Compounds and Methods for Tumor-Specific Targeting

Summary A novel strategy for developing cancer-homing drugs has been developed by Dr. Amin Kassis that combines Enzyme-Mediated Cancer Imaging and Therapy (EMCIT) with radionuclides (see figure below). This powerful method achieves a multimodal effect, since it can be exploited for therapeutic efficacy as well as tumor imaging. The technology exploits molecular database mining, chemistry, and biology to generate accumulation of radionuclides only at sites of tumor growth. EMCIT capitalizes on the tumor-specific secretion of extracellular hydrolases and proteases that reside principally in the tumor pericellular microenvironment, with only a small percentage diffusing out of the tumor bed. A concentration gradient is then formed, with the highest concentration existing pericellular to the tumor. Water-soluble, cell membrane impermeable, RadioActive Prodrugs (RAPs) have been chemically designed in silico to become water-insoluble following clipping by these tumor-specific catabolic enzymes (e.g., alkaline phosphatase).

Applications RAPs can be employed via EMCIT to target any solid tumor, whether it is a primary neoplasm or disseminated metastatic lesion. Consequently, this therapeutic strategy has broad utility. The relevant patient population incidence is staggering, as is the opportunity for capturing a significant share of the pharmaceutical market for cancer therapy, since the mainstay of cancer treatment, chemotherapy, has no specific targeting features, is toxic, and is frequently ineffective due to multidrug resistance. The expectation is that sales of drugs prescribed for treating breast cancer will increase by 10% annually for the next 5-7 years, attaining $6 billion by 2009. Hormone-refractory prostate cancer represents a large unmet medical need, and any treatment found effective against this disease or other advanced cancers that are poorly responsive to chemotherapy will have a wide market. For Further Information Please Contact the Director of Business Development Katie Gordon Email: katherine_gordon@hms.harvard.edu Telephone: (617) 432-0920

Inventor(s): Kassis, Amin I.

Type of Offer: Licensing



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