Drug intelligence / Profile preview

KN046 + ningetinib

Development stage
Preclinical
Lead developer
AlphaMab Oncology
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

KN046 + ningetinib is an experimental **combination therapy** consisting of two distinct agents with complementary mechanisms of action targeting malignant disease. KN046 is a bispecific humanized antibody that simultaneously targets **programmed death ligand 1 (PD-L1)** and **cytotoxic T lymphocyte antigen-4 (CTLA-4)**, blocking both pathways to restore and enhance T cell-mediated antitumor responses[1][3][4][6][7]. It is produced as a single-domain antibody-Fc fusion protein designed to combine the activity of immune checkpoint blockade with reduced toxicity compared to the combination of separate checkpoint inhibitors. Ningetinib (often referred to as ningetinib tosylate or CT-053) is a **novel small molecule tyrosine kinase inhibitor** targeting multiple kinases, most notably **FLT3, AXL, MerTK, VEGFR2, and c-Met**[2][5]. It is primarily under investigation for activity against cancers with kinase pathway dysregulation, including acute myeloid leukemia (AML) with FLT3 mutations and certain solid tumors. Combined, this regimen brings together an immune checkpoint bispecific antibody (KN046) and a broad-spectrum tyrosine kinase inhibitor (ningetinib) for potentially synergistic antitumor effects.

Other names
ningetinib tosylateCT-053CT053CT 053
02

Targets

AXL (AXL receptor tyrosine kinase)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)CD274 (Programmed cell death protein 1 ligand 1)VEGFR2 (Vascular endothelial growth factor receptor 2)MET (Mesenchymal-epithelial transition factor receptor)MERTK (MER proto-oncogene, tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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