Pertuzumab (Perjeta)

FDA approved 6/8/2012.

General information

Class/mechanism: Humanized monoclonal antibody that binds to the extracellular dimerization subdomain II of HER2, preventing dimerization with other HER receptors (i.e. EGFR/HER1, HER3, and HER4). Pertuzumab inhibits ligand-initiated intracellular signaling via the MAP (mitogen-activated protein) kinase and PI3K (phosphoinositide 3-kinase) pathways, which results in cell growth arrest and apoptosis. Also stimulates antibody-dependent cell-mediated cytotoxicity (ADCC).

Route: IV
Extravasation: no information

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the package insert.

Diseases for which it is used

• Breast cancer

Clinical trials

• CLEOPATRA trial
• NeoSphere trial

Patient drug information

• Pertuzumab (Perjeta) patient drug information (Chemocare)
• Pertuzumab (Perjeta) patient drug information
• Brief patient counseling information can be found on page 16 of the package insert
• Pertuzumab (Perjeta) patient drug information (UpToDate)

History of changes in FDA indication

• 6/8/2012: FDA approved "for use in combination with trastuzumab and docetaxel for the treatment of patients with HER2-positive metastatic breast cancer who have not received prior anti-HER2 therapy or chemotherapy for metastatic disease."

Also known as

2C4, Omnitarg, Rhumab 2C4.