{"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}
引用次数: 0
Abstract
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.