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The Safety of Regorafenib for the Treatment of Gastrointestinal Stromal Tumors

Piotr Rutkowski, Joanna Stępniak

Expert Opin Drug Saf. 2016 Jan;15(1):105-16.

PMID: 26651387

Abstract:

Introduction:
The management of gastrointestinal stromal tumors (GIST) evolved due to effective molecularly targeted therapy with imatinib and sunitinib which are used first- and second-line, respectively. However, due to the development of resistance to those drugs in the majority of patients, the need for third-line therapy arose.
Areas covered:
Regorafenib, an oral multitargeted inhibitor with activity against multiple kinases including KIT, RET, RAF1, BRAF, angiogenesis (VEGFR, TIE-2) and those involved in tumor microenvironment (PDGFR and FGFR) was introduced after the successful Phase III GRID (GIST - Regorafenib In progressive Disease) clinical trial. This study showed significant improvement in progression-free survival for patients receiving regorafenib compared to placebo (4.8 months vs 0.9 months). The treatment was reasonably well tolerated, with arterial hypertension, hand-foot syndrome, diarrhea being the most common grade ≥3 adverse events, which could be managed by dose reduction and supportive treatment. The aim of this paper is to describe, assess and advise on the safety of regorafenib as third-line therapy in GIST.
Expert opinion:
Regorafenib has demonstrated clinical benefit in GIST patients after progression on prior treatment with at least imatinib/sunitinib and currently it is the approved standard third-line option in therapy of advanced GIST. The safety profile is similar to other multikinase inhibitors with anti-VEGFR activity and is manageable.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR42415729 VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor Price
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