Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

Regorafenib

Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_7189-4

Synonyms

Definition

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).

Characteristics

  • Chemical Name

    4-[4-({[4-Chloro-3-(trifluoromethyl)phen...

Keywords

Renal Cell Carcinoma Gastrointestinal Stromal Tumor Oral Mucositis Disease Control Rate Correct Trial 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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References

  1. 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
  2. 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
  3. 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
  4. Eisen T, Joensuu H, Nathan PD, Harper PG, Wojtukiewicz MZ, Nicholson S et al (2012) Regorafenib for patients with previously untreated metastatic or unresectable renal-cell carcinoma: a single-group phase 2 trial. Lancet Oncol 13(10):1055–1062CrossRefPubMedGoogle Scholar
  5. Grothey A, Van Cutsem E, Sobrero A, Siena S, Falcone A, Ychou M et al (2013) Regorafenib monotherapy for previously treated metastatic colorectal cancer (CORRECT): an international, multicentre, randomised, placebo-controlled, phase 3 trial. Lancet 381(9863):303–312CrossRefPubMedGoogle Scholar
  6. 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
  7. Mross K, Frost A, Steinbild S, Hedbom S, Buchert M, Fasol U et al (2012) A phase I dose-escalation study of regorafenib (BAY 73–4506), an inhibitor of oncogenic, angiogenic, and stromal kinases, in patients with advanced solid tumors. Clin Cancer Res 18(9):2658–2667CrossRefPubMedGoogle Scholar
  8. Wilhelm SM, Dumas J, Adnane L, Lynch M, Carter CA, Schutz G et al (2011) 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 129(1):245–255CrossRefPubMedGoogle Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  1. 1.GI/Lymphoma Research UnitRoyal Marsden HospitalSurreyUK
  2. 2.Department of MedicineThe Royal Marsden NHS Foundation TrustLondonUK