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Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal Tumors

Just over a decade ago, gastrointestinal tumours were a poorly understood mesenchymal neoplasm unsuccessfully treated with chemotherapy. Cytotoxic therapy for advanced disease yielded response rates of 10% and median survival of just 18 months. However, the discovery of KIT and platelet derived grow...

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Detalles Bibliográficos
Autor principal: Ksienski, Doran
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Libertas Academica 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3235999/
https://www.ncbi.nlm.nih.gov/pubmed/22174597
http://dx.doi.org/10.4137/CMO.S4259
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author Ksienski, Doran
author_facet Ksienski, Doran
author_sort Ksienski, Doran
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description Just over a decade ago, gastrointestinal tumours were a poorly understood mesenchymal neoplasm unsuccessfully treated with chemotherapy. Cytotoxic therapy for advanced disease yielded response rates of 10% and median survival of just 18 months. However, the discovery of KIT and platelet derived growth factor receptor alpha (PDGFRA) mutations as oncogenic drivers of most gastrointestinal tumours, paved the way for targeted therapy. Imatinib mesylate, a tyrosine kinase inhibitor, produces a clinical benefit rate (complete response, partial response, and stable disease) of more than 80% in metastatic setting and a median survival of 57 months. Imatinib is now also approved in adult patients following resection of KIT-positive GIST. Major insights into the mechanism of action of imatinib, unique pharmacokinetics, drug resistance, and management of low grade but chronic adverse effects continue to be made.
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spelling pubmed-32359992011-12-15 Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal Tumors Ksienski, Doran Clin Med Insights Oncol Expert Review Just over a decade ago, gastrointestinal tumours were a poorly understood mesenchymal neoplasm unsuccessfully treated with chemotherapy. Cytotoxic therapy for advanced disease yielded response rates of 10% and median survival of just 18 months. However, the discovery of KIT and platelet derived growth factor receptor alpha (PDGFRA) mutations as oncogenic drivers of most gastrointestinal tumours, paved the way for targeted therapy. Imatinib mesylate, a tyrosine kinase inhibitor, produces a clinical benefit rate (complete response, partial response, and stable disease) of more than 80% in metastatic setting and a median survival of 57 months. Imatinib is now also approved in adult patients following resection of KIT-positive GIST. Major insights into the mechanism of action of imatinib, unique pharmacokinetics, drug resistance, and management of low grade but chronic adverse effects continue to be made. Libertas Academica 2011-11-09 /pmc/articles/PMC3235999/ /pubmed/22174597 http://dx.doi.org/10.4137/CMO.S4259 Text en © the author(s), publisher and licensee Libertas Academica Ltd. This is an open access article. Unrestricted non-commercial use is permitted provided the original work is properly cited.
spellingShingle Expert Review
Ksienski, Doran
Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal Tumors
title Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal Tumors
title_full Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal Tumors
title_fullStr Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal Tumors
title_full_unstemmed Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal Tumors
title_short Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal Tumors
title_sort imatinib mesylate: past successes and future challenges in the treatment of gastrointestinal stromal tumors
topic Expert Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3235999/
https://www.ncbi.nlm.nih.gov/pubmed/22174597
http://dx.doi.org/10.4137/CMO.S4259
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