Drug updated on 4/15/2024
| 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.
Summary
- Regorafenib (Stivarga) is a multi-kinase inhibitor approved for use in metastatic colorectal cancer, gastrointestinal stromal tumors, and hepatocellular carcinoma following prior therapy.
- A total of 21 studies were reviewed to compare the safety and effectiveness of regorafenib with other treatments.
- In second-line treatments for hepatocellular carcinoma post-sorafenib failure, regorafenib significantly prolongs both overall survival and progression-free survival compared to placebo but shows no significant differences in disease control rate when compared to nivolumab.
- For third-line treatment scenarios of metastatic colorectal cancer, regorafenib improves overall survival and progression-free survival compared to best supportive care, though it is highly sensitive to adverse effects such as hand-foot skin reactions, fatigue, and diarrhea.
- In treating gastrointestinal stromal tumors after imatinib mesylate and sunitinib malate failure, regorafenib extended patients' lifespan while maintaining an acceptable safety profile.
- The drug's tolerability varies among different patients, requiring dose adjustments due to its associated adverse events, including cardiovascular outcomes, which necessitates monitoring during the treatment period especially when used alongside TKI therapies like sunitinib or TAS-102.
- Specific population types, such as AFP levels in HCC patients or baseline NLR in mCRC patients treated with Stivarga, are important predictors of therapy response, indicating that tailored management strategies based on individual profiles rather than a one-size-fits-all approach should be considered.
- The decision to use this medication must weigh its potential serious side effects, necessitating a careful selection process before administration, particularly for individuals who have exhausted other treatment options available.
Product Monograph / Prescribing Information
| Document Title | Year | Source |
|---|---|---|
| Stivarga (regorafenib) Prescribing Information. | 2020 | Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ |