barasertib-hqpa

Barasertib-HQPA (AZD1152-HQPA) is the pharmacologically active metabolite of barasertib (also known as AZD1152), a small molecule, highly selective inhibitor of **Aurora B kinase** (Ki ≈ 0.36 nM), with much lower activity against Aurora A and C kinases[1][5][7]. After administration, the prodrug barasertib is rapidly converted in plasma to barasertib-HQPA via phosphatase-mediated cleavage. Barasertib-HQPA suppresses proliferation in cancer cells by inhibiting Aurora B kinase, resulting in impaired histone H3 phosphorylation, mitotic failure, disrupted chromosome alignment, accumulation of polyploid cells, and induction of apoptosis[1][2][3][6]. It has demonstrated **antitumor activity** in preclinical models of colon, lung, and hematological cancers, especially acute myeloid leukemia (AML), and it has shown limited clinical activity in early-phase trials of AML and advanced solid tumors, with neutropenia as a primary dose-limiting toxicity[4][8]. The agent was being developed by AstraZeneca primarily for cancer indications, particularly **acute myeloid leukemia**, but late-stage clinical development was discontinued[5].

Other names

barasertib-hydroxyquinazoline pyrazol anilideAZD1152-HQPAAZD-1152-HQPAAZD 1152-HQPA