Drug intelligence / Profile preview

AZD0466

Development stage
Discontinued
Lead developer
AstraZeneca
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

AZD0466 is a drug-dendrimer conjugate designed for cancer therapy. It consists of the dual BCL-2/BCL-xL inhibitor AZD4320 covalently attached to a proprietary 5-generation pegylated poly-L-lysine dendrimer via a hydrolytically labile linker. This design allows for gradual release of the active inhibitor, aiming to induce apoptosis in cancer cells by inhibiting anti-apoptotic proteins BCL-2 and BCL-xL. The drug has shown pro-apoptotic and antineoplastic activity in preclinical models, including efficacy against venetoclax-resistant tumors. It is administered intravenously and was developed primarily for hematologic malignancies such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL), as well as solid tumors[1][2][3][4][5][7].

02

Targets

BCL2L1 (B-cell lymphoma-extra large protein)

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