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Updated: Apr 30, 2026

Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
Published on: June 26, 2019
Regorafenib
Thomas J Ettrich1, Thomas Seufferlein
1Department of Internal Medicine I, University of Ulm, Albert-Einstein-Allee 23, 89081, Ulm, Germany, thomas.seufferlein@uniklinik-ulm.de.
Abstract:
Regorafenib (BAY 73-4506, Stivarga®) is an oral diphenylurea multikinase inhibitor that targets angiogenic (VEGFR1-3, TIE2), stromal (PDGFR-β, FGFR), and oncogenic receptor tyrosine kinases (KIT, RET, and RAF). Regorafenib is the first small-molecule multikinase inhibitor to achieve survival benefits in metastatic colorectal cancer that has progressed after all standard therapies. Consequently, regorafenib was FDA approved for this indication. In addition, regorafenib treatment resulted in a significant improvement in progression-free survival (PFS) compared with placebo in patients with metastatic gastrointestinal stromal tumors (GIST) after progression on standard treatments and is also an FDA approved indication. Currently, regorafenib is examined in several clinical trials (mostly phase II) in different tumor entities, including renal cell carcinoma (RCC), hepatocellular carcinoma (HCC), and soft tissue sarcoma (STS).
Insights
Regorafenib, a multikinase inhibitor, offers survival benefits for advanced colorectal cancer and metastatic gastrointestinal stromal tumors. It is approved by the FDA for these indications and is being studied in other cancer types.
Area of Science:
- Oncology
- Pharmacology
Background:
- Regorafenib is an oral multikinase inhibitor targeting key pathways in cancer, including angiogenesis and oncogenic signaling.
- It represents a novel therapeutic approach for cancers that have progressed despite standard treatments.
Purpose of the Study:
- To summarize the efficacy and regulatory status of regorafenib in specific cancer types.
- To highlight ongoing research into regorafenib for other malignancies.
Main Methods:
- Review of clinical trial data and FDA approvals for regorafenib.
- Analysis of regorafenib's molecular targets and mechanism of action.
Main Results:
- Regorafenib demonstrated survival benefits in metastatic colorectal cancer and metastatic gastrointestinal stromal tumors (GIST) after standard therapy progression.
- It received FDA approval for both indications.
- Ongoing trials are evaluating regorafenib in renal cell carcinoma (RCC), hepatocellular carcinoma (HCC), and soft tissue sarcoma (STS).
Conclusions:
- Regorafenib is an effective treatment option for refractory metastatic colorectal cancer and GIST.
- Its established efficacy and ongoing investigations suggest a significant role for regorafenib in various oncological settings.
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