Ac-HEHA and Related Compounds, Methods of Synthesis and Methods of Use
Description of Invention:
The invention is directed to a chelation complex comprising 225Actinium (225Ac) and 1,4,7,10,13,16- hexaazacyclohexadecane-N, N',N'',N''',N'''',N'''''-hexaacetic acid (HEHA) as well as bi-functional complexes consisting of 225Ac, HEHA and targeting agents in various combinations. Radioisotopes are chosen, in part, by the type of disease to be treated, and two important functions are tissue penetration of the emitted particles and the toxicity of the treatment agents. 225Ac, an alpha-emitter, offers high cytotoxicity with a short tissue range, and HEHA chelates 225Ac in such a manner as to provide increased in vivo stability to enable its use as a radiotherapeutic agent. Additionally, 225Ac's radioactive decay chain ends in a non-radioactive material. A targeting agent can be conjugated to 225Ac-HEHA in order to selectively affect a defined population of cells through a receptor, a substrate, an antigenic determinant or any other binding site on the target cell population. Therefore, the invention yields improvements over existing related technologies for the radiotherapeutic treatment of disease states such as cancer. The disclosed complexes could also be used in radioimaging, decontamination and detoxification protocols.
Inventors:
Martin W. Brechbiel and Kim A. Deal (NCI)
Patent Status:
DHHS Reference No. E-071-1999/0 --
U.S. Patent No. 6,696,551 issued 24 Feb 2004
U.S. Patent No. 6,995,247 issued 07 Feb 2006
Portfolios: Cancer
Cancer -Therapeutics
For Additional Information Please Contact: Mojdeh Bahar J.D.
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: (301)435-2950
Email: baharm@mail.nih.gov
Fax: (301) 402-0220
