Ripretinib: A narrative drug review

Gastrointestinal stromal tumors (GISTs) are rare primary neoplasms of the gastrointestinal tract, mesentery, or omentum. In the past, for patients with resectable tumors, surgery was the only viable treatment option. However, therapy of GISTs has undergone a fundamental change with the advent of receptor tyrosine kinase inhibitors primarily targeting the tyrosine-protein kinase KIT and the platelet-derived growth factor receptor alpha (PDGFRA). Ripretinib is one such novel Type-II tyrosine switch control inhibitor which is used in the treatment of advanced KIT proto-oncogene-driven and PDGFRA-induced tumors, including GISTs. The Food and Drug Administration approved ripretinib on May 15, 2020, for the treatment of adult patients with progressive GISTs who had undergone prior treatment with three or more kinase inhibitors. A comprehensive search in PubMed and other sources were done, using the search terms, “GIST” and ripretinib. On combining all the abstracts and conference proceedings, here we present a comprehensive review on ripretinib's history, pharmacology, and clinical applications.