Pertuzumab: a new agent in HER2-positive breast cancer Data from preclinical and clinical studies

摘要

Pertuzumab is a humanized monoclonal antibody against HER2 receptor. Overexpression of HER2 in tumors confers a poor prognosis. Receptor dimerization with other HER family members is an essential requirement for the activity of HER2. Interestingly, the primary property of pertuzumab is to inhibit HER2 dimerization. Clinical activity of pertuzumab has been shown in patients with HER2-positive metastatic breast cancer who received pertuzumab plus trastuzumab plus docetaxel: pertuzumab was given at a fixed loading dose of 840 mg followed by 420 mg every 3 weeks until disease progression. This optimal dosing regimen has been based on the results of preclinical and, phase I and II clinical studies. Furthermore, a population pharmacokinetic model has shown that the serum concentration of pertuzumab was similar with fixed-, body surface area-, and weight based-dosing, supporting the use of a fixed dose of pertuzumab. This review aims at describing the main results of the studies that have supported the optimal dosing regimen.