Ripretinib in advanced gastrointestinal stromal tumors: an overview of current evidence and drug approval.
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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 PDGFRα 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.
Drug Resistance, Neoplasm
Gastrointestinal Stromal Tumors
Protein Kinase Inhibitors
Proto-Oncogene Proteins c-kit
Translational Sarcoma, Melanoma and Rare Tumour Surgery
Mol and Systems Oncology
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Future Oncology, 2022, 18 (26), pp. 2967 - 2978
FUTURE MEDICINE LTD