Loading
A sorafenib successor that became the first second-line drug proven to prolong life in liver cancer (2017).
Regorafenib is an oral multi-kinase inhibitor of VEGFR1-3, TIE2, PDGFR, FGFR, KIT, RET and RAF, a successor to sorafenib with broader targets. It is approved for previously treated metastatic colorectal cancer (CORRECT, 2012), GIST after imatinib and sunitinib (GRID, 2013) and hepatocellular carcinoma after sorafenib (2017). RESORCE showed overall survival of 10.6 versus 7.8 months versus placebo after sorafenib progression (HR 0.63), the first second-line survival benefit in liver cancer; sequencing sorafenib then regorafenib gave a median 26 months from sorafenib start. Hand-foot skin reaction (53%, 13% grade 3 or higher), hypertension and fatigue are common at 160 mg, so start-low escalation (ReDOS in colorectal cancer) is widely used. Its colorectal benefit is small, and fruquintinib now competes there. For a newcomer, it is a broad anti-angiogenic pill used late in three cancers.
Oral inhibitor of VEGFR1-3, TIE2, PDGFR, FGFR, KIT, RET and RAF. Connects to VEGF / VEGFR, KIT and RET.
1.Regorafenib slips into a pocket on VEGF / VEGFR.
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026).
Covered for FDA-labelled and NCCN-listed uses, but almost always behind prior authorisation confirming diagnosis, biomarker and line of therapy; dispensed through a specialty pharmacy.
Part D out-of-pocket capped at $2,000 (2025) / $2,100 (2026). Medicare patients cannot use manufacturer co-pay cards; charity funds (PAN, HealthWell, CancerCare) and the Extra Help subsidy are the routes.
Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.
Sources: NICE TA555 · SMC advice: regorafenib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
| Region | Year | Indication |
|---|---|---|
| US | 2012 | Metastatic colorectal cancer, previously treated |
| US | 2013 | GIST after imatinib and sunitinib |
| US | 2017 | HCC previously treated with sorafenib |
| US | 2012 | Metastatic colorectal cancer after fluoropyrimidine, oxaliplatin, irinotecan, anti-VEGF and, if RAS wild-type, anti-EGFR therapy · Approved September 2012 on CORRECT. |
| EU | 2013 | Metastatic colorectal cancer after available therapies · Stivarga marketing authorisation issued 26 August 2013. |
| England (NICE) | 2023 | Metastatic colorectal cancer after previous treatment or when those treatments are unsuitable · TA866, published 8 February 2023, recommends it within its marketing authorisation subject to the commercial arrangement, a decade after the FDA approval. |
| Adverse event | Any grade | Grade 3+ |
|---|---|---|
| Hand-foot skin reaction | 53% | 13% |
| Hypertension | 31% | 15% |
| Fatigue | 40% | 9% |
RESORCE. Events listed without rates were not read from a primary source; see the label. Blank cells mean the figure was not sourced, not that it is zero.
Country and place are remembered in this browser only. A postcode is sent to OpenStreetMap's Nominatim service to find coordinates when you press the button; nothing else leaves your device.
A reminder that ivermectin interacts with cancer drugs: the dose that a healthy adult tolerates can poison a patient whose liver enzymes are already occupied by a kinase inhibitor.
Patients with metastatic colorectal cancer carrying a KRAS G12C mutation (about 3-4% of cases) who have exhausted standard chemotherapy now have a targeted option that works far better than trifluridine-tipiracil or regorafenib. The higher sotorasib dose is clearly superior, and the EGFR antibody is essential because KRAS inhibition alone has little effect in bowel cancer. Responses are still modest and short-lived compared with EGFR or ALK inhibitors in lung cancer.
It is the definitive negative result for unselected checkpoint blockade in microsatellite-stable colorectal cancer, and the reason later attempts have moved to Fc-enhanced CTLA-4 antibodies, TGF-beta blockade and vaccines rather than PD-L1 plus MEK.
Regorafenib is the standard third-line treatment for GIST after imatinib and sunitinib.
The start of the refractory-line era in colorectal cancer: a survival benefit measured in weeks, with real toxicity, which is why dose-escalation strategies and patient selection have occupied the field since.
Query for this drug: (TITLE:"Regorafenib" OR ABSTRACT:"Regorafenib" OR TITLE:"Stivarga" OR ABSTRACT:"Stivarga") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Regorafenib, not a curated reading list.
Shares TATE and Pembrolizumab (MK3475) in mCRC and NSCLC, Injection of SHR-A1811 Versus Physician Choiced Treatment in Patients With Advanced Colorectal Cancer Who Had Failed to Respond to Oxaliplatin, 5-fu, , Teclison, 5-Fluorouracil/Leucovorin (5FU/LV) in Combination With Regorafenib in Patients With Metastatic Colorectal Cancer.
Shares CONCUR, CORRECT, KRAS G12C-mutant colorectal cancer, VEGF / VEGFR.
Shares TIE2 receptor (TEK), Anti-VEGF class toxicities (hypertension, proteinuria, bleeding, perforation), Hand-foot syndrome and hand-foot skin reaction, The angiogenic switch & tumour vessels.
Shares CRAF (RAF1), Hand-foot syndrome and hand-foot skin reaction, The angiogenic switch & tumour vessels, Hepatocellular carcinoma (KEGG map).
Shares Injection of SHR-A1811 Versus Physician Choiced Treatment in Patients With Advanced Colorectal Cancer Who Had Failed to Respond to Oxaliplatin, 5-fu, , A Study Comparing BL-M07D1 With Physician's Choice Therapy in Patients With HER2 IHC3+ Advanced Colorectal Cancer Who Failed Prior Treatment With Oxaliplatin, F, Colorectal cancer drugs in England: what NICE has recommended, The angiogenic switch & tumour vessels.
Shares GRID: regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib, KIT exon 11-mutant GIST, Imatinib-resistant GIST, The angiogenic switch & tumour vessels.
Shares PDGFRA D842V-mutant GIST, KIT exon 11-mutant GIST, Imatinib-resistant GIST, KIT.
Shares KIT exon 11-mutant GIST, Imatinib-resistant GIST, KIT, Gastrointestinal stromal tumour (GIST).