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Drug ReportsPREXASERTIB
PREXASERTIB
Prexasertib is a small molecule pharmaceutical. It is currently being investigated in clinical studies. It is known to target serine/threonine-protein kinase Chk2, serine/threonine-protein kinase Chk1, and ribosomal protein S6 kinase alpha-1.
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5D
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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
20 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
CarcinomaD002277C80.0122
Urologic neoplasmsD014571C64-C68111
Ovarian neoplasmsD010051EFO_0003893C56111
Endometrial neoplasmsD016889EFO_0004230111
Uterine neoplasmsD014594EFO_0003859C55111
Endometrioid carcinomaD018269111
Transitional cell carcinomaD002295111
AdenocarcinomaD000230111
Ovarian epithelial carcinomaD000077216111
Squamous cell carcinoma of head and neckD00007719511
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Indications Phases 1
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Indications Without Phase
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common namePREXASERTIB
INNprexasertib
Description
Prexasertib (LY2606368) is a small molecule checkpoint kinase inhibitor, mainly active against CHEK1, with minor activity against CHEK2. This causes induction of DNA double-strand breaks resulting in apoptosis. It was developed by Eli Lilly but the company announced in 2019 it was dropping prexasertib from active development, although clinical trials continue. Research continues into the efficacy of prexasertib in treatment of acute myeloid leukemia, myelodysplastic syndrome, rhabdomyosarcoma, and medulloblastoma.
Classification
Small molecule
Drug classserine/threonine kinase inhibitors
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
COc1cccc(OCCCN)c1-c1cc(Nc2cnc(C#N)cn2)n[nH]1
Identifiers
PDB
CAS-ID1234015-52-1
RxCUI
ChEMBL IDCHEMBL3544911
ChEBI ID
PubChem CID
DrugBank
UNII ID820NH671E6 (ChemIDplus, GSRS)
Target
Agency Approved
No data
Alternate
CHEK2
CHEK2
CHEK1
CHEK1
RPS6KA1
RPS6KA1
Organism
Homo sapiens
Gene name
CHEK2
Gene synonyms
CDS1, CHK2, RAD53
NCBI Gene ID
Protein name
serine/threonine-protein kinase Chk2
Protein synonyms
Cds1 homolog, Checkpoint kinase 2, checkpoint-like protein CHK2, CHK2 checkpoint homolog, hCds1, Hucds1
Uniprot ID
Mouse ortholog
Chek2 (50883)
serine/threonine-protein kinase Chk2 (Q9Z265)
Variants
No data
Financial
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Trends
PubMed Central
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Additional graphs summarizing 957 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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3 adverse events reported
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