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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FDA approval date
EMA approval date
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Study first post date
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Commercial
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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 neoplasms | D001943 | EFO_0003869 | C50 | 3 | 3 | — | — | — | 5 |
| Neoplasms | D009369 | — | C80 | 3 | 2 | — | — | — | 4 |
| Non-small-cell lung carcinoma | D002289 | — | — | — | 1 | — | — | — | 1 |
| Lung neoplasms | D008175 | HP_0100526 | C34.90 | — | 1 | — | — | — | 1 |
| Colorectal neoplasms | D015179 | — | — | — | 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 name | SAPITINIB |
| INN | sapitinib |
| 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 class | tyrosine 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-ID | 848942-61-0 |
| RxCUI | — |
| ChEMBL ID | CHEMBL2408045 |
| ChEBI ID | — |
| PubChem CID | 11488320 |
| DrugBank | — |
| UNII ID | 3499328002 (ChemIDplus, GSRS) |
Target
Agency Approved
ERBB3
ERBB3
ERBB2
ERBB2
EGFR
EGFR
Organism
Homo sapiens
Gene name
ERBB3
Gene synonyms
HER3
NCBI Gene ID
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
Mouse ortholog
Erbb3 (13867)
receptor tyrosine-protein kinase erbB-3 (Q8K317)
Alternate
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Variants
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Financial
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Trends
PubMed Central
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Safety
Black-box Warning
No Black-box warning
Adverse Events
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