Pertuzumab

Pertuzumab, a humanized IgG1 monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer. IC50 & Target:EGFR^[1] In Vitro: Trastuzumab and Pertuzumab are highly synergistic inhibitors of BT474 breast cancer cell survival. The combination of trastuzumab and Pertuzumab mediates a loss of up to 60% of cells at doses in which individual drugs do not alter cell survival. The combination of trastuzumab and Pertuzumab reduces the percentage of proliferating (S-phase) cells by more than 2-fold. A combination of trastuzumab and Pertuzumab inhibits cell proliferation and survival to a greater degree than does either agent alone^[1]. In Vivo: In Calu-3 NSCLC xenografts, monotherapy with pertuzumab or trastuzumab is able to significantly inhibit tumor growth, with treatment-to-control ratios (TCR) of 0.23 and 0.27, respectively. The combination of trastuzumab and pertuzumab produces a dramatically enhanced antitumor activity compared with single-agent treatments (TCR 0.05, resulting in tumor regression and, in 3 of 10 animals, complete tumor remission). Treatment of KPL-4 breast cancer xenografts with either trastuzumab or pertuzumab inhibits tumor growth with TCRs of 0.67 and 0.65, respectively. Pertuzumab maintains antitumor activity after progression on trastuzumab^[2].