Drug updated on 12/11/2024
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
- Hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.
Latest News
Summary
- This summary is based on the review of 24 systematic review(s)/meta-analysis(es). [1-24]
- In Hepatocellular Carcinoma (HCC), Nivolumab demonstrated statistically insignificantly longer overall survival (OS), time to progression (TTP), and progression-free survival (PFS) compared to Regorafenib; however, Nivolumab had a higher overall response rate (ORR) with mixed disease control rate (DCR) results. Regorafenib combined with PD-1 inhibitors significantly improved OS (hazard ratio (HR), 0.61) and PFS (HR, 0.51) compared to monotherapy.
- For Metastatic Colorectal Cancer (mCRC), TAS-102 plus Bevacizumab was the most effective regimen in terms of median overall survival (mOS) and median progression-free survival (mPFS), outperforming standard and dose-escalated Regorafenib treatments.
- In Gastrointestinal Stromal Tumors (GIST), Regorafenib showed improved survival rates after the failure of Imatinib and Sunitinib, with acceptable safety profiles; it also resulted in better PFS compared to placebo, Imatinib, and Sunitinib, although Ripretinib and Masitinib exhibited superior OS.
- Combination therapies, specifically Nivolumab plus Ipilimumab, yielded significantly higher ORR and longer OS compared to Regorafenib, Cabozantinib, and Nivolumab monotherapy.
- Nivolumab exhibited fewer side effects and improved tolerance compared to Regorafenib in patients with HCC. However, Regorafenib combined with programmed death-1 inhibitors (R-P) resulted in a higher incidence of adverse events, including hypothyroidism, thrombocytopenia, and rash, relative to Regorafenib monotherapy.
- In mCRC, Fruquintinib was linked to a significantly higher risk of serious adverse events compared to TAS-102 and Regorafenib, highlighting differing safety profiles among these treatments.
- Adverse events associated with Regorafenib in GIST were predominantly mild to moderate; however, monitoring for grade 4 or higher adverse events is necessary, as Regorafenib was found to have the highest rates of high-grade adverse events compared to Ripretinib and Masitinib, which had lower rates of severe events.
- Regorafenib demonstrates significant superiority in OS for patients with low-level alpha-fetoprotein (AFP) in HCC, while no statistical differences were observed in patients with elevated AFP; in mCRC, the studies included primarily middle-aged to elderly individuals with a slight male predominance, mostly Caucasian, and TAS-102 plus Bevacizumab ranked highest across various subgroups including age, gender, and ECOG performance status.
Product Monograph / Prescribing Information
Document Title | Year | Source |
---|---|---|
Stivarga (regorafenib) Prescribing Information. | 2020 | Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ |
Systematic Reviews / Meta-Analyses
Clinical Practice Guidelines
Document Title | Year | Source |
---|---|---|
2023 GEIS guidelines for gastrointestinal stromal tumors | 2023 | Therapeutic Advances in Medical Oncology |
Clinical practice guidelines and real-life practice in hepatocellular carcinoma: a Taiwan perspective | 2023 | Clinical and Molecular Hepatology |
Clinical practice guidelines and real-life practice in hepatocellular carcinoma: a Chinese perspective | 2023 | Clinical and Molecular Hepatology |
AGA clinical practice guideline on systemic therapy for hepatocellular carcinoma | 2022 | Gastroenterology |
Argentinian clinical practice guideline for surveillance, diagnosis, staging and treatment of hepatocellular carcinoma | 2020 | Annals of Hepatology |
Nonsurgical management of advanced hepatocellular carcinoma: a clinical practice guideline | 2020 | Current Oncology |
Systemic therapy for advanced hepatocellular carcinoma: ASCO guideline | 2020 | Journal of Clinical Oncology |
Third- or later-line therapy for metastatic colorectal cancer: reviewing best practice | 2019 | Clinical Colorectal Cancer |