Crenolanib
Crenolanib is a small molecule pharmaceutical. It is currently being investigated in clinical studies. The pharmaceutical is active against receptor-type tyrosine-protein kinase FLT3, platelet-derived growth factor receptor alpha, and platelet-derived growth factor receptor beta. In addition, it is known to target mast/stem cell growth factor receptor Kit and macrophage colony-stimulating factor 1 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
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Agency Specific
FDA
EMA
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Patent Expiration
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ATC Codes
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HCPCS
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Clinical
Clinical Trials
20 clinical trials
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Indications Phases 4
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Myeloid leukemia acute | D015470 | C92.0 | 3 | 6 | 3 | — | — | 10 | |
| Gastrointestinal stromal tumors | D046152 | EFO_0000505 | C49.A | — | 1 | 1 | — | — | 2 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Non-small-cell lung carcinoma | D002289 | — | 1 | — | — | — | 1 | ||
| Glioma | D005910 | EFO_0000520 | — | 1 | — | — | — | 1 | |
| Glioblastoma | D005909 | EFO_0000515 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Neoplasms | D009369 | C80 | 1 | — | — | — | — | 1 | |
| Diffuse intrinsic pontine glioma | D000080443 | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | CRENOLANIB |
| INN | crenolanib |
| Description | Crenolanib is a member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a 8-(4-aminopiperidin-1-yl)quinolin-2-yl group at position 1 and by a (3-methyloxetan-3-yl)methoxy group at position 5. It is an inhibitor of type III tyrosine kinases, PDGFRalpha/beta and FLT3 (IC50 of 11, 3.2, and 4 nM). Currently under clinical development for the treatment of acute myeloid leukemia. It has a role as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an angiogenesis inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of benzimidazoles, an aromatic ether, a member of quinolines, a member of oxetanes, an aminopiperidine and a tertiary amino compound. |
| Classification | Small molecule |
| Drug class | angiogenesis inhibitors |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | CC1(COc2ccc3c(c2)ncn3-c2ccc3cccc(N4CCC(N)CC4)c3n2)COC1 |
Identifiers
| PDB | 6JOJ |
| CAS-ID | 670220-88-9 |
| RxCUI | — |
| ChEMBL ID | CHEMBL2105728 |
| ChEBI ID | — |
| PubChem CID | 10366136 |
| DrugBank | DB11832 |
| UNII ID | LQF7I567TQ (ChemIDplus, GSRS) |
Target
Agency Approved
FLT3
FLT3
PDGFRA
PDGFRA
PDGFRB
PDGFRB
Organism
Homo sapiens
Gene name
FLT3
Gene synonyms
CD135, FLK2, STK1
NCBI Gene ID
Protein name
receptor-type tyrosine-protein kinase FLT3
Protein synonyms
CD135, CD135 antigen, fetal liver kinase 2, Fetal liver kinase-2, FL cytokine receptor, FLK-2, FLT-3, fms related tyrosine kinase 3, Fms-like tyrosine kinase 3, growth factor receptor tyrosine kinase type III, Stem cell tyrosine kinase 1, STK-1
Uniprot ID
Mouse ortholog
Flt3 (14255)
receptor-type tyrosine-protein kinase FLT3 (Q00342)
Alternate
KIT
KIT
CSF1R
CSF1R
Organism
Homo sapiens
Gene name
KIT
Gene synonyms
SCFR
NCBI Gene ID
Protein name
mast/stem cell growth factor receptor Kit
Protein synonyms
c-Kit protooncogene, CD117, p145 c-kit, PBT, Piebald trait protein, Proto-oncogene c-Kit, proto-oncogene tyrosine-protein kinase Kit, Tyrosine-protein kinase Kit, v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog, v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene-like protein
Uniprot ID
Mouse ortholog
Kit (16590)
mast/stem cell growth factor receptor Kit (Q8C8K9)
Variants
Clinical Variant
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Financial
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Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 930 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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4 adverse events reported
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