Drug intelligence / Profile preview

barasertib + cytarabine

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous
01

Overview

barasertib + cytarabine is a combination therapy evaluated primarily for **acute myeloid leukemia (AML)**, particularly in elderly or relapsed patients ineligible for intensive chemotherapy. Barasertib, also known as AZD1152, is a highly selective and reversible ATP-competitive inhibitor of **Aurora kinase B**. It impairs mitosis by inhibiting chromosomal alignment and segregation, leading to polyploidy and apoptosis in cancer cells. Cytarabine (also known as cytosine arabinoside or ara-C) is a pyrimidine nucleoside analog that is converted intracellularly to ara-CTP and inhibits DNA synthesis, exerting cytotoxic effects selectively during the S-phase of the cell cycle. The combination exploits the complementary cell-cycle specificities of both agents, with barasertib targeting the M-phase and cytarabine the S-phase of leukemic cells. Studies show that the combination exhibits greater anti-leukemic effects than either agent alone in preclinical and early clinical studies. The primary developer and sponsor of clinical studies was AstraZeneca[2][3][6][9].

Other names
AZD1152 + cytosine arabinosidebarasertib + LDACbarasertib + ara-C
02

Targets

AURKA (Aurora kinase A)AURKB (Aurora kinase B)AURKC (Aurora kinase C)DNA polymerase family

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