Herceptin® (Trastuzumab)

Full Prescribing Information, including Boxed Warnings

Herceptin is a humanized monoclonal antibody (also called a biologic therapy). Antibodies are part of the body's normal defense against bacteria, viruses and abnormal cells such as cancer cells. Therapeutic monoclonal antibodies are created and produced in a laboratory through a complex and resource-intensive process. Their name comes from the fact that they are produced from a single cell.¹

Herceptin works on both the extracellular and the intracellular domains of the HER2 receptor:^2-5

• Continuously suppresses HER2 activity that may lead to tumor proliferation³
• Leads to cell stasis and death³
• In preclinical studies, synergy with Herceptin enhanced the effects of chemotherapy^4,6,7
• Herceptin provides constant inhibition of the HER2 receptor
  • Extended half-life enables Herceptin to maintain constant exposure

Mechanism of Action of Herceptin^3-5,8-10

View Herceptin full prescribing information, including BOXED WARNINGS.

Administration

• Herceptin can be administered in a physician's office.
• The recommended dose for HER2-positive metastatic breast cancer is a loading dose of 4 mg/kg of Herceptin administered over a 90-minute period and subsequent weekly infusions of 2 mg/kg administered over a 30-minute period. Herceptin is given as a weekly infusion until disease progression.
• The recommended dose for the adjuvant treatment of HER2-positive breast cancer is a loading dose of 4 mg/kg of Herceptin administered over a 90-minute period and subsequent weekly infusions of 2 mg/kg administered over a 30-minute period. Herceptin is given concurrently with paclitaxel for 12 weeks and without paclitaxel for an additional 40 weeks. Herceptin should not be administered concurrently with doxorubicin (anthracyclines) and cyclophosphamide.
• Dosing should be modified for infusion reactions and cardiomyopathy.

 

¹ Carter P, Presta L, Gorman CM, et al. Humanization of an anti-p185HER2 antibody for human cancer therapy. Proc Natl Acad Sci. 1992;89:4285-4289.

² Sliwkowski MX, Lofgren JA, Lewis GD, Hotaling TE, Fendly BM, Fox JA. Nonclinical studies addressing the mechanism of action of trastuzumab (Herceptin). Semin Oncol. 1999;26:60-70.

³ Yakes FM, Chinratanalab W, Ritter CA, King W, Seelig S, Arteaga CL. Herceptin-induced inhibition of phosphatidyli-nositol-3 kinase and Akt is required for antibody-mediated effects on p27, cyclin D1, and antitumor action. Cancer Research. 2002;62:4132-4141.

⁴ Arnould L, Gelly M, Penault-Llorca F. Trastuzumab-based treatment of HER2-positive breast cancer: an antibody-dependent cellular cytotoxicity mechanism? Br J Cancer. 2006;94:259-267.

⁵ Bianco AR. Targeting c-erb2 and other receptors of the c-erB family: rationale and clinical applications. J Chemother. 2004;16:52-54.

⁶ Pegram MD, Konecny GE, O'Callaghan C, Beryt M, Pietras R, Slamon DJ. Rational combinations of trastuzumab with chemotherapeutic drugs used in the treatment of breast cancer. J Nat Cancer Inst. 2004;96:739-749.

⁷ Baselga J, Norton L, Albanell J, Kim Y-M, Mendelsohn J. Recombinant humanized anti-HER2 antibody (HerceptinTM) enhances the antitumor activity of paclitaxel and doxorubicin against HER2/neu overexpressing human breast cancer xenografts. Cancer Res. 1998;58:2825-2831.

⁸ Lewis GD, Figari I, Fendly B. Differential responses of human tumor cell lines to anti-p185HER2 monoclonal antibodies. Cancer Immunol Immunother. 1993;37:255-263.

⁹ Yarden Y. Biology of HER2 and its importance in breast cancer. Oncology. 2001;61:1-13.

¹⁰ Harari D, Yarden Y. Molecular mechanisms underlying ErbB2/HER2 action in breast cancer. Oncogene. 2000;19:6102-6114.