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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Clinical
Clinical Trials
20 clinical trials
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Indications Phases 4
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 1 | 1 | — | — | — | 2 |
| Triple negative breast neoplasms | D064726 | — | — | — | 1 | — | — | — | 1 |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | — | 1 | — | — | — | 1 |
| Ovarian epithelial carcinoma | D000077216 | — | — | — | 1 | — | — | — | 1 |
| Lung neoplasms | D008175 | — | C34.90 | — | 1 | — | — | — | 1 |
| Small cell lung carcinoma | D055752 | — | — | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Neoplasms | D009369 | — | C80 | 8 | — | — | — | — | 8 |
| Colorectal neoplasms | D015179 | — | — | 2 | — | — | — | — | 2 |
| Neoplasm metastasis | D009362 | EFO_0009708 | — | 2 | — | — | — | — | 2 |
| Non-small-cell lung carcinoma | D002289 | — | — | 2 | — | — | — | — | 2 |
| Recurrence | D012008 | — | — | 1 | — | — | — | — | 1 |
| Brain neoplasms | D001932 | EFO_0003833 | C71 | 1 | — | — | — | — | 1 |
| Central nervous system neoplasms | D016543 | — | — | 1 | — | — | — | — | 1 |
| Medulloblastoma | D008527 | — | — | 1 | — | — | — | — | 1 |
| Head and neck neoplasms | D006258 | — | — | 1 | — | — | — | — | 1 |
| Leukemia | D007938 | — | C95 | 1 | — | — | — | — | 1 |
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | PREXASERTIB |
| INN | prexasertib |
| 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 class | serine/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-ID | 1234015-52-1 |
| RxCUI | — |
| ChEMBL ID | CHEMBL3544911 |
| ChEBI ID | — |
| PubChem CID | — |
| DrugBank | — |
| UNII ID | 820NH671E6 (ChemIDplus, GSRS) |
Target
Agency Approved
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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
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Safety
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