Regorafenib is a multi-kinase inhibitor developed by Bayer HealthCare Pharmaceuticals that is structurally identical to sorafenib apart from a single fluorine atom added to the central aromatic ring. It has multiple tyrosine kinase and serine/threonine kinase targets which include vascular endothelial growth factor receptors 1–3 (VEGFR1–3), platelet-derived growth factor receptor-β (PDGFRβ), fibroblast growth factor receptor 1 (FGFR1), Raf-1, tyrosine kinase with immunoglobulin and epidermal growth factor homology domain 2 (TIE2), and the oncogenic kinases c-KIT, RET, C-RAF, B-RAF, and B-RAF V600E mutant. Regorafenib has been demonstrated to improve the overall survival of patients with heavily pretreated, metastatic colorectal cancer (mCRC) and to significantly improve progression-free survival in treatment-refractory gastrointestinal stromal tumors (GIST).
KeywordsRenal Cell Carcinoma Gastrointestinal Stromal Tumor Oral Mucositis Disease Control Rate Correct Trial
- Argiles G, Saunders MP, Rivera F, Sobrero A, Benson A, Ponce CG et al (2015) Regorafenib plus modified FOLFOX6 as first-line treatment of metastatic colorectal cancer: A phase II trial Eur J of Canc 51 (8): 942–949Google Scholar
- Bruix J, Tak WY, Gasbarrini A, Santoro A, Colombo M, Lim HY et al (2013) Regorafenib as second-line therapy for intermediate or advanced hepatocellular carcinoma: Multicentre, open-label, phase II safety study Eur J of Canc 49 (16): 3412–3419Google Scholar
- Demetri GD, Reichardt P, Kang YK, Blay JY, Rutkowski P, Gelderblom H et al (2013) 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 trial. Lancet 381(9863):295–302CrossRefPubMedGoogle Scholar
- Li J, Qin S, Xu R, Yau TCC, Ma B, Pan H et al (2015) Regorafenib plus best supportive care versus placebo plus best supportive care in Asian patients with previously treated metastatic colorectal cancer (CONCUR): a randomised, double-blind, placebo-controlled, phase 3 trial. Lancet Oncol 16(6): 619–629CrossRefPubMedGoogle Scholar