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BSA 02-06: Halogenated Carboranyl Porphyrins as Radiosensitizers

BNL Reference Number: BSA 02-06

Patent Status: U.S. Patent Number 6,759,403 was issued on July 6, 2004

Summary
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Halogenated Carboranyl Tetraphenyl Porphyrin

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.

Description

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.

Benefits

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.

Applications and Industries

The addition of a radiation sensitizing agent to the cancer therapeutic repertoire of an oncology-focused company will be of significant value. The fact that these compounds provide enhanced treatment planning guidance and treatment monitoring potential creates further value.

Journal Publication
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For more information about this technology, contact Christine Brakel, (631) 344-7134.

Tags: cancer, imaging

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