In vivo
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Treosulfan (L-threitol-1,4-bismethanesulfonate, Ovastat) was tested on human renal tumor cells growing as xenografts in athymic nude mice and as monolayers in vitro, in comparison with clinically used cytostatic drugs (in vivo, cyclophosphamide, vinblastine, and 5-fluorouracil; in vitro, vinblastine and 5-fluoro-2'-deoxyuridine) which were administered at equitoxic or equivalent dose levels, respectively. Four human renal tumor xenografts (N-U 2, N-U 26, MRI-H 121, KTCTL-1M) were investigated in vivo, and seven renal tumor cell lines (KTCTL-1M, KTCTL-2, KTCTL-26A, KTCTL-30, KTCTL-84, MRI-H 121, N-U 2) under in vitro conditions. The investigations of the four human renal tumor xenografts revealed that treosulfan is capable of inducing pronounced growth inhibitions ranging from 60-100% in comparison with untreated control tumors. ⋯ These results reveal the remarkable antitumor efficacy of treosulfan towards human renal-cell carcinomas, especially under in vivo conditions. This activity was similarly high or even better than in cyclophosphamide and vinblastine. The in vitro data obtained in monolayer cultures also confirmed the remarkable antiproliferative activity of treosulfan in renal tumor cells, but did not mirror very well the pattern of antitumor activity observed in vivo.