Ripretinib for the treatment of adult patients with advanced gastrointestinal stromal tumors.
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Embargo End Date
ICR Authors
Authors
Sargsyan, A
Kucharczyk, MA
Jones, RL
Constantinidou, A
Kucharczyk, MA
Jones, RL
Constantinidou, A
Document Type
Journal Article
Date
2023-02-01
Date Accepted
2023-01-09
Abstract
INTRODUCTION: Gastrointestinal stromal tumor (GIST) is the most common mesenchymal tumor of the gastrointestinal tract. Imatinib mesylate revolutionized the management of advanced/metastatic GIST, and remains the standard first-line therapy in this setting. Upon development of secondary resistance, sunitinib and regorafenib are used as subsequent treatments, although clinical benefit is often non-durable. Ripretinib is a type II kinase inhibitor targeting KIT and PDGFRA mutations and resistance through switching active I and inactive II forms. AREAS COVERED: This drug profile article provides an overview of the current state of the art treatment algorithm for advanced/metastatic GIST, focusing on the role of ripretinib in the fourth-line setting as defined by currently available clinical trials evidence. The mechanism of action, the safety profile, efficacy, and clinical application of ripretinib are presented. In addition, the Phase I study (NCT02571036) through which the optimal dose was established and the Phase III trials that assessed the efficacy and safety of ripretinib as fourth- (INVICTUS) and second-line treatment (INTRIGUE) are presented. EXPERT OPINION: Ripretinib is a safe and an effective therapy for the fourth-line setting in advanced/metastatic GIST. Future studies should evaluate combination schedules and the identification of markers predictive of benefit from ripretinib.
Citation
Expert Review of Gastroenterology and Hepatology, 2023, 17 (2), pp. 119 - 127
Source Title
Expert Review of Gastroenterology and Hepatology
Publisher
TAYLOR & FRANCIS LTD
ISSN
1747-4124
eISSN
1747-4132
1747-4132
1747-4132