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Pertuzumab

A humanized monoclonal antibody is being developed in collaboration with Roche. Pertuzumab is the first in a new class of targeted anticancer agents known as HER2 dimerization inhibitors (HDIs) and is designed to block the dimerization of HER2 with other HER proteins.^11,12

Inhibition of HER2 dimerization may prevent abnormal activation of HER-mediated intracellular signaling cascades in cancer cells.¹¹ Preclinical studies have identified HER dimerization as a key step in the ability of cells to independently proliferate, regardless of HER2 overexpression.¹¹ These preclinical studies suggest that pertuzumab may be an effective anticancer strategy in tumors with either normal or elevated expression of HER2.¹¹

1. Pertuzumab is a humanized monoclonal antibody designed to bind to the extracellular dimerization domain of HER2-a region essential for HER protein pairing.¹³

   

2. Pertuzumab, the first in a new class of targeted anticancer therapeutic agents known as HDIs, is designed to bind to HER2 and prevent it from forming homo- or heterodimers with any other HER family member.^12,13

   

3. HER2 is the preferred dimerization partner in the activation of HER signaling. Preclinical studies have shown that inhibition of HER2 dimer pairs may prevent the activation of several intracellular signaling cascades that can drive carcinogenesis, including the PI3K/Akt and Ras/Raf/MEK/MAPK pathways.¹³

   

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