HEALTH PROFESSIONAL · SOURCE READING
Regorafenib
Source: Colon Cancer Treatment (PDQ®)–Health Professional Version, National Cancer Institute.
Source updated: February 12, 2025 · Captured 2026-09-09.
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Regorafenib is an inhibitor of multiple tyrosine kinase pathways, including VEGF. In 2012, the FDA approved regorafenib for patients who had progressed on previous therapy.
Evidence (regorafenib):
The safety and effectiveness of regorafenib were evaluated in a single, clinical study of 760 patients with previously treated metastatic colorectal cancer. Patients were randomly assigned 2:1 to receive regorafenib or a placebo in addition to the best supportive care.[94,95]
The safety and effectiveness of regorafenib were evaluated in a single, clinical study of 760 patients with previously treated metastatic colorectal cancer. Patients were randomly assigned 2:1 to receive regorafenib or a placebo in addition to the best supportive care.[94,95]
Patients treated with regorafenib had a statistically significant improvement in OS (6.4 months in the regorafenib group vs. 5.0 months in the placebo group; HR, 0.77; 95% CI, 0.64–0.94; one-sided P = .0052).
With the improved OS from the combination of trifluridine-tipiracil and bevacizumab discussed above, regorafenib is now often considered a fourth-line or later option for treatment of patients with metastatic colorectal cancer.
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