Leslie Lawrence Anderson

US Patent:

43394264, Jul 13, 1982

Filed:

Mar 18, 1980

Appl. No.:

6/131685

Inventors:

Claude F. Meares - Davis CA
Leslie D. Anderson - Davis CA

Assignee:

Regents of the University of California - Berkeley CA

International Classification:

A61K 4900
A61K 4300

US Classification:

424 1

Abstract:

Bleomycin's affinity for tumorous tissue and its ability to complex with cobalt has lead to its use in vivo as a complex with. sup. 57 Cobalt. This complex has given excellent tumor images and has been useful for diagnostic purposes. Unfortunately,. sup. 57 Co has the undesirable property of a 270 day half-life. The present invention provides a bleomycin analog which has a powerful meal-chelating substituent covalently bound to and chemically modifying a bleomycin. However, the inclusion of this chelating substituent in the bleomycin analog does not significantly modify the in vivo biological properties thereof with respect to unmodified bleomycin. The inventive bleomycin analog forms stable chelates with a variety of metal ions, and is particularly useful when labelled with radionuclides having short half-lives. So labelled, the bleomycin analog may be utilized for diagnostic purposes.