In vivo radiosensitization efficacy of KU-2285 and etanidazole at clinically relevant low radiation doses

Journal Article · Tue Nov 30 23:00:00 EST 1993 · International Journal of Radiation Oncology, Biology and Physics; (United States)

DOI:https://doi.org/10.1016/0360-3016(93)90532-Z· OSTI ID:6857424

Oya, Natsuo; Shibamoto, Yuta; Sasai, Keisuke; Abe, Mitsuyuki; Sugiyama, Taketoshi ^[1]

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1. Kyoto Univ. (Japan)

The in vivo radiosensitization efficacy of KU-2285 (a fluorinated nitroimidazole derivative) at clinically relevant low radiation doses (2-4 Gy) was compared with that of etanidazole using four types of assays with EMT6, SCCVII, and C[sup 3]H mammary tumors. The in vivo-in vitro cytokinesis-block micronucleus assay and the chromosomal aberration assay were used to assess the sensitizing effect at single doses of 2-4 Gy. After in vivo treatment for tumors, tumor cells were cultured in the presence of cytochalasin B for the former assay or demecolcine for the latter assay, and the micronucleus frequency in binucleate cells and the chromosomal frequency in metaphase cells were evaluated after 42 hr and 3 hr of culture. In addition, an in vivo-in vitro colony assay and a growth delay assay were performed using fractionated irradiation regimens (4 Gy [times] 5). The sensitizer enhancement ratio for 100-400 mg/kg of KU-2285 was between 1.12 and 1.42. KU-2285 was a more efficient sensitizer than etanidazole in 3 of 9 experiments and as efficient as etanidazole in the remaining six experiments. Both the micronucleus assay and the chromosomal aberration assay appeared to be very useful in evaluating the in vivo sensitizing effect at low radiation doses. KU-2285 had a definite radiosensitizing effect even at low radiation doses, and clinical trials of KU-2285 may be warranted. 23 refs., 5 figs., 1 tab.

• OSTI ID: 6857424
• Journal Information: International Journal of Radiation Oncology, Biology and Physics; (United States), Journal Name: International Journal of Radiation Oncology, Biology and Physics; (United States) Vol. 27:5; ISSN IOBPD3; ISSN 0360-3016
• Country of Publication: United States
• Language: English

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