Ripretinib in advanced gastrointestinal stromal tumors: an overview of current evidence and drug approval

Over the past 20 years, the management of gastrointestinal stromal tumors has acted as an important model in the advancement of molecularly targeted therapies for solid tumors. The success of imatinib has established it as a lasting therapy in the management of early-stage and advanced disease in the first-line setting. Imatinib resistance inevitably develops, resulting in the need for further lines of therapy. Ripretinib is an orally administered switch-control tyrosine kinase inhibitor, specifically developed to target both primary and secondary KIT and PDGFR alpha resistance mutations. Herein, the authors discuss the molecular rationale, the preclinical evidence and the clinical use of ripretinib in the treatment of gastrointestinal stromal tumors in the advanced stages of disease.

Automated summary

The management of gastrointestinal stromal tumors has played a crucial role in advancing targeted therapies for solid tumors. Imatinib has been a successful first-line therapy, but the development of resistance necessitates the use of other treatments. Ripretinib is a switch-control tyrosine kinase inhibitor that specifically targets resistance mutations, and its molecular rationale and clinical use are discussed in this article.