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.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
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Summary of Clinical Use Click here for help
The FDA approved (within their accelerated approval scheme) zenocutuzumab on 4th December 2024 [1], to treat advanced unresectable/metastatic pancreatic adenocarcinoma or non-small cell lung cancer (NSCLC) that carry a neuregulin 1 (NRG1) gene fusion.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03321981 MCLA-128 With Trastuzumab/Chemotherapy in HER2+ and With Endocrine Therapy in ER+ and Low HER2 Breast Cancer. Phase 2 Interventional Merus N.V.
NCT05588609 Study Evaluating Zenocutuzumab in Patients with or Without Molecularly Defined Cancers Phase 2 Interventional Merus N.V.
NCT02912949 A Study of Zenocutuzumab (MCLA-128) in Patients With Solid Tumors Harboring an NRG1 Fusion (eNRGy) Phase 2 Interventional Merus N.V. 5,7