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Updated: Sep 10, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
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A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors

Published on: December 7, 2014

Regorafenib

Thomas J Ettrich1, Thomas Seufferlein2

  • 1Department of Internal Medicine I, University of Ulm, Albert-Einstein-Allee 23, 89081, Ulm, Germany.

Recent Results in Cancer Research. Fortschritte Der Krebsforschung. Progres Dans Les Recherches Sur Le Cancer
|August 3, 2018
PubMed

Insights

Regorafenib, a multi-kinase inhibitor, offers survival benefits for patients with advanced metastatic colorectal cancer, gastrointestinal stromal tumors, and hepatocellular carcinoma. It targets key kinases involved in tumor growth and angiogenesis.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Regorafenib is an oral multi-kinase inhibitor targeting angiogenic, stromal, and oncogenic receptor tyrosine kinases.
  • It represents a significant advancement in small-molecule targeted therapies for various cancers.

Purpose of the Study:

  • To review the efficacy and FDA approvals of Regorafenib in specific cancer indications.
  • To highlight its role in treating refractory metastatic colorectal cancer, gastrointestinal stromal tumors, and advanced hepatocellular carcinoma.

Main Methods:

  • Review of clinical trial data and FDA approval history for Regorafenib.
  • Analysis of Regorafenib's mechanism of action as a multi-kinase inhibitor.

Main Results:

  • Regorafenib demonstrated survival benefits in metastatic colorectal cancer, leading to FDA approval in 2012.
  • Significant improvement in progression-free survival (PFS) was observed in metastatic gastrointestinal stromal tumors (GIST) and advanced hepatocellular carcinoma (HCC).
  • Regorafenib is FDA-approved for GIST (2013) and HCC (2017) after prior treatments.

Conclusions:

  • Regorafenib is an effective therapeutic option for patients with refractory metastatic colorectal cancer, GIST, and HCC.
  • Ongoing trials are exploring its utility in other tumor types like renal cell carcinoma and soft-tissue sarcoma.
Keywords:
CRCGISTHCCRegorafenibTKI

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