Ripretinib in advanced gastrointestinal stromal tumors: an overview of current evidence and drug approval.
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Date
2022-07-26Author
Goggin, C
Stansfeld, A
Mahalingam, P
Thway, K
Smith, MJ
Huang, P
Jones, RL
Napolitano, A
Type
Journal Article
Metadata
Show full item recordAbstract
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.
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Subject
DCC-2618
GIST
INTRIGUE
INVICTUS
KIT
PDGFR
resistance mutation
ripretinib
Antineoplastic Agents
Drug Approval
Drug Resistance, Neoplasm
Gastrointestinal Neoplasms
Gastrointestinal Stromal Tumors
Humans
Imatinib Mesylate
Mutation
Naphthyridines
Protein Kinase Inhibitors
Proto-Oncogene Proteins c-kit
Urea
Research team
Translational Sarcoma, Melanoma and Rare Tumour Surgery
Mol and Systems Oncology
Language
eng
Date accepted
2022-06-24
License start date
2022-07-26
Citation
Future Oncology, 2022, 18 (26), pp. 2967 - 2978
Publisher
FUTURE MEDICINE LTD