Drug updated on 9/4/2024
| Dosage Form | Tablet (oral; 40 mg) |
| Drug Class | Kinase inhibitors |
| Ongoing and Completed Studies | ClinicalTrials.gov |
Indication
- Indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an antiVEGF therapy, and, if RAS wild-type, an anti-EGFR therapy.
- Indicated for the treatment of patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate.
- Indicated for the treatment of patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.
Latest News
Summary
- Stivarga (regorafenib) is indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if RAS wild-type, an anti-EGFR therapy; for the treatment of patients with locally advanced, unresectable, or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate; and for the treatment of patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.
- This summary is based on the review of 21 systematic review(s)/meta-analysis(es). [1-21]
- Regorafenib, as a second-line treatment for advanced hepatocellular carcinoma (HCC), significantly improved overall survival (OS) and progression-free survival (PFS) compared to placebo and ranked highest for OS among second-line options such as cabozantinib, ramucirumab, and pembrolizumab.
- In metastatic colorectal cancer (mCRC), regorafenib used as third-line therapy improved OS and PFS compared to best supportive care (BSC) and showed similar OS and PFS to TAS-102, with better tumor response rates. Fruquintinib had slightly better PFS, but regorafenib demonstrated a favorable tumor response profile.
- For gastrointestinal stromal tumors (GIST), regorafenib improved survival in patients who had failed previous treatments with imatinib and sunitinib.
- Common side effects of regorafenib include diarrhea, fatigue, and hand-foot skin reaction, with a noted higher risk of thrombocytopenia and arterial hypertension compared to other drugs.
- Regorafenib is associated with significant cardiovascular events, particularly severe thrombocytopenia, and poses cardiovascular risks such as cardiac ischemia and left ventricular systolic dysfunction, although it wasn't highlighted as having the highest risk among TKIs.
- In comparisons, regorafenib showed a lower incidence of severe adverse events in metastatic colorectal cancer (mCRC) compared to fruquintinib and similar toxicity profiles to cabozantinib in hepatocellular carcinoma (HCC), though cabozantinib had marginally higher risks for hand-foot syndrome and diarrhea.
- Regorafenib demonstrated improved overall survival (OS) in hepatocellular carcinoma (HCC) patients with low alpha-fetoprotein (AFP) levels, and it was effective across various subgroups in metastatic colorectal cancer (mCRC), including those with KRAS and BRAF mutations. For gastrointestinal stromal tumors (GIST), regorafenib was beneficial in patients who failed prior imatinib and sunitinib treatments.
Product Monograph / Prescribing Information
| Document Title | Year | Source |
|---|---|---|
| Stivarga (regorafenib) Prescribing Information. | 2020 | Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ |