Drug intelligence / Profile preview

letaplimab + azacitidine

Development stage
Unknown
Lead developer
Innovent Biologics
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

Letaplimab (IBI188) is a fully human monoclonal antibody that targets the CD47 antigen on tumor cells, developed by Innovent Biologics. By binding to CD47, it blocks the CD47-SIRPα signaling pathway, inhibiting the "Don't Eat Me" signal and promoting phagocytosis of tumor cells by macrophages. Azacitidine is a small molecule chemotherapeutic agent classified as a demethylation agent or antimetabolite; it works by helping bone marrow produce normal blood cells and killing abnormal cells through interference with DNA synthesis and repair. The combination of letaplimab and azacitidine is under investigation as a first-line treatment for newly diagnosed higher-risk myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML)[2][5][6][8]. Letaplimab’s mechanism includes antibody-dependent cell cytotoxicity and T lymphocyte stimulation[8], while azacitidine acts primarily via DNA hypomethylation.

Other names
human anti-CD47 monoclonal antibody (IBI188)AZA
02

Targets

CD47 (Cluster of Differentiation 47)DNMT (DNA methyltransferase)

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