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Regorafenib: A Review of Its Use in Patients with Advanced Gastrointestinal Stromal Tumours

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Abstract

Regorafenib (Stivarga®) is an orally administered small molecule inhibitor of multiple protein kinases, including kinases involved in oncogenesis and tumour angiogenesis. It was initially approved for use in patients with previously treated metastatic colorectal cancer. Based on the findings of the phase III GRID clinical trial, approval for regorafenib has been expanded to include the treatment of advanced gastrointestinal stromal tumours (GISTs) following the failure of imatinib and sunitinib. In the GRID trial, regorafenib significantly improved progression-free survival and was associated with a significantly higher disease control rate than placebo. No significant between-group difference was observed in overall survival (OS) in the trial; however, the high proportion of patients who crossed over from placebo to regorafenib likely impacted the OS analysis. Regorafenib has an acceptable tolerability profile, with most adverse events being manageable with dose modification and/or supportive measures. The most commonly reported drug-related adverse events among patients receiving regorafenib in the GRID trial were hand-foot skin reaction, hypertension, diarrhoea and fatigue. In conclusion, regorafenib presents a valuable new tool in the treatment of patients with advanced GISTs following the failure of imatinib and sunitinib.

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Disclosure

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made by the authors on the basis of scientific and editorial merit. Matt Shirley and Gillian Keating are salaried employees of Adis/Springer.

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Correspondence to Matt Shirley.

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The manuscript was reviewed by: C. R. Garrett, Department of Gastrointestinal Medical Oncology, University of Texas MD Anderson Cancer Center, Houston, TX, USA; P. Rutkowski, Department of Soft Tissue/Bone Sarcoma and Melanoma, Maria Sklodowska-Curie Memorial Cancer Center and Institute of Oncology, Warsaw, Poland.

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Shirley, M., Keating, G.M. Regorafenib: A Review of Its Use in Patients with Advanced Gastrointestinal Stromal Tumours. Drugs 75, 1009–1017 (2015). https://doi.org/10.1007/s40265-015-0406-x

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  • DOI: https://doi.org/10.1007/s40265-015-0406-x

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