What if you could inhibit HER2 dimerization and further disrupt the oncogenic cascade? HER2+ breast cancer is an aggressive and complex disease.1 As our understanding of HER2+ disease evolves, we are finding that novel methods of targeting HER2 may offer a more comprehensive blockade of HER2 signaling.2 HER2 and dimerization HER2 dimerization, or receptor pairing, is a critical driver of tumor growth.3 When HER2 is overexpressed, as in HER2+ disease, it promotes excessive dimerization leading to overactive oncogenic signaling.1 Learn more HER2:HER3—The most potent oncogenic HER pair Although HER2 can dimerize with any HER receptor, preclinical studies suggest that HER2:HER3 is the most potent oncogenic HER pair.4 HER2 activates the MAPK (mitogen-activated protein kinase) pathway, causing cell proliferation, while HER3 activates the PI3K (phosphatidylinositol 3-kinase) pathway, leading to cell survival signaling.1,5-7 Available HER2-targeted agents do not block HER2 receptor ligand-induced dimerization, thus potentially allowing for continued HER signaling.2 Learn more Learn more about the potential of HER2 Dimerization Inhibitors (HDIs) Inhibition of ligand-induced HER2 dimerization in HER2+ disease while administering other HER2-targeted agents may offer a more comprehensive blockade of signaling.2   Visit ResearchHDIs.com   to watch an animated video and explore more. References: 1. Jones KL, Buzdar AU. Evolving novel anti-HER2 strategies. Lancet Oncol. 2009;10:1179-1187. 2. Nahta R, Yu D, Hung MC, et al. Mechanisms of disease: understanding resistance to HER2-targeted therapy in human breast cancer. Nat Clin Pract Oncol. 2006;3:269-280. 3. Arpino G, Gutierrez C, Weiss H, et al. Treatment of human epidermal growth factor receptor 2-overexpressing breast cancer xenografts with multiagent HER-targeted therapy. J Natl Cancer Inst. 2007;99:694-705. 4. Amin DN, Sergina N, Ahuja D, et al. Resiliency and vulnerability in the HER2-HER3 tumorigenic driver. Sci Transl Med. 2010;2:16ra7. 5. M�nard S, Tagliabue E, Campiglio M, Pupa SM. Role of HER2 gene overexpression in breast carcinoma. J Cell Physiol. 2000;182:150-162. 6. Holbro T, Civenni G, Hynes NE. The ErbB receptors and their role in cancer progression. Exp Cell Res. 2003;284:99-110. 7. Koutras AK, Fountzilas G, Kalogeras KT, et al. The upgraded role of HER3 and HER4 receptors in breast cancer. Crit Rev Oncol Hematol. 2010;74:73-78. Privacy Policy | Terms and Conditions | Contact Genentech® This e-mail is intended for U.S. healthcare professionals only. Genentech USA, Inc. 1 DNA Way South San Francisco, CA 94080-4990 © 2011 Genentech USA, Inc. All rights reserved. To unsubscribe from the Genentech BioOncology mailing list, please click here. BIO0000647400