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Sapitinib
Sapitinib is a small molecule pharmaceutical. It is currently being investigated in clinical studies. The pharmaceutical is active against receptor tyrosine-protein kinase erbB-3, receptor tyrosine-protein kinase erbB-2, and epidermal growth factor receptor.
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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)
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Labels
FDA
EMA
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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
12 clinical trials
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Indications Phases 4
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Indications Phases 3
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Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Breast neoplasmsD001943EFO_0003869C5033———5
NeoplasmsD009369C8022———3
Non-small-cell lung carcinomaD002289—1———1
Colorectal neoplasmsD015179—1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Healthy volunteers/patients—3————3
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameSAPITINIB
INNsapitinib
Description
Sapitinib is a member of the class of quinazolines that is 4-amino-7-methoxyquinazoline in which the amino group has been substituted by a 3-chloro-2-fluorophenyl group and in which position 6 of the quinoline ring has been substituted by a {1-[2-(methylamino)-2-oxoethyl]piperidin-4-yl}oxy group. Sapitinib is a dual tyrosine kinase inhibitor (TKI) of epithelial growth factor receptors (EGFR) HER2 and HER3. It has a role as an epidermal growth factor receptor antagonist and an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is a member of quinazolines, a member of piperidines, a member of monofluorobenzenes, a member of monochlorobenzenes, an aromatic ether, a secondary amino compound and a tertiary amino compound.
Classification
Small molecule
Drug classtyrosine kinase inhibitors
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
CNC(=O)CN1CCC(Oc2cc3c(Nc4cccc(Cl)c4F)ncnc3cc2OC)CC1
Identifiers
PDB—
CAS-ID848942-61-0
RxCUI—
ChEMBL IDCHEMBL2408045
ChEBI ID—
PubChem CID11488320
DrugBank—
UNII ID3499328002 (ChemIDplus, GSRS)
Target
Agency Approved
ERBB3
ERBB3
ERBB2
ERBB2
EGFR
EGFR
Organism
Homo sapiens
Gene name
ERBB3
Gene synonyms
HER3
NCBI Gene ID
2065
Protein name
receptor tyrosine-protein kinase erbB-3
Protein synonyms
human epidermal growth factor receptor 3, Proto-oncogene-like protein c-ErbB-3, Tyrosine kinase-type cell surface receptor HER3, v-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3
Uniprot ID
P21860
Mouse ortholog
Erbb3 (13867)
receptor tyrosine-protein kinase erbB-3 (Q8K317)
Alternate
No data
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 132 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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2 adverse events reported
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