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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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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
Clinical Trials
18 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
NeoplasmsD009369C8061———7
Breast neoplasmsD001943EFO_0003869C5011———2
Ovarian neoplasmsD010051EFO_0003893C56—2———2
RhabdomyosarcomaD01220811———1
Desmoplastic small round cell tumorD05840511———1
Triple negative breast neoplasmsD064726—1———1
Small cell lung carcinomaD055752—1———1
Prostatic neoplasmsD011471C61—1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Central nervous system neoplasmsD0165432————2
Colorectal neoplasmsD0151792————2
Myeloid leukemia acuteD015470C92.02————2
Non-small-cell lung carcinomaD0022892————2
Brain neoplasmsD001932EFO_0003833C711————1
MedulloblastomaD0085271————1
Head and neck neoplasmsD0062581————1
Neoplasm metastasisD009362EFO_00097081————1
Myelodysplastic syndromesD009190D461————1
Myelomonocytic leukemia chronicD015477C93.11————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 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)
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 CID46700756
DrugBankDB12008
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
11200
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
O96017
Mouse ortholog
Chek2 (50883)
serine/threonine-protein kinase Chk2 (Q9Z265)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 513 documents
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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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