BLEDTA: Tumor localization by a bleomycin analogue containing a metal-chelating group

Leslie H. DeRiemer, Claude F. Meares, David A. Goodwin, Carol I. Diamanti

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Abstract

Two different Co(III) complexes of the antitumor antibiotic bleomycin have been prepared, and their in vivo distribution in mice has been investigated. The more thermodynamically stable of the Co(III)-bleomycin complexes has been modified by reaction with the bifunctional chelating agent 1-(p-bromoacetamidophenyl)ethylenedinitrilotetraacetic acid, to give a bleomycin derivative (BLEDTA) containing a powerful metal-chelating group. BLEDTA was radiolabeled with 111In(III) and its in vivo distribution in mice was examined. The potential of 111In-labeled BLEDTA as a tumor-visualizing agent was also investigated in humans with biopsy-proven cancers, predominantly (70%) squamous carcinoma of the head and neck. All of the 29 patients studied had at least one clinically proven site of the disease visualized with 111In-BLEDTA. These clinical results are significantly better than results we obtained in a comparable group of patients using directly labeled 111In-bleomycin and are similar to those reported by Nouel for 57Co-bleomycin [GANN Monogr. Cancer Res., 19, 301 (1976)].

Original languageEnglish (US)
Pages (from-to)1019-1023
Number of pages5
JournalJournal of Medicinal Chemistry
Volume22
Issue number9
StatePublished - 1979

ASJC Scopus subject areas

  • Organic Chemistry

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    DeRiemer, L. H., Meares, C. F., Goodwin, D. A., & Diamanti, C. I. (1979). BLEDTA: Tumor localization by a bleomycin analogue containing a metal-chelating group. Journal of Medicinal Chemistry, 22(9), 1019-1023.