Regorafenib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2012
- First approval year
- 2012
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Regorafenib
- Molecular weight
- 482.82
- Structure (SMILES)
- CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)c(F)c2)ccn1
- stivarga
- Stivarga
- bay 73 4506
- bay 73 4506 monohydrate
- BAY 73-4506
- BAY 73-4506 monohydrate
- bay 734506
- bay 734506 monohydrate
- BAY-73-4506
- BAY-73-4506 MONOHYDRATE
- BAY-734506
- BAY-734506 MONOHYDRATE
- cadonilimab regorafenib
- regorafenib
- Regorafenib
- Regorafenib (BAY 73-4506)
- Regorafenib (BAY73-4506)
- Regorafenib (CT)
- Regorafenib (Stivarga)
- regorafenib [INN]
- REGORAFENIB [MI]
- REGORAFENIB [VANDF]
- Regorafenib [WHO-DD]
- Regorafenib 160 mg
- Regorafenib 20MG
- Regorafenib 30 mg capsules
- Regorafenib 30 MG Oral Tablet
And 14 more, listed on the interactive page.
- ATC classification codes
- L01EX05
Sources for recorded values
- CAS registry numbers
- 755037-03-7
- ChEMBL ID
- CHEMBL1946170
- InChIKey
- FNHKPVJBJVTLMP-UHFFFAOYSA-N
- PubChem compound IDs
- 11167602
- RxNorm IDs (RxCUI)
- 1312397
- FDA ingredient codes (UNII)
- 24T2A1DOYB
- Applicant
- BAYER HLTHCARE
- Approval date
- 27 Sept 2012
- Application number
- NDA203085
- Status
- Authorised
- Status date
- 26 Aug 2013
- Authorisation date
- 26 Aug 2013
- Approved indications
- Stivarga is indicated as monotherapy for the treatment of adult patients with: metastatic colorectal cancer (CRC) who have been previously treated with, or are not considered candidates for, available therapies - these include fluoropyrimidine-based chemotherapy, an anti-VEGF therapy and an anti-EGFR therapy; unresectable or metastatic gastrointestinal stromal tumors (GIST) who progressed on or are intolerant to prior treatment with imatinib and sunitinib; hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.
- Product number
- EMEA/H/C/002573
- Authorisation holder
- Bayer Pharma AG
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Colorectal Neoplasms
European medicines record
- Patents
- 4
- Designations
- 4
- Earliest recorded loss of exclusivity
- 9 Jul 2032
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- regorafenib
- Type
- Synthetic organic
- Drug name stem
- -rafenib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- B-Raf proto-oncogene, serine/threonine kinase
- Gene symbol
- BRAF
- Protein identifier
- P15056
- Median affinity
- 7.55
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- kinase insert domain receptor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Median affinity
- 7.9
- Affinity units
- pIC50
- Mechanism
- Discoidin domain-containing receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Discoidin domain-containing receptor 2
- Protein identifier
- Q16832
- Mechanism
- Ephrin type-A receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Ephrin type-A receptor 2
- Protein identifier
- P29317
- Mechanism
- Fibroblast growth factor receptor 1 inhibitor
- Action type
- Inhibitor
- Target
- Fibroblast growth factor receptor 1
- Protein identifier
- P11362
- Mechanism
- Fibroblast growth factor receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Fibroblast growth factor receptor 2
- Protein identifier
- P21802
- Mechanism
- MAP kinase p38 beta inhibitor
- Action type
- Inhibitor
- Target
- Mitogen-activated protein kinase 11
- Protein identifier
- Q15759
- Mechanism
- Nerve growth factor receptor Trk-A inhibitor
- Action type
- Inhibitor
- Target
- High affinity nerve growth factor receptor
- Protein identifier
- P04629
- Mechanism
- Platelet-derived growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Platelet-derived growth factor receptor
- Protein identifier
- P09619
- Mechanism
- Platelet-derived growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Platelet-derived growth factor receptor
- Protein identifier
- P16234
- Mechanism
- Serine/threonine-protein kinase B-raf inhibitor
- Action type
- Inhibitor
- Target
- Serine/threonine-protein kinase B-raf
- Protein identifier
- P15056
- Mechanism
- Serine/threonine-protein kinase RAF inhibitor
- Action type
- Inhibitor
- Target
- RAF proto-oncogene serine/threonine-protein kinase
- Protein identifier
- P04049
- Mechanism
- Stem cell growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Mast/stem cell growth factor receptor Kit
- Protein identifier
- P10721
- Mechanism
- Tyrosine-protein kinase ABL inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase ABL1
- Protein identifier
- P00519
- Mechanism
- Tyrosine-protein kinase FRK inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase FRK
- Protein identifier
- P42685
- Mechanism
- Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Proto-oncogene tyrosine-protein kinase receptor Ret
- Protein identifier
- P07949
- Mechanism
- Tyrosine-protein kinase TIE-2 inhibitor
- Action type
- Inhibitor
- Target
- Angiopoietin-1 receptor
- Protein identifier
- Q02763
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P17948
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P35916
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P35968
- Mechanism
- Discoidin domain-containing receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Discoidin domain-containing receptor 2
- Mechanism
- Ephrin type-A receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Ephrin type-A receptor 2
- Mechanism
- Fibroblast growth factor receptor 1 inhibitor
- Action type
- Inhibitor
- Target
- Fibroblast growth factor receptor 1
- Mechanism
- Fibroblast growth factor receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Fibroblast growth factor receptor 2
- Mechanism
- MAP kinase p38 beta inhibitor
- Action type
- Inhibitor
- Target
- Mitogen-activated protein kinase 11
- Mechanism
- Nerve growth factor receptor Trk-A inhibitor
- Action type
- Inhibitor
- Target
- High affinity nerve growth factor receptor
- Mechanism
- Platelet-derived growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Platelet-derived growth factor receptor
- Mechanism
- Serine/threonine-protein kinase B-raf inhibitor
- Action type
- Inhibitor
- Target
- Serine/threonine-protein kinase B-raf
- Mechanism
- Serine/threonine-protein kinase RAF inhibitor
- Action type
- Inhibitor
- Target
- RAF proto-oncogene serine/threonine-protein kinase
- Mechanism
- Stem cell growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Mast/stem cell growth factor receptor Kit
- Mechanism
- Tyrosine-protein kinase ABL inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase ABL1
- Mechanism
- Tyrosine-protein kinase FRK inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase FRK
- Mechanism
- Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Proto-oncogene tyrosine-protein kinase receptor Ret
- Mechanism
- Tyrosine-protein kinase TIE-2 inhibitor
- Action type
- Inhibitor
- Target
- Angiopoietin-1 receptor
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Action type
- Inhibitor
- Gene symbol
- BRAF
- Protein identifier
- P15056
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- EPHX2
- Protein identifier
- P34913
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Action type
- Inhibitor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Carcinoma, Adenoid Cystic
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000231
- Subject identifier
- D003528
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000365
- Subject identifier
- D015179
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000389
- Subject identifier
- D008545
- Condition
- Glioblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Liposarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000569
- Subject identifier
- D008080
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Osteosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000637
- Subject identifier
- D012516
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Sarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000691
- Subject identifier
- D012509
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001075
- Subject identifier
- D010051
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Rhabdomyosarcoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002918
- Subject identifier
- D012208
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003893
- Subject identifier
- D010051
- Condition
- Hemangiosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003968
- Subject identifier
- D006394
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0004142
- Subject identifier
- D015179
- Condition
- Cholangiocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005221
- Subject identifier
- D018281
- Condition
- Bile Duct Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005540
- Subject identifier
- D001650
- Condition
- Macular Degeneration
- Highest recorded phase
- 2
- Condition identifier
- EFO:0009606
- Subject identifier
- D008268
- Condition
- Bone Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:1000350
- Subject identifier
- D001859
- Condition
- Rectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000657
- Subject identifier
- D012004
And 16 more, listed on the interactive page.
- Condition identifier
- EFO_0000174
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000182
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000222
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000231
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000365
- Condition identifier
- EFO_0000519
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000637
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000681
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000691
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003893
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003968
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004142
- Condition identifier
- EFO_0004920
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005221
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005540
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000657
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001480
- Condition identifier
- EFO_1001480
- Highest recorded phase
- 4
- Condition identifier
- EFO_1001513
- Condition identifier
- EFO_1001949
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001951
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001961
- Highest recorded phase
- 2
And 77 more, listed on the interactive page.
Warnings
- Warning
- Black Box Warning
- Effect
- hepatotoxicity
Open Targets warnings
- Warning
- Black Box Warning
- Effect
- hepatotoxicity
- Country
- United States
- Event
- abdominal pain
- Reports
- 244
- Reporting signal score
- 138.351
- Event
- abdominal pain upper
- Reports
- 169
- Reporting signal score
- 111.216
- Event
- alpha 1 foetoprotein increased
- Reports
- 19
- Reporting signal score
- 62.0471
- Event
- ascites
- Reports
- 86
- Reporting signal score
- 115.348
- Event
- asthenia
- Reports
- 421
- Reporting signal score
- 326.333
- Event
- back pain
- Reports
- 146
- Reporting signal score
- 58.1083
- Event
- blister
- Reports
- 223
- Reporting signal score
- 426.451
- Event
- blood bilirubin increased
- Reports
- 116
- Reporting signal score
- 171.666
- Event
- blood pressure increased
- Reports
- 210
- Reporting signal score
- 224.476
- Event
- carcinoembryonic antigen increased
- Reports
- 60
- Reporting signal score
- 219.337
- Event
- colon cancer
- Reports
- 99
- Reporting signal score
- 237.101
- Event
- colon cancer metastatic
- Reports
- 24
- Reporting signal score
- 78.6843
- Event
- colorectal cancer
- Reports
- 119
- Reporting signal score
- 512.941
- Event
- colorectal cancer metastatic
- Reports
- 132
- Reporting signal score
- 632.47
- Event
- constipation
- Reports
- 205
- Reporting signal score
- 137.61
- Event
- decreased appetite
- Reports
- 544
- Reporting signal score
- 846.707
- Event
- dehydration
- Reports
- 237
- Reporting signal score
- 229.793
- Event
- diarrhoea
- Reports
- 690
- Reporting signal score
- 495.439
- Event
- dry mouth
- Reports
- 93
- Reporting signal score
- 89.8488
- Event
- dry skin
- Reports
- 141
- Reporting signal score
- 212.403
- Event
- dysphonia
- Reports
- 437
- Reporting signal score
- 1,131.24
- Event
- erythema
- Reports
- 159
- Reporting signal score
- 90.1444
- Event
- exercise tolerance decreased
- Reports
- 33
- Reporting signal score
- 70.117
- Event
- fatigue
- Reports
- 836
- Reporting signal score
- 693.921
- Event
- gait disturbance
- Reports
- 137
- Reporting signal score
- 76.7402
And 24 more, listed on the interactive page.
- NCT00664326
- NCT00934882
- NCT01289821
- NCT01584830
- NCT01939223
- NCT02096354
- NCT02195011
- NCT02465502
- NCT04776148
- NCT05328908
- NCT05426811
- NCT00960258
- NCT01096030
- NCT01117623
- NCT01287598
- NCT01322438
- NCT01339104
- NCT01853046
- NCT01973868
- NCT02001909
- NCT02106845
- NCT02168777
- NCT02466802
- NCT02925234
- NCT03406871
And 118 more, listed on the interactive page.
- Dose
- 160 mg
- Route
- Oral
- How often
- Once daily for the first 21 days of each 28-day cycle
- Do not take two doses on the same day
- Swallow whole with water
- Take after a low-fat meal with less than 600 calories and less than 30% fat
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 3
- Polar surface area
- 92.35
- Calculated partition coefficient (ALogP)
- 5.69
- Calculated partition coefficient (XLogP)
- 4.2
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 5
- Heavy atoms
- 33
- Molecular formula
- C21H15ClF4N4O3
- Monoisotopic mass
- 482.0768807
- Natural product
- No
- Recorded assays
- 1,391
- Active assays
- 387
- Confirmatory
- Other
- Screening
These details could not be displayed.
Related records
Trials (389)
- "Thymalfasin Immunotherapy Study with Triple Regimen in Advanced MSS/pMMR Colorectal Cancer"
- (VOYAGER) Study of Avapritinib vs Regorafenib in Patients With Locally Advanced Unresectable or Metastatic GIST
- [18F]FLT-PET as a Predictive Imaging Biomaker of Treatment Responses to Regorafenib
- [18F]Fluoroestradiol-PET/CT Companion Imaging Study to the FORESEE Trial
- [18F]Fluoroestradiol-PET/CT Imaging of Invasive Lobular Carcinoma
- [68 Ga]-DOTANOC PET/CT in GEP-NETs
- [68Ga]Ga-FAPI-46 in Staging of Head and Neck Carcinomas
- [68Ga]Ga-PentixaFor PET/CT in Acute Myocardial Inflammation
- 11C-methionine in Diagnostics and Management of Glioblastoma Multiforme Patients (GlioMET)
- 18F-DCFBC PET/CT in Prostate Cancer
- 18F-DCFPyL Positron Emission Tomography (PET)/Computed Tomography (CT) in Men With Prostate Cancer
- 5-Fluorouracil/Leucovorin (5FU/LV) in Combination With Regorafenib in Patients With Metastatic Colorectal Cancer
- 68Ga-NODAGA-RGD PET/ CT for Tumoral Neoangiogenesis
- 68Ga-NY104 PET/CT Guided Radiation Therapy in CcRCC.
- 68Ga-NYM096/177Lu-NYM096 in Metastatic ccRCC
- 68Ga-PSMA PET/CT in Prostate Cancer
- 68Ga-PSMA PET/CT in Prostate Cancer
- 68Ga-RM2 Compared to 68Ga-PSMA-617 PET/CT for Intermediate Risk Prostate Cancer Imaging
- 68Ga-RM2 Compared to 68Ga-PSMA-617 PET/CT for Prostate Cancer Imaging According to Various Metastatic Risks
- 89Zr-TLX250 for PET/CT Imaging of ccRCC - ZIRCON-CP Study
Approved for (6)
In development for (36)
- Acute myeloid leukemia Phase 1
- Adenoid cystic carcinoma Phase 2
- Angiosarcoma Phase 2
- Bile duct carcinoma Phase 2
- Biliary tract cancer Phase 2
- Bone cancer Phase 1
- Cholangiocarcinoma Phase 2
- Colon adenocarcinoma Phase 2
- Cutaneous melanoma Phase 2
- Digestive system cancer Phase 2
- Esophageal cancer Phase 3
- Ewing sarcoma Phase 1
- Exocrine pancreatic carcinoma Phase 2
- Fallopian tube cancer Phase 2
- Gastric cancer Phase 2
- Gastrointestinal stromal tumor Phase 3
- Glioblastoma Phase 2
- Grade III meningioma Phase 2
- Hepatocellular carcinoma Phase 3
- Intrahepatic cholangiocarcinoma Phase 2
Targets (18)
- ABL1 Tyrosine-protein kinase ABL inhibitor
- BRAF Serine/threonine-protein kinase B-raf inhibitor
- DDR2 Discoidin domain-containing receptor 2 inhibitor
- EPHA2 Ephrin type-A receptor 2 inhibitor
- FGFR1 Fibroblast growth factor receptor 1 inhibitor
- FGFR2 Fibroblast growth factor receptor 2 inhibitor
- FLT1 Vascular endothelial growth factor receptor inhibitor
- FLT4 Vascular endothelial growth factor receptor inhibitor
- FRK Tyrosine-protein kinase FRK inhibitor
- KDR Vascular endothelial growth factor receptor inhibitor
- KIT Stem cell growth factor receptor inhibitor
- MAPK11 MAP kinase p38 beta inhibitor
- NTRK1 Nerve growth factor receptor Trk-A inhibitor
- PDGFRA Platelet-derived growth factor receptor inhibitor
- PDGFRB Platelet-derived growth factor receptor inhibitor
- RAF1 Serine/threonine-protein kinase RAF inhibitor
- RET Tyrosine-protein kinase receptor RET inhibitor
- TEK Tyrosine-protein kinase TIE-2 inhibitor