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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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Commercial
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Clinical
Clinical Trials
43 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Type 2 diabetes mellitusD003924EFO_0001360E11123
Diabetes mellitusD003920EFO_0000400E08-E13112
ThrombosisD01392711
Coronary diseaseD00332711
Coronary artery diseaseD003324I25.111
Myocardial ischemiaD017202EFO_1001375I20-I2511
Indications Phases 3
No data
Indications Phases 2
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MeSH
Ontology
ICD-10
Ph 1
Ph 2
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SyndromeD013577213
LeukemiaD007938C95123
Hematologic neoplasmsD019337112
Fallopian tube neoplasmsD005185212
Ovarian epithelial carcinomaD000077216212
GlioblastomaD005909EFO_0000515212
AstrocytomaD001254EFO_0000271212
Brain neoplasmsD001932EFO_0003833C71222
Myelodysplastic syndromesD009190D4622
Precursor cell lymphoblastic leukemia-lymphomaD054198C91.022
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Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Multiple myelomaD009101C90.011
Blast crisisD00175211
Colorectal neoplasmsD01517911
Rectal neoplasmsD01200411
CarcinomaD002277C80.011
Hepatocellular carcinomaD006528C22.011
Liver neoplasmsD008113EFO_1001513C22.011
LymphomaD008223C85.911
B-cell chronic lymphocytic leukemiaD015451C91.111
MelanomaD00854511
Indications Without Phase
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)Loading
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
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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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