Drug intelligence / Profile preview

AZD2811 + azacitidine

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous (AZD2811), Intravenous Or Subcutaneous (azacitidine; Note: Most Trials Co-administer Both Intravenously)
01

Overview

This is a **combination drug** consisting of AZD2811 and azacitidine. - **AZD2811** is a potent, selective small-molecule inhibitor of Aurora kinase B, a key regulator of mitosis. AZD2811 is formulated as a nanoparticle for intravenous administration and is being developed primarily for the treatment of hematological malignancies, especially acute myeloid leukemia (AML). - **Azacitidine** is a nucleoside metabolic inhibitor and DNA methyltransferase inhibitor that incorporates into DNA and RNA, resulting in hypomethylation and disruption of abnormal gene expression. - The combination is under clinical investigation for synergistic antileukemic effects that stem from concomitant inhibition of cell-cycle progression (via Aurora kinase B inhibition by AZD2811) and epigenetic modulation (via DNA methyltransferase inhibition by azacitidine). - Preclinical studies have shown enhanced efficacy of the combination compared to either agent alone in AML models. - Developed for patients not eligible for intensive induction therapy, the combination is being trialed in relapsed/refractory or newly diagnosed AML.

Other names
AZD2811 nanoparticle + azacitidineAZD2811/azacitidine
02

Targets

DNMT3A (DNA methyltransferase 3 alpha)AURKB (Aurora kinase B)DNMT1 (DNA (cytosine-5)-methyltransferase 1)DNMT3B (DNA (cytosine-5)-methyltransferase 3B)

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