Use of ¹¹¹in‐bleomycin for combining radiotherapy and chemotherapy on glioma‐bearing mice

Abstract

Mice bearing transplanted glioma received 0.9% NaCl, 0.1 mg of BLM, or 200-250 microCi of 111In-BLM (0.1 mg BLM) daily for 5 days intraperitoneally. After therapy, tumor sizes were in the order NaCl greater than BLM greater than 111In-BLM. On the 11th day after the first injection, tumor size (mm3) in the 111In-BLM group was 1,220; in the BLM group, it was 2,310 (P less than .025). After intratumor injection of a total dose of 0.1 mg of BLM/gm tumor weight, or of 1 mCi/gm tumor weight of 111In-BLM (carried by 0.1 mg of BLM/gm tumor weight), the tumor size decreased in the 111In-BLM group more than in the BLM group. On the 5th day after the 2nd dose therapy, the tumor size in the 111In-BLM group was 2,020; in the BLM group it was 4,220 (P less than .05). Host weights for these two groups were similar. The necrotic area in the tumor was much greater in the 111In-BLM group than in the BLM group. These results suggest the use for radiotherapy and chemotherapy.

Targeting the Nucleus: An Overview of Auger-Electron Radionuclide Therapy

“…The cytotoxicity of 111 In-BLMC has been demonstrated in human small cell lung cancer and head-and-neck carcinoma cell lines [120][121][122]. Moreover, in glioma-or head-and-neck-tumour xenograft bearing nude mice, 111 In-BLMC diminished tumour size better than unlabelled BLMC [123][124][125]. 111 In-BLMC is stable in vitro and in vivo and because it does not bind to transferrin, it does not cause toxicity to the bone marrow [117,[126][127][128].…”

Distribution of 111 in‐bleomycin complex in small cell lung cancer cells by autoradiography

“…Our results in animal experiments and gel electrophoresis indicate that '' 'In-BLM [4], ' "In-BLM-A2, or -B2 [5] were stable in vivo and that "'In-BLM was an effective compound for therapy of mouse glioma [6]. However, this conventional ' I 'In-BLM binds to transferrin, which is distributed throughout the body such that the ' ' In-BLM yield a high whole body dose, thereby limiting its practical value in the clinic.…”

Kinetics of111In-labeled bleomycin in patients with brain tumors: Compartmental vs. non-compartmental models

“…22 The binding of indium-111 labeled bleomycin complex ( I I I In-BLMC) has been studied in mice tumors and cell lines. 23 The initial distri -b u t i o n o f t 1 I In-BLMC is reported to be similar to that of cobalt-labeled bleomycin with a fast clearance from the blood into other organs and tissues, an early uptake in the kidneys, and excretion of a large part during the first 24-48 h. 24,25 Recently radiolabeled bleomycin complexes have been used as tracers in the diagnosis and staging of human head and neck cancers. 26 Huhmar et al 27 have preliminarily reported ... In-BLMC to be a useful SPECT tracer for the grading of human gliomas.…”