barasertib

Barasertib is an investigational, orally bioavailable small molecule that acts as a dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor, specifically targeting Aurora B kinase. Upon administration, it is rapidly converted in plasma to its active form, barasertib-HQPA. Barasertib exhibits high selectivity and potency for Aurora B kinase (IC50 ~0.37 nM), with much lower activity against Aurora A and other kinases. Inhibition of Aurora B disrupts chromosome alignment during mitosis, prevents cell division, induces polyploidy and apoptosis in tumor cells. Barasertib has been studied primarily for the treatment of acute myeloid leukemia (AML), solid tumors including small-cell lung cancer (SCLC), lymphoma, and other malignancies. It was developed by AstraZeneca but clinical development for AML was discontinued after phase III trials[1][2][3][4].

Other names

barasertib-HQPA2-(ethyl(3-((4-((5-(2-((3-fluorophenyl)amino)-2-oxoethyl)-1h-pyrazol-3-yl)amino)quinazolin-7-yl)oxy)propyl)amino)ethyl dihydrogen phosphate