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patritumab deruxtecan   Click here for help

GtoPdb Ligand ID: 14121

Synonyms: HER3-DXd | MK-1022 | U3-1402
Immunopharmacology Ligand
Compound class: Antibody
Comment: Patritumab deruxtecan (MK-1022; HER3-DXd) is an anti-Erb-B2 receptor tyrosine kinase 3 (ERBB3; HER3) antibody-drug conjugate. The conjugate is a camptothecin derivative that inhibits topoisomerase I activity to kill tumour cells [5]. HER3 is a key dimerisation partner for HER receptors. Antibody binding induces rapid receptor internalisation and inhibits HER signalling.
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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
References
1. Arnett SO, Teillaud JL, Wurch T, Reichert JM, Dunlop C, Huber M. (2011)
IBC's 21st Annual Antibody Engineering and 8th Annual Antibody Therapeutics International Conferences and 2010 Annual Meeting of the Antibody Society. December 5-9, 2010, San Diego, CA USA.
MAbs, 3 (2): 133-52. [PMID:21304271]
2. Forveille S, Zhao L, Sauvat A, Cerrato G, Leduc M, Doffe F, Pan Y, Liu P, Kroemer G, Kepp O. (2025)
Patritumab deruxtecan induces immunogenic cell death.
Oncoimmunology, 14 (1): 2514050. [PMID:40458967]
3. Le Rhun E, Franceschi E, Weller M. (2025)
TUXEDO-3: A phase 2 trial of patritumab deruxtecan for patients with leptomeningeal metastasis.
Neuro Oncol, [Epub ahead of print]. [PMID:40461013]
4. Li C, Brand TM, Iida M, Huang S, Armstrong EA, van der Kogel A, Wheeler DL. (2013)
Human epidermal growth factor receptor 3 (HER3) blockade with U3-1287/AMG888 enhances the efficacy of radiation therapy in lung and head and neck carcinoma.
Discov Med, 16 (87): 79-92. [PMID:23998444]
5. Steuer CE, Hayashi H, Su WC, Nishio M, Johnson ML, Kim DW, Massarelli E, Felip E, Gold KA, Murakami H et al.. (2025)
Patritumab Deruxtecan (HER3-DXd; MK-1022) in Non-Small Cell Lung Cancer After Platinum-Based Chemotherapy and Immunotherapy.
J Clin Oncol, 43 (25): 2816-2826. [PMID:40554742]