Disease relevance of RP-170

• RESULTS: RP-170 showed neither signs of toxicity nor significant alterations in glucose metabolism in brain or tumor at doses up to 4 g/kg b.w. up to 4 h [1].
• Hypoxia also reduced the surviving fraction of the cells treated either with RP-170 alone or with RP-170 plus heat [2].
• Hyperthermia enhances the cytotoxicity against hypoxic cells of RP-170, a new 2-nitroimidazole nucleoside hypoxic cell sensitizer [2].

High impact information on RP-170

• SER at 5% LD50 doses of RP-343, RP-170 and etanidazole was 1.66, 1.59 and 1.56 [3].
• The lower toxicity of RP-343 was supported by its lower concentrations in the brain; the RP-343 AUC for brain was 0.43 times that of RP-170 [3].
• Radiosensitization by 2-nitroimidazole nucleoside analog RP-170: radiosensitizing effects under both intravenous and oral administration [4].
• The radiosensitizing activity, pharmacokinetics and toxicity of RP-170, 2-nitroimidazole nucleoside analog, were investigated and compared with those of etanidazole (SR-2508) [4].
• These results might suggest the potential usefulness of KU-2285 and RP-170 in clinical radiotherapy [5].

Chemical compound and disease context of RP-170

• Although RP-170 does not show any advantages over etanidazole in terms of sensitization or toxicity, RP-170 might be preferable under certain circumstances because it can be given orally [6].
• At the same toxicity levels, RP-343 was found to have better sensitization of solid tumors over both etanidazole and RP-170 [3].

Biological context of RP-170

• Moreover, LD50 in mice of RP-170 (4.3 g/kg on i.v.) was increased to 5.2 g/kg by oral administration [4].
• The maximum tumor concentration/AUC for brain (Cmax,tumor/AUCbrain) ratios for RP-343 and RP-170 were 9.62 and 3.98 [3].

References