in the development of avutometinib and defactinib leading to this first approval for KRAS-mutated recurrent LGSOC.
期刊介绍:
Drugs is a journal that aims to enhance pharmacotherapy by publishing review and original research articles on key aspects of clinical pharmacology and therapeutics. The journal includes:
Leading/current opinion articles providing an overview of contentious or emerging issues.
Definitive reviews of drugs and drug classes, and their place in disease management.
Therapy in Practice articles including recommendations for specific clinical situations.
High-quality, well designed, original clinical research.
Adis Drug Evaluations reviewing the properties and place in therapy of both newer and established drugs.
AdisInsight Reports summarising development at first global approval.
Moreover, the journal offers additional digital features such as animated abstracts, video abstracts, instructional videos, and podcasts to increase visibility and educational value. Plain language summaries accompany articles to assist readers with some knowledge of the field in understanding important medical advances.