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defosbarasertib
- Development stage
- Phase 2
- Lead developer
- AstraZeneca
- Modality
- Nanoparticles → Drug Delivery Systems, Small Molecules
- Administration
- Intravenous
01
Overview
Defosbarasertib (formerly known as AZD2811) is a potent and selective small-molecule inhibitor of Aurora kinase B (AURKB), a serine-threonine kinase involved in the regulation of chromosome segregation and cytokinesis during mitosis. By inhibiting AURKB activity, defosbarasertib disrupts phosphorylation of histone H3 at serine 10, leading to mitotic failure with polyploidy and cell death in cancer cells. The drug has been developed using nanoparticle encapsulation technology to improve pharmacokinetics and reduce toxicity compared to earlier formulations. Defosbarasertib is being investigated primarily for the treatment of advanced solid tumors, small cell lung cancer (SCLC), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL). It was originally developed by AstraZeneca in collaboration with BIND Therapeutics; Pfizer later joined as a developer[1][3][4][5][6][7].
- Other names
- defosbarasertibAZD2811 nanoparticleAZD-2811 nanoparticleAZD 2811 nanoparticle
02
Targets
AURKB (Aurora kinase B)AURKA (Aurora kinase A)
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