zenocutuzumab   Click here for help

GtoPdb Ligand ID: 13649

Synonyms: Bizengri® | MCLA-128 | PB4188 [3] | R040517 | zenocutuzumab-zbco
Approved drug
zenocutuzumab is an approved drug (FDA (2024))
Compound class: Antibody
Comment: Zenocutuzumab (MCLA-128) is a humanized IgG1 bispecific anti-epidermal growth factor receptor 2/3 (HER2/HER3) monoclonal antibody [2-3]. It prevents binding of the ligand neuregulin 1 (NRG1) to HER3 and this suppresses HER2/HER3 dimerization, phosphorylation and downstream signalling [8]. Genetic NRG1 fusions have been identified as oncogenic drivers in a small number of tumour types [4,6]. Zenocutuzumab-mediated modulation inhibits signalling through the PI3K-AKT-mTOR pathway and reduces tumour cell growth and invasiveness. Low fucose glycoengineering enhances zenocutuzumab's antibody-dependent cellular cytotoxicity (ADCC) activity.
Click here for help
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
erb-b2 receptor tyrosine kinase 3 Hs Antibody Antagonist 10.5 pEC50 - 3
pEC50 10.5 (EC50 3.5x10-11 M) [3]
Description: Inhibition of NRG1-driven growth of N87 carcinoma cells