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Zotiraciclib
Zotiraciclib is a small molecule pharmaceutical. It is currently being investigated in clinical studies. It is known to target receptor-type tyrosine-protein kinase FLT3, cyclin-dependent kinase 1, cyclin-dependent kinase 3, macrophage colony-stimulating factor 1 receptor, cyclin-dependent kinase 2, cyclin-dependent kinase 9, tyrosine-protein kinase JAK2, cyclin-dependent kinase 5, non-receptor tyrosine-protein kinase TYK2, and tyrosine-protein kinase JAK1.
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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
Indications Phases 4
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Indications Phases 3
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Indications Phases 2
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Indications Phases 1
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Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameZOTIRACICLIB
INNzotiraciclib
Description
Zotiraciclib (TG02) is a potent oral spectrum selective[clarification needed] kinase inhibitor for the treatment of cancer. It was discovered in Singapore by S*BIO Pte Ltd and falls under the category of small molecule macrocycles. It crosses the blood brain barrier and acts by depleting Myc through the inhibition of cyclin-dependent kinase 9 (CDK9). It is one of a number of CDK inhibitors under investigation; others targeting CDK9 for the treatment of acute myeloid leukemia include alvocidib and atuveciclib. Myc overexpression is a known factor in many cancers, with 80 percent of glioblastomas characterized by this property. Zotiraciclib has been granted orphan drug designation by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of gliomas.
Classification
Small molecule
Drug classcyclin dependent kinase inhibitors (formerly-cidib)
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
CN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1
Identifiers
PDB—
CAS-ID1204918-72-8
RxCUI—
ChEMBL IDCHEMBL1944698
ChEBI ID—
PubChem CID16739650
DrugBank—
UNII ID40D08182TT (ChemIDplus, GSRS)
Target
Agency Approved
No data
Alternate
FLT3
FLT3
CDK1
CDK1
CDK3
CDK3
CSF1R
CSF1R
CDK2
CDK2
CDK9
CDK9
JAK2
JAK2
CDK5
CDK5
TYK2
TYK2
JAK1
JAK1
Organism
Homo sapiens
Gene name
FLT3
Gene synonyms
CD135, FLK2, STK1
NCBI Gene ID
2322
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
Q13414
Mouse ortholog
Flt3 (14255)
receptor-type tyrosine-protein kinase FLT3 (Q00342)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
0 adverse events reported
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