pertuzumab   Click here for help

GtoPdb Ligand ID: 5046

Synonyms: 2C4 | Omnitarg® (obsolete trade name) | Perjeta®
Approved drug
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.
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No information available.
Summary of Clinical Use Click here for help
Used for the treatment of HER2 overexpressing breast cancer, in combination with trastuzumab and docetaxel.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
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.
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