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...

Full description

Bibliographic Details
Main Author: Doran Ksienski
Format: Article
Language:English
Published: SAGE Publishing 2011-01-01
Series:Clinical Medicine Insights: Oncology
Online Access:https://doi.org/10.4137/CMO.S4259
_version_ 1811333427787464704
author Doran Ksienski
author_facet Doran Ksienski
author_sort Doran Ksienski
collection DOAJ
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.
first_indexed 2024-04-13T16:51:37Z
format Article
id doaj.art-f6efa0f2ada04b719ff134fc2feb7171
institution Directory Open Access Journal
issn 1179-5549
language English
last_indexed 2024-04-13T16:51:37Z
publishDate 2011-01-01
publisher SAGE Publishing
record_format Article
series Clinical Medicine Insights: Oncology
spelling doaj.art-f6efa0f2ada04b719ff134fc2feb71712022-12-22T02:38:55ZengSAGE PublishingClinical Medicine Insights: Oncology1179-55492011-01-01510.4137/CMO.S4259Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal TumorsDoran Ksienski0Victoria Island Cancer Center, Victoria, British Columbia, Canada, 2410 Lee Avenue V8R 6V5.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.https://doi.org/10.4137/CMO.S4259
spellingShingle Doran Ksienski
Imatinib Mesylate: Past Successes and Future Challenges in the Treatment of Gastrointestinal Stromal Tumors
Clinical Medicine Insights: Oncology
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
url https://doi.org/10.4137/CMO.S4259
work_keys_str_mv AT doranksienski imatinibmesylatepastsuccessesandfuturechallengesinthetreatmentofgastrointestinalstromaltumors