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Drug ReportsRegorafenib
Stivarga(regorafenib)
Regorafenib, Stivarga (regorafenib) is a small molecule pharmaceutical. Regorafenib was first approved as Stivarga on 2012-09-27. It is used to treat colorectal neoplasms, gastrointestinal stromal tumors, and hepatocellular carcinoma in the USA. It has been approved in Europe to treat colorectal neoplasms. The pharmaceutical is active against serine/threonine-protein kinase B-raf. In addition, it is known to target vascular endothelial growth factor receptor 2.
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Commercial
Clinical
Drug
Target
Variants
Financial
Trends
Safety
Events Timeline
5D
1M
3M
6M
YTD
1Y
2Y
5Y
Max
Events
FDA approval date
EMA approval date
Patent expiration date
Study first post date
Last update post date
Start date
Primary completion date
Completion date
Results first post date
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
neoplasmsD009369
digestive system diseasesD004066
Trade Name
FDA
EMA
Stivarga (discontinued: Regorafenib)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Regorafenib
Tradename
Company
Number
Date
Products
STIVARGABayerN-203085 RX2012-09-27
1 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
stivargaNew Drug Application2025-02-25
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
colorectal neoplasms—D015179—
hepatocellular carcinoma—D006528C22.0
gastrointestinal stromal tumorsEFO_0000505D046152C49.A
Agency Specific
FDA
EMA
Expiration
Code
REGORAFENIB, STIVARGA, BAYER HLTHCARE
2024-04-27ODE-139
Patent Expiration
Patent
Expires
Flag
FDA Information
Regorafenib, Stivarga, Bayer Hlthcare
99572322032-07-09DP
94581072031-04-08DP
86375532031-02-16DS, DP
86801242030-06-02U-1506
ATC Codes
L: Antineoplastic and immunomodulating agents
— L01: Antineoplastic agents
— L01E: Protein kinase inhibitors, antineoplastic and immunomodulating agents
— L01EX: Other protein kinase inhibitors in atc
— L01EX05: Regorafenib
HCPCS
No data
Clinical
Clinical Trials
339 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Colorectal neoplasmsD015179——321421544
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
CarcinomaD002277—C80.0282—213
Hepatocellular carcinomaD006528—C22.0262—211
Liver neoplasmsD008113EFO_1001513C22.0262—211
Gastrointestinal stromal tumorsD046152EFO_0000505C49.A241—410
Neoplasm metastasisD009362EFO_0009708—131——5
Colonic neoplasmsD003110—C18—21——3
GlioblastomaD005909EFO_0000515——21——2
RecurrenceD012008———11——1
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
NeoplasmsD009369—C80178——225
SarcomaD012509——14———4
Stomach neoplasmsD013274EFO_0003897C1613———3
Ovarian neoplasmsD010051EFO_0003893C56—3———3
Renal cell carcinomaD002292EFO_0000376—12———2
Urologic neoplasmsD014571—C64-C6812———2
Non-small-cell lung carcinomaD002289——12———2
Triple negative breast neoplasmsD064726——12———2
Thyroid neoplasmsD013964EFO_0003841—12———2
Biliary tract neoplasmsD001661—C24.912———2
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Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
PharmacokineticsD010599——2————2
OncogenesD009857——1————1
Myeloid leukemia acuteD015470—C92.01————1
Renal insufficiencyD051437—N191————1
Dietary fatsD004041——1————1
Ewing sarcomaD012512EFO_0000173—1————1
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Covid-19D000086382—U07.1————11
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameRegorafenib
INNregorafenib
Description
Regorafenib is a pyridinecarboxamide obtained by condensation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]pyridine-2-carboxylic acid with methylamine. Used for for the treatment of metastatic colorectal cancer in patients who have previously received chemotherapy, anti-EGFR or anti-VEGF therapy. It has a role as an antineoplastic agent, a tyrosine kinase inhibitor and a hepatotoxic agent. It is an aromatic ether, a pyridinecarboxamide, a member of monochlorobenzenes, a member of (trifluoromethyl)benzenes, a member of monofluorobenzenes and a member of phenylureas.
Classification
Small molecule
Drug classrapidly accelerated fibrosarcoma (RAF) kinase inhibitors
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)c(F)c2)ccn1
Identifiers
PDB—
CAS-ID755037-03-7
RxCUI—
ChEMBL IDCHEMBL1946170
ChEBI ID68647
PubChem CID11167602
DrugBankDB08896
UNII ID24T2A1DOYB (ChemIDplus, GSRS)
Target
Agency Approved
BRAF
BRAF
Organism
Homo sapiens
Gene name
BRAF
Gene synonyms
BRAF1, RAFB1
NCBI Gene ID
673
Protein name
serine/threonine-protein kinase B-raf
Protein synonyms
94 kDa B-raf protein, B-Raf proto-oncogene serine/threonine-protein kinase (p94), B-Raf serine/threonine-protein, murine sarcoma viral (v-raf) oncogene homolog B1, p94, Proto-oncogene B-Raf, v-raf murine sarcoma viral oncogene homolog B, v-Raf murine sarcoma viral oncogene homolog B1
Uniprot ID
Q9Y6T3
Mouse ortholog
Braf (109880)
serine/threonine-protein kinase B-raf (Q3USE9)
Alternate
KDR
KDR
Organism
Homo sapiens
Gene name
KDR
Gene synonyms
FLK1, VEGFR2
NCBI Gene ID
3791
Protein name
vascular endothelial growth factor receptor 2
Protein synonyms
CD309, Fetal liver kinase 1, fetal liver kinase-1, FLK-1, KDR, Kinase insert domain receptor, kinase insert domain receptor (a type III receptor tyrosine kinase), Protein-tyrosine kinase receptor flk-1, soluble VEGFR2, tyrosine kinase growth factor receptor
Uniprot ID
Q14178
Mouse ortholog
Kdr (16542)
vascular endothelial growth factor receptor 2 (Q8VCD0)
Variants
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 13,888 documents
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Safety
Black-box Warning
Black-box warning for: Stivarga
Adverse Events
Top Adverse Reactions
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10,768 adverse events reported
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