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found this on the net..
Advances in Breast Cancer
New Molecular “Linker” May Increase Potency of Trastuzumab While Lowering Toxicity
Perhaps one of the biggest breakthroughs in breast cancer treatment over the past decade was the discovery of trastuzumab (Herceptin), a drug that specifically targets HER2-expressing cancer cells, an indication of an aggressive form of breast cancer likely to spread elsewhere in the body. Dosing, however, is often limited because of toxicity. Early phase I trials are underway to study the effect of a “linker” combination of compounds that may deliver trastuzumab more directly into malignant cells with less damage to healthy tissue. “A number of compounds have failed when the 'linker' has become unstable during IV drug delivery while avoiding uptake in normal cells,” Dr. Howard A. Burris III of the Sarah Cannon Research Institute of Nashville, Tennessee said during his presentation. In one small phase I trial, 24 patients aged 35 to 70 were given trastuzumab-DM1 (T-DM1), with a linker molecule (a derivative of maytansine). “The MCC linker molecule has been engineered to provide a stable bond between trastuzumab and DM1 to potentially enhance the therapeutic window of DM1 by minimizing systemic exposure to free DM1 and improving exposure to T-DM1,” Dr. Burris said, calling the antitumor activity observed in patients “quite incredible”, even in some patients with liver and lung metastases.
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