GlaxoSmithKline plc has announced the submission of a New Drug Application (NDA) to the US Food and Drug Administration (FDA) for approval to market Tykerb (lapatinib ditosylate), in combination with Xeloda (capecitabine), for the treatment of advanced or metastatic HER2 (ErbB2) positive breast cancer in women who have received prior therapy, including Herceptin (trastuzumab). The compound has been granted Fast track status by the FDA in this patient population. TYKERB is a small molecule dual kinase inhibitor developed by GSK as an oral therapy, and is currently being investigated in breast cancer and other solid tumours. TYKERB is an investigational drug and has not been approved for marketing by any regulatory body.

"This filing is the result of many years of tremendous research and development work by the scientists at GSK. It is truly an outstanding milestone, especially for the many thousands of women who are facing the devastating effects of advanced breast cancer," said Paolo Paoletti, MD, senior vice president of the Oncology Medicine Development Centre at GSK. "Many of these women are desperately in need of alternative treatments, and this filing demonstrates that we have turned the corner toward a new era of targeted agents."

GSK plans to submit the Marketing Authorization Application (MAA) for Tykerb in Europe during the 4th quarter of this year.

Tykerb, a small molecule that is administered orally, inhibits the tyrosine kinase components of EGFR (ErbB1) and HER2 receptors. Stimulation of EGFR and HER2 is associated with cell proliferation and with multiple processes involved in tumour progression, invasion, and metastases. Over expression of these receptors has been reported in a variety of human tumours and is associated with poor prognosis and reduced overall survival.


GSK is using advanced technologies, including pharmacogenetics, to better define patient populations that may respond to Tykerb.