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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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Financial
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5D
1M
3M
6M
YTD
1Y
2Y
5Y
Max
Events
FDA approval date
EMA approval date
Patent expiration date
Study first post date
Last update post date
Start date
Primary completion date
Completion date
Results first post date
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Commercial
No data
Clinical
Clinical Trials
20 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
Breast neoplasmsD001943EFO_0003869C5011———2
Triple negative breast neoplasmsD064726———1———1
Ovarian neoplasmsD010051EFO_0003893C56—1———1
Ovarian epithelial carcinomaD000077216———1———1
Lung neoplasmsD008175—C34.90—1———1
Small cell lung carcinomaD055752———1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
NeoplasmsD009369—C809————9
Colorectal neoplasmsD015179——2————2
Neoplasm metastasisD009362EFO_0009708—2————2
Non-small-cell lung carcinomaD002289——2————2
RecurrenceD012008——1————1
Brain neoplasmsD001932EFO_0003833C711————1
Central nervous system neoplasmsD016543——1————1
MedulloblastomaD008527——1————1
Head and neck neoplasmsD006258——1————1
Myelodysplastic syndromesD009190—D461————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
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 1,277 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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