Abstract
Regorafenib is an orally administered multikinase inhibitor. It is administered on a continuous dosing schedule and shows non-specific binding to several intracellular kinases, with potent inhibitory activity against vascular endothelial growth factor receptors 1–3 (VEGFR1 [also known as FLT1], VEGFR2 [KDR], and VEGFR3 [FLT4]), PDGFRB, FGFR1, RAF, TIE2, and the mutant oncogenic kinases KIT, RET, and BRAF. 1 Wilhelm SM Dumas J Adnane L et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer. 2011; 129: 245-255 Crossref PubMed Scopus (921) Google Scholar Commonly reported (>10%) toxic effects include fatigue, hand-foot skin reaction, diarrhoea, anorexia, voice changes, hypertension, oral mucositis, rash, and weight loss. 2 Grothey A Van Cutsem E Sobrero A et al. for the CORRECT Study GroupRegorafenib monotherapy for previously treated metastatic colorectal cancer (CORRECT): an international, multicentre, randomised, placebo-controlled, phase 3 trial. Lancet. 2012; (published online Nov 22.)http://dx.doi.org/10.1016/S0140-6736(12)61900-X Google Scholar , 3 Demetri GD Reichardt P Kang Y-K et al. on behalf of all GRID study investigatorsEfficacy and safety of regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib (GRID): an international, multicentre, randomised, placebo-controlled, phase 3 trial. Lancet. 2012; (published online Nov 22.)http://dx.doi.org/10.1016/S0140-6736(12)61857-1 Google Scholar Clinical trials are underway assessing regorafenib in the treatment of colorectal cancer, gastrointestinal stromal tumours (GIST), lung cancer, renal cell carcinoma, and hepatocellular carcinoma. Regorafenib monotherapy for previously treated metastatic colorectal cancer (CORRECT): an international, multicentre, randomised, placebo-controlled, phase 3 trialRegorafenib is the first small-molecule multikinase inhibitor with survival benefits in metastatic colorectal cancer which has progressed after all standard therapies. The present study provides evidence for a continuing role of targeted treatment after disease progression, with regorafenib offering a potential new line of therapy in this treatment-refractory population. Full-Text PDF Efficacy and safety of regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib (GRID): an international, multicentre, randomised, placebo-controlled, phase 3 trialThe results of this study show that oral regorafenib can provide a significant improvement in progression-free survival compared with placebo in patients with metastatic GIST after progression on standard treatments. As far as we are aware, this is the first clinical trial to show benefit from a kinase inhibitor in this highly refractory population of patients. Full-Text PDF
Published Version
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call