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Brivanib alaninate
Brivanib alaninate is a small molecule pharmaceutical. It is currently being investigated in clinical studies. The pharmaceutical is active against vascular endothelial growth factor receptor 2. In addition, it is known to target fibroblast growth factor receptor 1 and vascular endothelial growth factor receptor 1.
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Commercial
Therapeutic Areas
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Trade Name
FDA
EMA
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Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
No data
Labels
FDA
EMA
No data
Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
No data
HCPCS
No data
Clinical
Clinical Trials
26 clinical trials
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Indications Phases 4
No data
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Liver neoplasmsD008113EFO_1001513C22.02—3——5
Colorectal neoplasmsD015179221——4
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Hepatocellular carcinomaD006528C22.013———3
Uterine cervical neoplasmsD002583—2———2
Squamous cell carcinomaD002294—2———2
Renal cell carcinomaD002292—1———1
Endometrioid carcinomaD018269—1———1
Acinar cell carcinomaD018267—1———1
Pancreatic neoplasmsD010190EFO_0003860C25—1———1
Non-small-cell lung carcinomaD002289—1———1
SarcomaD012509—1———1
Transitional cell carcinomaD002295—1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
NeoplasmsD009369C805————5
Gastrointestinal neoplasmsD005770C26.92————2
Ovarian neoplasmsD010051EFO_0003893C561————1
Neoplasm metastasisD009362EFO_00097081————1
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameBRIVANIB ALANINATE
INNbrivanib alaninate
Description
Brivanib alaninate is a carboxylic ester resulting from the formal condensation of the carboxy group of L-alanine with the hydroxy group of brivanib. It is a prodrug of brivanib (BMS-540215), a potent oral dual inhibitor of VEGFR-2 and FGFR-1 (IC50 of 25 nM and 148 nM, respectively) and was in development for the treatment of hepatocellular and colon carcinomas. It has a role as an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, a prodrug, an apoptosis inducer, a fibroblast growth factor receptor antagonist and an angiogenesis inhibitor. It is a pyrrolotriazine, an aromatic ether, a fluoroindole, a diether, a carboxylic ester and a L-alanine derivative. It is functionally related to a brivanib.
Classification
Small molecule
Drug classangiogenesis inhibitors
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
Cc1cc2c(F)c(Oc3ncnn4cc(OC[C@@H](C)OC(=O)[C@H](C)N)c(C)c34)ccc2[nH]1
Identifiers
PDB—
CAS-ID649735-63-7
RxCUI—
ChEMBL IDCHEMBL270995
ChEBI ID—
PubChem CID11154925
DrugBankDB11865
UNII IDU2Y5OFN795 (ChemIDplus, GSRS)
Target
Agency Approved
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)
Alternate
FGFR1
FGFR1
FLT1
FLT1
Organism
Homo sapiens
Gene name
FGFR1
Gene synonyms
BFGFR, CEK, FGFBR, FLG, FLT2, HBGFR
NCBI Gene ID
Protein name
fibroblast growth factor receptor 1
Protein synonyms
Basic fibroblast growth factor receptor 1, bFGF-R-1, BFGFR, CD331, FGFR1/PLAG1 fusion, FLT-2, FMS-like tyrosine kinase 2, fms-related tyrosine kinase 2, heparin-binding growth factor receptor, hydroxyaryl-protein kinase, N-sam, Proto-oncogene c-Fgr
Uniprot ID
Mouse ortholog
Fgfr1 (14182)
fibroblast growth factor receptor 1 (P16092)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 240 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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149 adverse events reported
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