Overview

Generic Name(s):
barasertib
NCI Definition [1]:
An orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152-hydroxyquinazoline pyrazol anilide (AZD1152-HQPA) with potential antineoplastic activity. Upon administration and rapid conversion from the prodrug form in plasma, AZD1152-HQPA specifically binds to and inhibits Aurora kinase B, which results in the disruption of spindle checkpoint functions and chromosome alignment and, so, the disruption of chromosome segregation and cytokinesis. Consequently, cell division and cell proliferation are inhibited and apoptosis is induced in Aurora kinase B-overexpressing tumor cells. Aurora kinase B, a serine/threonine protein kinase that functions in the attachment of the mitotic spindle to the centromere, is overexpressed in a wide variety of cancer cell types.

Barasertib has been investigated in 2 clinical trials, of which 1 is open and 1 is closed. Of the trials investigating barasertib, 1 is phase 1/phase 2 (0 open) and 1 is phase 2 (1 open).

Acute myeloid leukemia and small cell lung carcinoma are the most common diseases being investigated in barasertib clinical trials [2].

Drug Details

Synonyms [2]:
aurora kinase inhibitor azd1152, 1h-pyrazole-3-acetamide, 5-((7-(3-(ethyl(2-(phosphonooxy)ethyl)amino)propoxy)-4-quinazolinyl)amino)-n-(3-fluorophenyl)-, barasertib, azd-1152, azd1152, azd1152-hqpa, azd 1152, aurora kinase inhibitor azd1152, azd-2811, azd 2811, azd2811
Drug Categories [2]:
Serine/threonine kinase inhibitors
Drug Target(s) [2]:
AURKB
NCIT ID [1]:
C62502

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.