Stivarga(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
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| neoplasms | D009369 |
| digestive system diseases | D004066 |
Trade Name
FDA
EMA
Stivarga
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| stivarga | New Drug Application | 2020-12-09 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| colorectal neoplasms | — | D015179 | — |
| hepatocellular carcinoma | — | D006528 | C22.0 |
| gastrointestinal stromal tumors | EFO_0000505 | D046152 | C49.A |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
REGORAFENIB, STIVARGA, BAYER HLTHCARE | |||
| 2024-04-27 | ODE-139 | ||
HCPCS
No data
Clinical
Clinical Trials
317 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 neoplasms | D015179 | — | — | 29 | 82 | 18 | 4 | 29 | 143 |
| Neoplasms | D009369 | — | C80 | 29 | 21 | — | 1 | 2 | 44 |
| Gastrointestinal stromal tumors | D046152 | EFO_0000505 | C49.A | 5 | 14 | 2 | 1 | 7 | 26 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Carcinoma | D002277 | — | C80.0 | 10 | 31 | 3 | — | 10 | 48 |
| Hepatocellular carcinoma | D006528 | — | C22.0 | 7 | 25 | 3 | — | 13 | 44 |
| Liver neoplasms | D008113 | EFO_1001513 | C22.0 | 5 | 24 | 3 | — | 12 | 41 |
| Neoplasm metastasis | D009362 | EFO_0009708 | — | 4 | 14 | 2 | — | 2 | 20 |
| Adenocarcinoma | D000230 | — | — | 6 | 15 | 1 | — | — | 18 |
| Sarcoma | D012509 | — | — | 2 | 10 | 1 | — | 1 | 12 |
| Colonic neoplasms | D003110 | — | C18 | 3 | 6 | 1 | — | 1 | 11 |
| Glioblastoma | D005909 | EFO_0000515 | — | 2 | 4 | 1 | — | 2 | 7 |
| Esophageal neoplasms | D004938 | — | C15 | 3 | 5 | 1 | — | — | 6 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Renal cell carcinoma | D002292 | EFO_0000376 | — | 3 | 7 | — | — | 1 | 9 |
| Rectal neoplasms | D012004 | — | — | 3 | 6 | — | — | — | 9 |
| Osteosarcoma | D012516 | — | — | 1 | 6 | — | — | 1 | 7 |
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | 1 | 5 | — | — | — | 6 |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | 1 | 6 | — | — | — | 6 |
| Gastrointestinal neoplasms | D005770 | — | C26.9 | 2 | 4 | — | — | 2 | 6 |
| Myeloid leukemia acute | D015470 | — | C92.0 | 4 | 1 | — | — | 1 | 5 |
| Recurrence | D012008 | — | — | 2 | 2 | — | — | 1 | 5 |
| Non-small-cell lung carcinoma | D002289 | — | — | 3 | 4 | — | — | — | 5 |
| Stomach neoplasms | D013274 | EFO_0003897 | C16 | 3 | 5 | — | — | — | 5 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Leukemia | D007938 | — | C95 | 2 | — | — | — | 1 | 3 |
| Precursor cell lymphoblastic leukemia-lymphoma | D054198 | — | — | 1 | — | — | — | 1 | 2 |
| Lymphoid leukemia | D007945 | — | C91 | 1 | — | — | — | 1 | 2 |
| Myelodysplastic syndromes | D009190 | — | D46 | 2 | — | — | — | — | 2 |
| Preleukemia | D011289 | — | — | 2 | — | — | — | — | 2 |
| Pharmacokinetics | D010599 | — | — | 2 | — | — | — | — | 2 |
| Myeloproliferative disorders | D009196 | — | D47.1 | 1 | — | — | — | — | 1 |
| Primary myelofibrosis | D055728 | — | D47.4 | 1 | — | — | — | — | 1 |
| Lymphoma | D008223 | — | C85.9 | 1 | — | — | — | — | 1 |
| B-cell chronic lymphocytic leukemia | D015451 | — | C91.1 | 1 | — | — | — | — | 1 |
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Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Acute disease | D000208 | — | — | — | — | — | — | 1 | 1 |
| Disease progression | D018450 | — | — | — | — | — | — | 1 | 1 |
| Progression-free survival | D000077982 | — | — | — | — | — | — | 1 | 1 |
| Leiomyosarcoma | D007890 | — | — | — | — | — | — | 1 | 1 |
| Malignant fibrous histiocytoma | D051677 | — | — | — | — | — | — | 1 | 1 |
| Therapeutic chemoembolization | D016461 | — | — | — | — | — | — | 1 | 1 |
| Covid-19 | D000086382 | — | — | — | — | — | — | 1 | 1 |
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Regorafenib |
| INN | regorafenib |
| 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 class | rapidly accelerated fibrosarcoma (RAF) kinase inhibitors |
| Image (chem structure or protein) |  |
| 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-ID | 755037-03-7 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1946170 |
| ChEBI ID | 68647 |
| PubChem CID | 11167602 |
| DrugBank | DB08896 |
| UNII ID | 24T2A1DOYB (ChemIDplus, GSRS) |
Target
Agency Approved
BRAF
BRAF
Organism
Homo sapiens
Gene name
BRAF
Gene synonyms
BRAF1, RAFB1
NCBI Gene ID
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
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
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
Mouse ortholog
Kdr (16542)
vascular endothelial growth factor receptor 2 (Q8VCD0)
Variants
No data
Financial
No data
Trends
PubMed Central
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Safety
Black-box Warning
Black-box warning for: Stivarga
Adverse Events
Top Adverse Reactions
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9,898 adverse events reported
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