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Drug ReportsZotiraciclib
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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5D
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5Y
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FDA approval date
EMA approval date
Patent expiration date
Study first post date
Last update post date
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Commercial
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Clinical
Clinical Trials
43 clinical trials
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Indications Phases 4
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Indications Phases 3
No data
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Multiple sclerosisD009103EFO_0003885G35—1———1
Disease progressionD018450———1———1
Neoplasm metastasisD009362EFO_0009708——1———1
Autoimmune diseasesD001327EFO_0000540M30-M36—1———1
Nervous system diseasesD009422—G00-G99—1———1
Autoimmune diseases of the nervous systemD020274———1———1
Chronic progressive multiple sclerosisD020528EFO_0003840——1———1
SclerosisD012598———1———1
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)
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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
TYK2
TYK2
Organism
Homo sapiens
Gene name
TYK2
Gene synonyms
NCBI Gene ID
Protein name
non-receptor tyrosine-protein kinase TYK2
Protein synonyms
Uniprot ID
Mouse ortholog
Tyk2 (54721)
non-receptor tyrosine-protein kinase TYK2 (Q9R117)
Variants
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
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1 adverse events reported
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