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Synonyms: HER3-DXd | MK-1022 | U3-1402
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.
Ligand Activity Visualisation ChartsThese 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. ✖ |
| No information available. |
Summary of Clinical Use  |
| Patritumab deruxtecan (MK-1022; HER3-DXd) was advanced to clinical evaluations in advanced solid tumours, in particular for EGFR-mutant NSCLC. The unconjugated monoclonal (U3-1287) has also been extensively studied for clinical efficacy in lung, head and neck and breast cancers [4]. |
| Clinical Trials | |||||
| Clinical Trial ID | Title | Type | Source | Comment | References |
| NCT06596694 | Study of Patritumab Deruxtecan in Participants With Gastrointestinal Cancers (MK-1022-011) (HERTHENA-PanTumor02) | Phase 1/Phase 2 Interventional | Merck Sharp & Dohme LLC | ||
| NCT07060807 | A Clinical Study of Patritumab Deruxtecan to Treat Breast Cancer (MK-1022-016) | Phase 3 Interventional | Merck Sharp & Dohme LLC | ||
| NCT05338970 | HERTHENA-Lung02: A Study of Patritumab Deruxtecan Versus Platinum-based Chemotherapy in Metastatic or Locally Advanced EGFRm NSCLC After Failure of EGFR TKI Therapy | Phase 3 Interventional | Daiichi Sankyo | ||
| NCT00000189 | Gepirone vs Placebo in Treatment of Cocaine Dependence - 3 | Phase 2 Interventional | University of Pennsylvania | 3 | |
| NCT03260491 | U3-1402 in Metastatic or Unresectable Non-Small Cell Lung Cancer | Phase 1 Interventional | Daiichi Sankyo | 5 | |
| NCT05865990 | HER3-DXd in Breast Cancer and NSCLC Brain Metastases and Solid Tumor Leptomeningeal Disease | Phase 2 Interventional | MedSIR | 3 | |
