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Synonyms: 2C4 | Omnitarg® (obsolete trade name) | Perjeta®
pertuzumab is an approved drug (FDA (2012), EMA (2013))
Compound class:
Antibody
Comment: Annotated peptide sequences for this antibody are available in its IMGT/mAB-DB record.
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  |
| Used for the treatment of HER2 overexpressing breast cancer, in combination with trastuzumab and docetaxel. |
| Mechanism Of Action and Pharmacodynamic Effects |
| Pertuzumab binds to the ERBB2 (HER2) receptor at the domain that facilitates dimerisation with HER3 and prevents heterodimer formation [1,3]. HER2-HER3 heterodimers are most the potent HER2 complexes that are involved in EGF pathway activation in HER2 positive tumour cells [4]. Pertuzumab's action reduces activation of downstream pro-proliferative signalling pathways [2] and ultimately slows cancer cell growth. In contrast, trastuzumab binds to the HER2-HER2 dimerisation domain and prevents homodimers from forming. Thus treatment with pertuzumab plus trastuzumab mounts a double-pronged attack on EGF-mediated proliferation signals in HER2 positive cancer cells. |
| External links |
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For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |
