IDEA #6IKQAQ Synthetic strategies to Anticancer Antibody-Drug Conjugates Based on Gold Compounds. Application for the treatment of Cancer. 19A0002

Key Words: cancer, antibody drug conjugates, gold, Trastuzumab, phosphane, N-heterocyclic carbenes This invention’s purpose is the development of novel targeted chemotherapeutics for the treatment of cancer based on gold compounds. This invention improves the delivery of these drugs so that they can be efficiently released at the specific tumor site without affecting healthy tissues. More specifically, the invention describes synthetic procedures to prepare antibody drug conjugates containing gold compounds. While these strategies can be applied to different antibodies, the preliminary data we have is for Trastuzumab (HerceptinTM, Genentech) a humanised IgG1 mAb which has been exploited successfully as both a therapeutic agent and radiotracer. Its main use in cancer therapy has been for breast cancer. Our in vitro preliminary data is for breast cancer cell lines.