Available Technology

BSA 01-10: Halogenated Carboranyl Porphyrins for Imageable Tumor-Targeting Agents for Radiation Therapy

Improvement in the efficacy of conventional radiotherapy using chemical agents is a key area of interest in experimental radiation oncology. Approximately one million patients in the US receive radiation therapy for cancer per year. Success has been limited due to restriction of the tumor dose to avoid normal tissue morbidity. Radiation sensitizing agents targeting hypoxic cells in tumors, which are several times less sensitive to radiation than oxygenated cells, have been particularly elusive. The compounds of this invention are particularly useful for purposes of radiation sensitization.
Patent Abstract: 
Halogenated and nitrated tetraphenylporphyrins and their use as imageable tumor-targeting agents for ionizing and/or non-ionizing radiation therapy are disclosed. Halogenated tetracarboranylporphyrins of the present invention are octahalogen analogs of the carborane-containing tetraphenylporphyrins previously known. Tests in animals hae shown that the carboranylporphyrins of the present invention provide low toxicity and high tumor accumulation of the described porphyrins. In addition to their use in a variety of cancer treatment modalities, the halogenated or nitrated carboranylporphyrins are imageable by a number of different methods.
All previous attempts to develop highly effective, non-toxic radiation sensitizing agents have been unsuccessful. These agents readily accumulate in neoplastic tissue and their electron withdrawing character makes them particularly attractive as radiation sensitizers. Other modes of cancer therapy are enabled with these compounds - including boron neutron capture therapy and photodynamic therapy. A particularly favorable aspect of these compounds includes their use as imaging agents to enhance treatment planning and treatment monitoring.
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